PMID-sentid	Pub_year	Sent_text	compound_name	comp_offset	prot_official_name	organism	prot_offset
9618706-8	1998	Some antihistamines (i.e., levocabastine, terfenadine, loratadine, azelastine and oxatomide) can reduce ICAM-1 expression.	azelastine	67-77	intercellular adhesion molecule 1	Homo sapiens	104-110
9482706-9	1998	Only theophylline and azelastine (both at 10(-4) M or more) were able to inhibit EPO release by both C5a and FMLP.	azelastine	22-32	eosinophil peroxidase	Homo sapiens	81-84
9482706-9	1998	Only theophylline and azelastine (both at 10(-4) M or more) were able to inhibit EPO release by both C5a and FMLP.	azelastine	22-32	complement C5a receptor 1	Homo sapiens	101-104
9482706-9	1998	Only theophylline and azelastine (both at 10(-4) M or more) were able to inhibit EPO release by both C5a and FMLP.	azelastine	22-32	formyl peptide receptor 1	Homo sapiens	109-113
9585822-1	1998	The efficacy and safety of the nasally administered histamine H1 receptor blocking drug Azelastine was investigated in an open, multicenter, randomized comparative trial with Ebastine in seasonal allergic rhinitis.	azelastine	88-98	histamine receptor H1	Homo sapiens	52-73
9585152-5	1998	Azelastine inhibited TNF-alpha release at concentrations lower than those needed for the inhibition of degranulation.	azelastine	0-10	tumor necrosis factor	Rattus norvegicus	21-30
9585152-6	1998	In antigen-stimulated cells, azelastine also inhibited equipotently TNF-alpha mRNA expression/protein synthesis, TNF-alpha release and Ca2+ influx.	azelastine	29-39	tumor necrosis factor	Rattus norvegicus	68-77
9585152-6	1998	In antigen-stimulated cells, azelastine also inhibited equipotently TNF-alpha mRNA expression/protein synthesis, TNF-alpha release and Ca2+ influx.	azelastine	29-39	tumor necrosis factor	Rattus norvegicus	113-122
9585152-7	1998	In ionomycin-stimulated cells, however, azelastine inhibited TNF-alpha release to a greater extent than TNF-alpha mRNA expression/protein synthesis and Ca2+ influx, indicating that azelastine inhibits the release process more potently than transcription or production of TNF-alpha by interfering with a signal other than Ca2+.	azelastine	40-50	tumor necrosis factor	Rattus norvegicus	61-70
9585152-4	1998	We compared the effects of azelastine, an anti-allergic drug, on TNF-alpha secretion, on Ca2+ signal, and on degranulation in an antigen- or ionomycin-stimulated rat mast RBL-2H3 cell line.	azelastine	27-37	tumor necrosis factor	Rattus norvegicus	65-74
9506001-1	1997	Azelastine, an antihistamine with additional pharmacologic properties, was evaluated for a possible influence on pharmacokinetic and electrocardiographic parameters due to its coadministration with CYP3A4 inhibitor ketoconazole (200 mg every 12 hrs).	azelastine	0-10	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	198-204
9431823-0	1997	Inhibitory effect of azelastine hydrochloride on synthesis and release of platelet activating factor from human alveolar macrophages.	azelastine	21-45	PCNA clamp associated factor	Homo sapiens	74-100
9431823-1	1997	The effect of azelastine hydrochloride (azelastine) on synthesis and release of platelet activating factor (PAF) in alveolar macrophages obtained from asthmatic and non-asthmatic subjects was examined.	azelastine	14-38	PCNA clamp associated factor	Homo sapiens	80-106
9431823-1	1997	The effect of azelastine hydrochloride (azelastine) on synthesis and release of platelet activating factor (PAF) in alveolar macrophages obtained from asthmatic and non-asthmatic subjects was examined.	azelastine	14-38	PCNA clamp associated factor	Homo sapiens	108-111
9431823-1	1997	The effect of azelastine hydrochloride (azelastine) on synthesis and release of platelet activating factor (PAF) in alveolar macrophages obtained from asthmatic and non-asthmatic subjects was examined.	azelastine	14-24	PCNA clamp associated factor	Homo sapiens	80-106
9431823-1	1997	The effect of azelastine hydrochloride (azelastine) on synthesis and release of platelet activating factor (PAF) in alveolar macrophages obtained from asthmatic and non-asthmatic subjects was examined.	azelastine	14-24	PCNA clamp associated factor	Homo sapiens	108-111
9431823-4	1997	PAF activity released from alveolar macrophages (AMs) from asthmatics without preincubation of azelastine was 15.97 [2.17] (mean [SD], ng/10(7) cells) in supernatants and 42.52 [10.16] in cell pellets.	azelastine	95-105	PCNA clamp associated factor	Homo sapiens	0-3
9431823-5	1997	After preincubation with 10(-8), 10(-6), and 10(-4) M of azelastine, PAF activity reduced to 10.71 [2.73] (mean [SD], ng/10(7) cells), 7.86 [0.94], and 3.52 [0.31] in the supernatants, and 35.58 [7.37], 21.57 [4.36], and 14.77 [0.99] (n = 15) in the cell pellets, respectively.	azelastine	57-67	PCNA clamp associated factor	Homo sapiens	69-72
9431823-6	1997	PAF activity in non-asthmatic subjects without preincubation of azelastine was 8.55 [1.16] (mean [SD], ng/10(7) cells) in supernatants and 32.64 [3.37] in cell pellets.	azelastine	64-74	PCNA clamp associated factor	Homo sapiens	0-3
9431823-7	1997	After preincubation with 10(-8), 10(-6), and 10(-4) M of azelastine, PAF activity reduced to 6.68 [0.78] (mean [SD], ng/10(7) cells), 4.47 [0.51], and 2.97 [0.36] in the supernatants, and 29.53 [3.75], 14.78 [1.95], and 6.16 [0.55] (n = 20) in the cell pellets, respectively.	azelastine	57-67	PCNA clamp associated factor	Homo sapiens	69-72
9431823-8	1997	Our results showed that preincubation with azelastine caused a dose-dependent inhibition of intra- and extracellular PAF activity from asthmatic and non-asthmatic macrophages in the same manner.	azelastine	43-53	PCNA clamp associated factor	Homo sapiens	117-120
9506001-7	1997	Azelastine did not inhibit CYP3A4 activity but it did inhibit CYP2D6 and CYP2C19 activity with Ki values exceeding maximum plasma concentration by 120 to 800-fold.	azelastine	0-10	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	62-68
9506001-7	1997	Azelastine did not inhibit CYP3A4 activity but it did inhibit CYP2D6 and CYP2C19 activity with Ki values exceeding maximum plasma concentration by 120 to 800-fold.	azelastine	0-10	cytochrome P450 family 2 subfamily C member 19	Homo sapiens	73-80
9506001-8	1997	Therefore, in vitro tests and the absence of electrocardiographic effects suggests azelastine can be safely administered with CYP3A4 inhibitors.	azelastine	83-93	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	126-132
9365503-7	1997	Compatible with these in vivo results, Azeptin and PLM contradictively regulated protein tyrosine phosphorylation and c-myc mRNA expression in human gingival and mouse pulmonary fibroblasts.	azelastine	39-46	MYC proto-oncogene, bHLH transcription factor	Homo sapiens	118-123
9365503-8	1997	In addition, NF-kappa B was activated by fibroblast treatment with 5 micrograms/ml PLM for 1 h, but intranuclear NF-kappa B was decreased by cell treatment with 10(-5) M Azeptin.	azelastine	170-177	nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105	Mus musculus	113-123
9300717-0	1997	Suppression of TNF-alpha secretion by azelastine in a rat mast (RBL-2H3) cell line: evidence for differential regulation of TNF-alpha release, transcription, and degranulation.	azelastine	38-48	tumor necrosis factor	Rattus norvegicus	15-24
9300717-4	1997	In a rat mast RBL-2H3 cell line, azelastine inhibited Ag- and ionomycin-induced TNF-alpha release with IC50 values of 25.7 +/- 3.4 microM and 1.66 +/- 0.45 microM, respectively.	azelastine	33-43	tumor necrosis factor	Rattus norvegicus	80-89
9300717-6	1997	In Ag-stimulated cells, azelastine also inhibited TNF-alpha mRNA expression, TNF-alpha protein synthesis and release, and, possibly related to these effects, Ca2+ influx.	azelastine	24-34	tumor necrosis factor	Rattus norvegicus	50-59
9300717-6	1997	In Ag-stimulated cells, azelastine also inhibited TNF-alpha mRNA expression, TNF-alpha protein synthesis and release, and, possibly related to these effects, Ca2+ influx.	azelastine	24-34	tumor necrosis factor	Rattus norvegicus	77-86
9300717-7	1997	In ionomycin-stimulated cells, however, azelastine inhibited TNF-alpha release to a greater extent than mRNA expression/protein synthesis and Ca2+ influx, suggesting that azelastine inhibits the release process more potently than transcription or production of TNF-alpha by interfering with a signal other than Ca2+.	azelastine	40-50	tumor necrosis factor	Rattus norvegicus	61-70
9300717-8	1997	Azelastine added 1 h after ionomycin stimulation also immediately blocked subsequent release of TNF-alpha, which had been produced in the cells, without affecting Ca2+ influx.	azelastine	0-10	tumor necrosis factor	Rattus norvegicus	96-105
9074948-0	1997	Suppression by azelastine hydrochloride of NF-kappa B activation involved in generation of cytokines and nitric oxide.	azelastine	15-39	nuclear factor kappa B subunit 1	Homo sapiens	43-53
9209598-6	1997	Azelastine and oxatomide effectively reduced SP levels in nasal secretions (p < 0.005), but they did not significantly decrease VIP levels.	azelastine	0-10	tachykinin precursor 1	Homo sapiens	45-47
9146938-0	1997	Topical azelastine has a 12-hour duration of action as assessed by histamine challenge-induced exudation of alpha 2-macroglobulin into human nasal airways.	azelastine	8-18	alpha-2-macroglobulin	Homo sapiens	108-129
9146938-3	1997	OBJECTIVE: The present study, involving healthy subjects, examined the effect of topical azelastine on luminal entry of alpha 2-macroglobulin and symptoms evoked by repeat histamine challenges during 24 h. The effect was compared to a clinical dose of the oral anti-histamine cetirizine and to placebo treatments.	azelastine	89-99	alpha-2-macroglobulin	Homo sapiens	120-141
9074948-1	1997	The influence of the anti-allergy agent azelastine hydrochloride (Azeptin) on NF-kappa B activation associated with the generation of cytokines and nitric oxide (NO) was investigated in various kinds of human and mouse cells.	azelastine	40-64	nuclear factor kappa B subunit 1	Homo sapiens	78-88
9074948-1	1997	The influence of the anti-allergy agent azelastine hydrochloride (Azeptin) on NF-kappa B activation associated with the generation of cytokines and nitric oxide (NO) was investigated in various kinds of human and mouse cells.	azelastine	66-73	nuclear factor kappa B subunit 1	Homo sapiens	78-88
9074948-3	1997	Generation of tumor necrosis factor-alpha, interleukin 1-beta, granulocyte-macrophage colony-stimulating factor and interleukin-6 from 10(-5) M Azeptin-treated PBL and human monocytes (HM) was decreased to approximately 1/3 to 2/3 of the control levels.	azelastine	144-151	colony stimulating factor 2	Homo sapiens	63-111
9074948-3	1997	Generation of tumor necrosis factor-alpha, interleukin 1-beta, granulocyte-macrophage colony-stimulating factor and interleukin-6 from 10(-5) M Azeptin-treated PBL and human monocytes (HM) was decreased to approximately 1/3 to 2/3 of the control levels.	azelastine	144-151	interleukin 6	Homo sapiens	116-129
9195148-1	1997	This study compared a new intranasal anti-allergic drug, azelastine (0.56 mg bid) with intranasal beclomethasone (0.2 mg bid) and placebo in the treatment of symptoms associated with seasonal rhinitis.	azelastine	57-67	BH3 interacting domain death agonist	Homo sapiens	77-80
8977510-0	1996	Topical azelastine reduces eosinophil activation and intercellular adhesion molecule-1 expression on nasal epithelial cells: an antiallergic activity.	azelastine	8-18	intercellular adhesion molecule 1	Homo sapiens	53-86
9074948-6	1997	Being compatible with those results, Azeptin (10(-5) M) suppressed activation of NF-kappa B in PBL, HM and HF.	azelastine	37-44	nuclear factor kappa B subunit 1	Homo sapiens	81-91
9074948-7	1997	These results appear to indicate that suppression of cytokine and NO generation by Azeptin results at least partially from the inhibition of NF-kappa B activation.	azelastine	83-90	nuclear factor kappa B subunit 1	Homo sapiens	141-151
9315512-4	1997	10(-6) M azelastine inhibited PGE2 production in these IL-1-stimulated fibroblasts.	azelastine	9-19	interleukin 1 beta	Homo sapiens	55-59
8977510-13	1996	After azelastine administration, significant decreases in total symptom score, eosinophilic and neutrophilic infiltration, and ICAM-1 expression were observed during both early- and late-phase reactions.	azelastine	6-16	intercellular adhesion molecule 1	Homo sapiens	127-133
8630722-9	1996	CONCLUSION: Results indicated that oxatomide and ketotifen inhibit the production of leukotriene C4 and leukotriene B4 by inhibiting phospholipase A2 activity, whereas, azelastine inhibits the leukotriene C4 production by inhibiting phospholipase A2 and leukotriene C4 synthase.	azelastine	169-179	phospholipase A2 group IB	Rattus norvegicus	233-249
8977510-16	1996	CONCLUSION: Azelastine exerts antiallergic activity, mainly affecting eosinophil function and downregulating ICAM-1 expression, on nasal epithelial cells.	azelastine	12-22	intercellular adhesion molecule 1	Homo sapiens	109-115
8630722-9	1996	CONCLUSION: Results indicated that oxatomide and ketotifen inhibit the production of leukotriene C4 and leukotriene B4 by inhibiting phospholipase A2 activity, whereas, azelastine inhibits the leukotriene C4 production by inhibiting phospholipase A2 and leukotriene C4 synthase.	azelastine	169-179	leukotriene C4 synthase	Rattus norvegicus	254-277
8735853-6	1996	Oral terfenadine and cetirizine and intranasal levocabastine and azelastine have also demonstrated a lowering of ICAM-1 expression on epithelial cells.	azelastine	65-75	intercellular adhesion molecule 1	Homo sapiens	113-119
8741163-0	1996	Azelastine protects against CA1 traumatic neuronal injury in the hippocampal slice.	azelastine	0-10	carbonic anhydrase 1	Homo sapiens	28-31
8741163-3	1996	Therefore, we investigated whether azelastine, an anti-allergic agent inhibiting the synthesis and release of leukotrienes, could protect against CA1 traumatic neuronal injury in the hippocampal slice.	azelastine	35-45	carbonic anhydrase 1	Homo sapiens	146-149
8829888-1	1995	The efficacy and safety of the nasally administered histamine H1 receptor blocking drug azelastine was investigated in a randomized comparative trial with ebastine.	azelastine	88-98	histamine receptor H1	Homo sapiens	52-73
8595539-6	1996	For the azelastine 2 sprays bid group, the overall results were significant at P = .05 for the major symptom complex score and at .05 < P = .10 for the total symptom complex score versus placebo.	azelastine	8-18	BH3 interacting domain death agonist	Homo sapiens	28-31
7759463-9	1995	This profile suggests that azelastine may be a novel inhibitor of Ca(2+)-dependent translocation of 5-lipoxygenase from cytosol to the nuclear envelope or a FLAP inhibitor rather than a direct 5-LO inhibitor.	azelastine	27-37	arachidonate 5-lipoxygenase	Homo sapiens	100-114
7517981-6	1994	Thus, AZE exerts its in vitro immunosuppressive activity preferentially by interfering with the IL-2 responsiveness, with partial inhibition of IL-2 production.	azelastine	6-9	interleukin 2	Homo sapiens	96-100
7517981-6	1994	Thus, AZE exerts its in vitro immunosuppressive activity preferentially by interfering with the IL-2 responsiveness, with partial inhibition of IL-2 production.	azelastine	6-9	interleukin 2	Homo sapiens	144-148
8032630-12	1994	Oedema induced by ovalbumin (50 or 200 micrograms/paw) was also inhibited by azelastine.	azelastine	77-87	serine (or cysteine) peptidase inhibitor, clade B, member 1, pseudogene	Mus musculus	18-27
8105785-1	1993	The efficacy and safety of a new antiallergic drug, intranasal azelastine (CAS 58581-89-8), in the treatment of seasonal allergic rhinitis was investigated in a 16 patient double-blind comparison with placebo and another 36 patient open comparison with budesonide (CAS 51333-22-3).	azelastine	63-73	BCAR1 scaffold protein, Cas family member	Homo sapiens	75-78
8162343-0	1993	Inhibitory effect of azelastine, a potent antiallergic agent, on release of tumor necrosis factor-alpha from activated human peripheral blood mononuclear cells and U937 cells.	azelastine	21-31	tumor necrosis factor	Homo sapiens	76-103
8162343-2	1993	In the present study, we investigated whether azelastine, a potent antiallergic agent, affects release of TNF-alpha from peripheral blood mononuclear cells (PBMC) and U937 cell line in vitro.	azelastine	46-56	tumor necrosis factor	Homo sapiens	106-115
8162343-4	1993	TNF-alpha levels in the culture supernatant of PHA-stimulated human PBMC and TPA-activated U937 cells decreased in a dose-dependent manner when these cells were cultured in the presence of azelastine.	azelastine	189-199	tumor necrosis factor	Homo sapiens	0-9
8162343-6	1993	Moreover, azelastine also inhibited release of TNF-alpha from U937 cells which were already activated by TPA.	azelastine	10-20	tumor necrosis factor	Homo sapiens	47-56
8162343-7	1993	These results suggest that the inhibitory effect of azelastine on TNF-alpha release plays an important role in its antiallergic action in addition to inhibition and/or antagonism of histamine and leukotrienes, which has been previously reported.	azelastine	52-62	tumor necrosis factor	Homo sapiens	66-75
8021845-6	1994	Furthermore, the production of TNF-alpha and GM-CSF in lymphocytes was suppressed in the presence of Azelastine, and the drug protected sheep red blood cells and epithelial tumor cell lines against hydrogen peroxide impairment and hypotonic shock.	azelastine	101-111	tumor necrosis factor	Ovis aries	31-40
8021845-6	1994	Furthermore, the production of TNF-alpha and GM-CSF in lymphocytes was suppressed in the presence of Azelastine, and the drug protected sheep red blood cells and epithelial tumor cell lines against hydrogen peroxide impairment and hypotonic shock.	azelastine	101-111	granulocyte-macrophage colony-stimulating factor	Ovis aries	45-51
7684672-6	1993	Potent histamine H1-receptor antagonists (e.g. azelastine and levocabastine) are approved for local treatment and lead to prompt relief of troublesome symptoms.	azelastine	47-57	histamine receptor H1	Homo sapiens	7-28
8405089-4	1993	Azelastine 15 microM significantly protected CA1 evoked responses from hypoxic injury, with CA1 population spike amplitude recovering to a mean 76 +/- 13% in azelastine treated slices, compared to 4 +/- 3% recovery in paired unmedicated slices.	azelastine	0-10	carbonic anhydrase 1	Homo sapiens	45-48
1333407-1	1992	Azelastine (1-300 microM) inhibited contractions of isolated porcine trachea induced by high K+, carbachol and endothelin-1 (ET-1) with a decrease in [Ca2+]cyt (as measured by fura-2-fluorescence).	azelastine	0-10	endothelin 1	Homo sapiens	111-123
7679943-0	1993	Effect of azelastine on substance P content in bronchoalveolar and nasal lavage fluids of patients with allergic asthma.	azelastine	10-20	tachykinin precursor 1	Homo sapiens	24-35
7679943-1	1993	The study was carried out to investigate the effect of azelastine on the Substance P (SP) concentration in bronchoalveolar (BAL) and nasal (NAL) lavage obtained from atopic grass pollen asthmatics and non-atopic healthy subjects.	azelastine	55-65	tachykinin precursor 1	Homo sapiens	73-84
7679943-1	1993	The study was carried out to investigate the effect of azelastine on the Substance P (SP) concentration in bronchoalveolar (BAL) and nasal (NAL) lavage obtained from atopic grass pollen asthmatics and non-atopic healthy subjects.	azelastine	55-65	tachykinin precursor 1	Homo sapiens	86-88
7679943-4	1993	Azelastine pre-treatment resulted in a significant reduction of SP in baseline concentration of SP in BAL and NAL from asthmatics.	azelastine	0-10	tachykinin precursor 1	Homo sapiens	64-66
7679943-4	1993	Azelastine pre-treatment resulted in a significant reduction of SP in baseline concentration of SP in BAL and NAL from asthmatics.	azelastine	0-10	tachykinin precursor 1	Homo sapiens	96-98
8222744-0	1993	Inhibitory effects of azelastine hydrochloride on Ca2+ influx, actin polymerization and release of eosinophil cationic protein of an eosinophilic leukaemia cell line EoL-1.	azelastine	22-46	ribonuclease A family member 3	Homo sapiens	99-126
8222744-3	1993	Azelastine hydrochloride inhibited PAF-induced and fMLP-induced Ca2+ influx ([Ca2+]i) in a dose-dependent manner with an IC50 of 1 x 10(-8) M and 1 x 10(-7) M, respectively.	azelastine	0-24	formyl peptide receptor 1	Homo sapiens	51-55
8222744-7	1993	Azelastine hydrochloride inhibited the secretion of ECP in a dose-dependent manner.	azelastine	0-24	ribonuclease A family member 3	Homo sapiens	52-55
8381149-12	1993	Furthermore, drugs that share the ability to impair PAF-induced eosinophilia, including azelastine and cetirizine, prevented the inhibitory effect of PAF on the antigen-induced pleurisy.	azelastine	88-98	PCNA clamp associated factor	Rattus norvegicus	52-55
8381149-12	1993	Furthermore, drugs that share the ability to impair PAF-induced eosinophilia, including azelastine and cetirizine, prevented the inhibitory effect of PAF on the antigen-induced pleurisy.	azelastine	88-98	PCNA clamp associated factor	Rattus norvegicus	150-153
8366765-3	1993	Interleukin (IL)-2, IL-3 and IL-4 production from PBL in response to Concanavalin A stimulation was also strongly suppressed when the cells were cultured in the presence of AZ.	azelastine	173-175	interleukin 4	Homo sapiens	29-33
1333407-1	1992	Azelastine (1-300 microM) inhibited contractions of isolated porcine trachea induced by high K+, carbachol and endothelin-1 (ET-1) with a decrease in [Ca2+]cyt (as measured by fura-2-fluorescence).	azelastine	0-10	endothelin 1	Homo sapiens	125-129
1333407-9	1992	Azelastine partially inhibited the contraction induced by 0.3 microM Ca2+ but not the contraction induced by 3 microM Ca2+, and strongly inhibited the potentiating effects of DPB, carbachol and ET-1.	azelastine	0-10	endothelin 1	Homo sapiens	194-198
1353762-2	1992	Chiral resolution of racemic azelastine, an antiallergic drug, was achieved on a conalbumin-conjugated silica gel column.	azelastine	29-39	transferrin (ovotransferrin)	Gallus gallus	81-91
1680533-0	1991	Effect of azelastine and ketotifen on the bronchial and skin responses to platelet-activating factor in humans.	azelastine	10-20	PCNA clamp associated factor	Homo sapiens	74-100
1355732-18	1992	It was concluded that the ability of azelastine to antagonize histamine and PAF is important for its effectiveness against anaphylactic shock.	azelastine	37-47	PCNA clamp associated factor	Rattus norvegicus	76-79
1680533-1	1991	In a randomized, double-blind placebo-controlled study we investigated the effect of single oral doses of 8 mg azelastine and 2 mg ketotifen on the immediate response to platelet-activating factor (PAF) inhalation and to increasing doses of PAF injected intradermally.	azelastine	111-121	PCNA clamp associated factor	Homo sapiens	170-196
1680533-1	1991	In a randomized, double-blind placebo-controlled study we investigated the effect of single oral doses of 8 mg azelastine and 2 mg ketotifen on the immediate response to platelet-activating factor (PAF) inhalation and to increasing doses of PAF injected intradermally.	azelastine	111-121	PCNA clamp associated factor	Homo sapiens	198-201
1676876-0	1991	Influence of azelastine on IL-1 beta generation in vitro and IL-1 beta-induced effect in vivo.	azelastine	13-23	interleukin 1 beta	Mus musculus	27-36
1687465-3	1991	These basal values were decreased by azelastine with an IC50 value of 1.1 +/- 0.3 x 10(-4) M. Endothelin-1 (10(-7) M) induced a rapid increase in free cytosolic calcium up to 806 +/- 314 nM, which returned to normal levels in 3-5 min.	azelastine	37-47	endothelin-1	Oryctolagus cuniculus	94-106
1676876-4	1991	These findings suggest that azelastine is not an IL-1 antagonist but inhibits IL-1 synthesis and/or release in leukocytes.	azelastine	28-38	interleukin 1 complex	Mus musculus	78-82
1675571-7	1991	Azelastine (A-5610, CAS 58581-89-8) significantly inhibited the O2- generation from the adherent IFN gamma-treated U937 cells stimulated by fMLP or PMA in a dose-dependent manner.	azelastine	0-10	interferon gamma	Homo sapiens	97-106
1675571-7	1991	Azelastine (A-5610, CAS 58581-89-8) significantly inhibited the O2- generation from the adherent IFN gamma-treated U937 cells stimulated by fMLP or PMA in a dose-dependent manner.	azelastine	0-10	formyl peptide receptor 1	Homo sapiens	140-144
1663088-4	1991	We found that azelastine, one of the antiallergic drugs, and isoproterenol inhibited FMLP-induced O2- generation in a dose-dependent fashion, whereas the other drugs exhibited no such inhibitory action except at very high concentrations.	azelastine	14-24	formyl peptide receptor 1	Homo sapiens	85-89
1645817-2	1991	Aminophylline (20 micrograms/ml) and Isoproterenol (10 nM) inhibited PAF (3 X 10(-8) M)-induced eosinophil chemotaxis nearly 30%, whereas no inhibitory effects were observed by Dexamethasone (0.1 microM), Tranilast, Ketotifen or Azelastine.	azelastine	229-239	PCNA clamp associated factor	Homo sapiens	69-72
2288496-0	1990	[Suppressive effect of azelastine on the induction of Df antigen specific IL-2 responsiveness in lymphocytes from patients with bronchial asthma].	azelastine	23-33	interleukin 2	Homo sapiens	74-78
2288496-1	1990	Effect of azelastine on the induction of Dermatophagoides farinae (Df)-antigen specific IL-2 responsiveness of the lymphocytes was examined.	azelastine	10-20	interleukin 2	Homo sapiens	88-92
2288496-2	1990	Azelastine suppressed the induction of IL-2 responsiveness induced by Df antigen in peripheral blood mononuclear cells from patients with bronchial asthma in a dose dependent manner.	azelastine	0-10	interleukin 2	Homo sapiens	39-43
1676876-1	1991	The effects of the novel antiasthmatic/antiallergic compound azelastine on IL-1 beta were investigated in vitro and in vivo.	azelastine	61-71	interleukin 1 beta	Mus musculus	75-84
1976840-2	1990	Inhibitory effect of azelastine hydrochloride (AZ), which is known as an inhibitor of 5-lipoxygenase, on MDD was also evaluated.	azelastine	21-45	arachidonate 5-lipoxygenase	Rattus norvegicus	86-100
1976840-2	1990	Inhibitory effect of azelastine hydrochloride (AZ), which is known as an inhibitor of 5-lipoxygenase, on MDD was also evaluated.	azelastine	47-49	arachidonate 5-lipoxygenase	Rattus norvegicus	86-100
34445767-4	2021	Although the antihistamine effect of Aze is well documented, the involvement of the JNK pathway in its action remains to be elucidated.	azelastine	37-40	mitogen-activated protein kinase 8	Mus musculus	84-87
34445767-5	2021	This study investigated the effects of Aze on lipopolysaccharide (LPS)-induced JNK phosphorylation, pro-inflammatory mediators, and cell migration in BV2 microglial cells.	azelastine	39-42	mitogen-activated protein kinase 8	Mus musculus	79-82
34445767-6	2021	Aze was found to inhibit the LPS-induced phosphorylation of JNK and c-Jun.	azelastine	0-3	mitogen-activated protein kinase 8	Mus musculus	60-63
34445767-6	2021	Aze was found to inhibit the LPS-induced phosphorylation of JNK and c-Jun.	azelastine	0-3	jun proto-oncogene	Mus musculus	68-73
34445767-9	2021	Furthermore, Aze inhibited LPS-induced IkappaB phosphorylation, thereby suppressing nuclear translocation of NF-kappaB.	azelastine	13-16	nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105	Mus musculus	109-118
34445767-10	2021	Collectively, our data demonstrate that Aze exerts anti-inflammatory and anti-migratory effects through inhibition of the JNK/NF-kappaB pathway in BV2 cells.	azelastine	40-43	mitogen-activated protein kinase 8	Mus musculus	122-125
34445767-10	2021	Collectively, our data demonstrate that Aze exerts anti-inflammatory and anti-migratory effects through inhibition of the JNK/NF-kappaB pathway in BV2 cells.	azelastine	40-43	nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105	Mus musculus	126-135
34052578-0	2021	Azelastine inhibits viropexis of SARS-CoV-2 spike pseudovirus by binding to SARS-CoV-2 entry receptor ACE2.	azelastine	0-10	surface glycoprotein	Severe acute respiratory syndrome coronavirus 2	44-49
35344122-6	2022	The limits of detection were 0.014 and 0.010 microg mL-1 and limits of quantitation were 0.043 and 0.029 microg mL-1 for CTZ and AZE, respectively.	azelastine	129-132	L1 cell adhesion molecule	Mus musculus	112-116
2571246-0	1989	The effect of azelastine and some other antiasthmatic and antiallergic drugs on calmodulin and protein kinase C. The antiallergic and antiasthmatic drug, azelastine, interacts strongly with calmodulin (but not bovine serum albumin) as determined by an indirect assay; it also moderately inhibited the Ca2+-calmodulin-dependent enzyme bovine brain phosphodiesterase.	azelastine	154-164	calmodulin	Bos taurus	80-90
2571246-0	1989	The effect of azelastine and some other antiasthmatic and antiallergic drugs on calmodulin and protein kinase C. The antiallergic and antiasthmatic drug, azelastine, interacts strongly with calmodulin (but not bovine serum albumin) as determined by an indirect assay; it also moderately inhibited the Ca2+-calmodulin-dependent enzyme bovine brain phosphodiesterase.	azelastine	154-164	calmodulin	Bos taurus	190-200
2571246-0	1989	The effect of azelastine and some other antiasthmatic and antiallergic drugs on calmodulin and protein kinase C. The antiallergic and antiasthmatic drug, azelastine, interacts strongly with calmodulin (but not bovine serum albumin) as determined by an indirect assay; it also moderately inhibited the Ca2+-calmodulin-dependent enzyme bovine brain phosphodiesterase.	azelastine	154-164	calmodulin	Bos taurus	190-200
2571246-1	1989	Ketotifen was less active than azelastine in both assays of calmodulin reactivity and both drugs were less active than the recognized calmodulin inhibitor, W-7.	azelastine	31-41	calmodulin	Bos taurus	60-70
2469707-0	1989	Azelastine inhibits IgE-mediated human basophil histamine release.	azelastine	0-10	immunoglobulin heavy constant epsilon	Homo sapiens	20-23
2469707-2	1989	Azelastine was found to significantly inhibit anti-IgE-stimulated basophil histamine release.	azelastine	0-10	immunoglobulin heavy constant epsilon	Homo sapiens	51-54
2480337-2	1989	The 50% inhibitory concentrations (IC50) of the agent were approximately 1.0 x 10(-5) M. In addition, azelastine significantly inhibited also 5-lipoxygenase activity in peritoneal cells with an IC50 of 1.0 x 10(-5) M, but not on LTC4 synthetase, LTA4 hydrolase or phospholipase A2 activity.	azelastine	102-112	arachidonate 5-lipoxygenase	Homo sapiens	142-156
2480337-2	1989	The 50% inhibitory concentrations (IC50) of the agent were approximately 1.0 x 10(-5) M. In addition, azelastine significantly inhibited also 5-lipoxygenase activity in peritoneal cells with an IC50 of 1.0 x 10(-5) M, but not on LTC4 synthetase, LTA4 hydrolase or phospholipase A2 activity.	azelastine	102-112	leukotriene A4 hydrolase	Homo sapiens	246-260
2480337-2	1989	The 50% inhibitory concentrations (IC50) of the agent were approximately 1.0 x 10(-5) M. In addition, azelastine significantly inhibited also 5-lipoxygenase activity in peritoneal cells with an IC50 of 1.0 x 10(-5) M, but not on LTC4 synthetase, LTA4 hydrolase or phospholipase A2 activity.	azelastine	102-112	phospholipase A2 group IB	Homo sapiens	264-280
2890562-3	1987	The stimulations of arachidonic acid release by formyl-methionyl-leucyl-phenylalanine (FMLP) were effectively diminished by 20 microM of azelastine as well as clemastine.	azelastine	137-147	formyl peptide receptor 1	Homo sapiens	87-91
2413739-4	1985	At IC50 level azelastine was about 18, 23, 28 and 425 times as effective as astemizole, ketotifen (newer histamine H1-receptor antagonists), diphenhydramine (a traditional H1-receptor antagonist), and theophylline (a phosphodiesterase inhibitor), respectively.	azelastine	14-24	histamine receptor H 1	Rattus norvegicus	105-126
34445767-0	2021	Suppression of LPS-Induced Inflammation and Cell Migration by Azelastine through Inhibition of JNK/NF-kappaB Pathway in BV2 Microglial Cells.	azelastine	62-72	mitogen-activated protein kinase 8	Mus musculus	95-98
34445767-0	2021	Suppression of LPS-Induced Inflammation and Cell Migration by Azelastine through Inhibition of JNK/NF-kappaB Pathway in BV2 Microglial Cells.	azelastine	62-72	nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105	Mus musculus	99-108
34445767-2	2021	To explore potential JNK3 inhibitors from the U.S. Food and Drug Administration-approved drug library, we performed structure-based virtual screening and identified azelastine (Aze) as one of the candidates.	azelastine	165-175	mitogen-activated protein kinase 10	Mus musculus	21-25
35066955-0	2022	Superior effect of MP-AzeFlu compared to monotherapy with fluticasone propionate or azelastine on GILZ, MKP-1, and TTP anti-inflammatory gene expression in healthy and inflamed upper airway mucosa.	azelastine	84-94	TSC22 domain family member 3	Homo sapiens	98-102
35066955-0	2022	Superior effect of MP-AzeFlu compared to monotherapy with fluticasone propionate or azelastine on GILZ, MKP-1, and TTP anti-inflammatory gene expression in healthy and inflamed upper airway mucosa.	azelastine	84-94	dual specificity phosphatase 1	Homo sapiens	104-109
35066955-0	2022	Superior effect of MP-AzeFlu compared to monotherapy with fluticasone propionate or azelastine on GILZ, MKP-1, and TTP anti-inflammatory gene expression in healthy and inflamed upper airway mucosa.	azelastine	84-94	ZFP36 ring finger protein	Homo sapiens	115-118
35125346-8	2022	To validate the optimized trafficking assay, we carried out a pilot screen that identified three drugs (ibutilide, azaperone, and azelastine) as drugs that increase KV11.1 trafficking.	azelastine	130-140	potassium voltage-gated channel subfamily H member 2	Homo sapiens	165-171
3207972-8	1988	Verapamil, azelastine, diltiazem and TMB-8 (each 10 microM) significantly attenuated PLA2-induced AH.	azelastine	11-21	phospholipase A2 group IB	Rattus norvegicus	85-89
3394583-4	1988	Azelastine (10 nM-1 microM) caused dose-dependent potentiation of PIA-induced relaxation.	azelastine	0-10	RPTOR independent companion of MTOR complex 2	Homo sapiens	66-69
3394583-9	1988	Since asthmatics show increased hyperreagibility (bronchospasm) to inhalation of adenosine, the inhibition of PIA-induced contraction by azelastine indicates that the drug may be worthwhile in the treatment bronchial hyperreactivity in asthmatic patients.	azelastine	137-147	RPTOR independent companion of MTOR complex 2	Homo sapiens	110-113
3596819-7	1987	The potent inhibition by azelastine might be partly a result of the inhibition of 5-lipoxygenase, since 5-hydroxyeicosatetraenoic acid formation in rat basophilic leukemia cell homogenate was inhibited by azelastine.	azelastine	25-35	arachidonate 5-lipoxygenase	Rattus norvegicus	82-96
3596819-7	1987	The potent inhibition by azelastine might be partly a result of the inhibition of 5-lipoxygenase, since 5-hydroxyeicosatetraenoic acid formation in rat basophilic leukemia cell homogenate was inhibited by azelastine.	azelastine	205-215	arachidonate 5-lipoxygenase	Rattus norvegicus	82-96
34052578-0	2021	Azelastine inhibits viropexis of SARS-CoV-2 spike pseudovirus by binding to SARS-CoV-2 entry receptor ACE2.	azelastine	0-10	angiotensin converting enzyme 2	Homo sapiens	102-106
34052578-4	2021	Here, we discovered antihistamine azelastine has an affinity to ACE2 by cell membrane chromatography (CMC); Then we determined the equilibrium dissociation constant (KD) of azelastine-ACE2 as (2.58 +- 0.48) x 10-7 M by surface plasmon resonance (SPR).	azelastine	34-44	angiotensin converting enzyme 2	Homo sapiens	64-68
34052578-4	2021	Here, we discovered antihistamine azelastine has an affinity to ACE2 by cell membrane chromatography (CMC); Then we determined the equilibrium dissociation constant (KD) of azelastine-ACE2 as (2.58 +- 0.48) x 10-7 M by surface plasmon resonance (SPR).	azelastine	34-44	angiotensin converting enzyme 2	Homo sapiens	184-188
34052578-4	2021	Here, we discovered antihistamine azelastine has an affinity to ACE2 by cell membrane chromatography (CMC); Then we determined the equilibrium dissociation constant (KD) of azelastine-ACE2 as (2.58 +- 0.48) x 10-7 M by surface plasmon resonance (SPR).	azelastine	173-183	angiotensin converting enzyme 2	Homo sapiens	64-68
34052578-4	2021	Here, we discovered antihistamine azelastine has an affinity to ACE2 by cell membrane chromatography (CMC); Then we determined the equilibrium dissociation constant (KD) of azelastine-ACE2 as (2.58 +- 0.48) x 10-7 M by surface plasmon resonance (SPR).	azelastine	173-183	angiotensin converting enzyme 2	Homo sapiens	184-188
32615812-3	2020	10-DHGD showed comparatively lower effect.Conclusion: Anti-calcifying effect of azelastine might be related to upregulation of apo A (HDL-c) and downregulation of apo B mRNA expression indeed good modulator of aortic calcification.Impact Statement: Many studies have indicated that high-density lipoprotein-cholesterol (HDL-c) is inversely correlated with atherosclerotic plaque progression and could reduce cardiovascular disease risk.	azelastine	80-90	apolipoprotein B	Rattus norvegicus	163-168
33309272-7	2021	Although mechanisms by which specific antihistamines exert antiviral effects is not clear, hydroxyzine, and possibly azelastine, bind Angiotensin Converting Enzyme-2 (ACE2) and the sigma-1 receptor as off-targets.	azelastine	117-127	angiotensin converting enzyme 2	Homo sapiens	134-165
33309272-7	2021	Although mechanisms by which specific antihistamines exert antiviral effects is not clear, hydroxyzine, and possibly azelastine, bind Angiotensin Converting Enzyme-2 (ACE2) and the sigma-1 receptor as off-targets.	azelastine	117-127	angiotensin converting enzyme 2	Homo sapiens	167-171
33408784-0	2021	Anti-allergic drug azelastine suppresses colon tumorigenesis by directly targeting ARF1 to inhibit IQGAP1-ERK-Drp1-mediated mitochondrial fission.	azelastine	19-29	ADP ribosylation factor 1	Homo sapiens	83-87
33408784-0	2021	Anti-allergic drug azelastine suppresses colon tumorigenesis by directly targeting ARF1 to inhibit IQGAP1-ERK-Drp1-mediated mitochondrial fission.	azelastine	19-29	IQ motif containing GTPase activating protein 1	Homo sapiens	99-105
33408784-0	2021	Anti-allergic drug azelastine suppresses colon tumorigenesis by directly targeting ARF1 to inhibit IQGAP1-ERK-Drp1-mediated mitochondrial fission.	azelastine	19-29	mitogen-activated protein kinase 1	Homo sapiens	106-109
33408784-0	2021	Anti-allergic drug azelastine suppresses colon tumorigenesis by directly targeting ARF1 to inhibit IQGAP1-ERK-Drp1-mediated mitochondrial fission.	azelastine	19-29	utrophin	Homo sapiens	110-114
33408784-8	2021	ARF1 was identified as a direct target of azelastine.	azelastine	42-52	ADP ribosylation factor 1	Homo sapiens	0-4
33408784-11	2021	Mechanistically, azelastine bound to Thr-48 in ARF1 and repressed its activity, decreasing Drp1 phosphorylation.	azelastine	17-27	ADP ribosylation factor 1	Homo sapiens	47-51
33408784-11	2021	Mechanistically, azelastine bound to Thr-48 in ARF1 and repressed its activity, decreasing Drp1 phosphorylation.	azelastine	17-27	utrophin	Homo sapiens	91-95
32776923-6	2020	AZ significantly decreased the expression of H1R and the proinflammatory cytokine IL-1SS in the ex vivo system, which were shown to be augmented by histamine addition.	azelastine	0-2	histamine receptor H1	Mus musculus	45-48
32615812-7	2020	Our findings showed that azelastine ameliorated aortic calcification and increased apoA expression along with a decline in apo B.	azelastine	25-35	apolipoprotein B	Rattus norvegicus	123-128
30079805-6	2019	Among the top-ranked drugs, azelastine, a selective histamine H1 receptor antagonist, showed the best binding affinity of -9.3 kcal/mol and showed interactions with several key residues of the acetyl lysine binding pocket.	azelastine	28-38	histamine receptor H1	Homo sapiens	52-73
29378195-6	2018	Histamine repressed while (H1) receptor antagonist azelastine increased apo A-I protein and mRNA levels within 48 h in a dose-dependent manner.	azelastine	51-61	apolipoprotein A1	Homo sapiens	72-79
31262903-0	2019	Histamine Receptor Antagonists, Loratadine and Azelastine, Sensitize P-gp-overexpressing Antimitotic Drug-resistant KBV20C Cells Through Different Molecular Mechanisms.	azelastine	47-57	ATP binding cassette subfamily B member 1	Homo sapiens	69-73
31262903-6	2019	Azelastine had a higher P-glycoprotein (P-gp)-inhibitory activity, similar to that of verapamil, indicating that sensitization by vincristine-azelastine involved the P-gp-inhibitory effects of azelastine.	azelastine	0-10	ATP binding cassette subfamily B member 1	Homo sapiens	24-38
31262903-6	2019	Azelastine had a higher P-glycoprotein (P-gp)-inhibitory activity, similar to that of verapamil, indicating that sensitization by vincristine-azelastine involved the P-gp-inhibitory effects of azelastine.	azelastine	0-10	ATP binding cassette subfamily B member 1	Homo sapiens	40-44
31262903-6	2019	Azelastine had a higher P-glycoprotein (P-gp)-inhibitory activity, similar to that of verapamil, indicating that sensitization by vincristine-azelastine involved the P-gp-inhibitory effects of azelastine.	azelastine	0-10	ATP binding cassette subfamily B member 1	Homo sapiens	166-170
31262903-6	2019	Azelastine had a higher P-glycoprotein (P-gp)-inhibitory activity, similar to that of verapamil, indicating that sensitization by vincristine-azelastine involved the P-gp-inhibitory effects of azelastine.	azelastine	142-152	ATP binding cassette subfamily B member 1	Homo sapiens	166-170
31183371-8	2019	Conclusions: Our study revealed for the first time that second-generation antihistamines, including cetirizine, fexofenadine, azelastine, and terfenadine, exert suppressive effects on lymphocyte Kv1.3-channels.	azelastine	126-136	potassium voltage-gated channel, shaker-related subfamily, member 3	Mus musculus	195-200
30721669-9	2019	The anti-proliferation effects of bepridil and azelastine on the cell lines with mutated and deleted p53 implied some p53-independent anti-proliferation effects.	azelastine	47-57	tumor protein p53	Homo sapiens	101-104
30721669-9	2019	The anti-proliferation effects of bepridil and azelastine on the cell lines with mutated and deleted p53 implied some p53-independent anti-proliferation effects.	azelastine	47-57	tumor protein p53	Homo sapiens	118-121
30574167-9	2018	Results: FP and MP-AzeFlu (all dilutions) and AZE (1:102) significantly reduced IL-6 secretion and eosinophil survival compared with positive controls.	azelastine	46-49	interleukin 6	Homo sapiens	80-84
29121401-8	2018	In wild-type C57BL6 mice, the reduction in beta-hexosaminidase levels (P < .0001) by AZE + FP treatment upon HDM challenge was found in parallel with a decreased transmucosal passage (P = .0012) and completely reversed eosinophilic inflammation (P = .0013).	azelastine	88-91	O-GlcNAcase	Mus musculus	43-62
29121401-9	2018	In vitro, repeated applications of AZE + FP desensitized sensory neurons expressing the transient receptor potential channels TRPA1 and TRPV1.	azelastine	35-38	transient receptor potential cation channel subfamily A member 1	Homo sapiens	126-131
29121401-9	2018	In vitro, repeated applications of AZE + FP desensitized sensory neurons expressing the transient receptor potential channels TRPA1 and TRPV1.	azelastine	35-38	transient receptor potential cation channel subfamily V member 1	Homo sapiens	136-141
29378195-7	2018	Azelastine and histamine increased and suppressed, respectively, apo A-I gene promoter activity through a peroxisome proliferator activated receptor alpha response element.	azelastine	0-10	apolipoprotein A1	Homo sapiens	65-72
29378195-7	2018	Azelastine and histamine increased and suppressed, respectively, apo A-I gene promoter activity through a peroxisome proliferator activated receptor alpha response element.	azelastine	0-10	peroxisome proliferator activated receptor alpha	Homo sapiens	106-154
28512667-4	2017	IL-31-induced itch-related response was inhibited by anti-allergic drugs (tranilast and azelastine), but not by an H1 histamine receptor antagonist (terfenadine).	azelastine	88-98	interleukin 31	Mus musculus	0-5
28512667-4	2017	IL-31-induced itch-related response was inhibited by anti-allergic drugs (tranilast and azelastine), but not by an H1 histamine receptor antagonist (terfenadine).	azelastine	88-98	itchy, E3 ubiquitin protein ligase	Mus musculus	14-18
24965018-0	2014	In silico analysis and experimental validation of azelastine hydrochloride (N4) targeting sodium taurocholate co-transporting polypeptide (NTCP) in HBV therapy.	azelastine	50-74	solute carrier family 10 member 1	Homo sapiens	139-143
27623823-12	2017	Histamine and methacholine stimulated MUC5AC secretion was greater in cells treated with budesonide but was lesser in those treated with azelastine, as compared to controls.	azelastine	137-147	mucin 5AC, oligomeric mucus/gel-forming	Homo sapiens	38-44
25119779-3	2014	Unlike other H1 antihistamines, azelastine decreased lipopolysaccharide-induced tumor necrosis factor alpha and interleukin-12 secretion from murine bone marrow-derived DC.	azelastine	32-42	tumor necrosis factor	Mus musculus	80-107
25060977-0	2015	Azelastine enhances the clinical efficacy of glucocorticoid by modulating MKP-1 expression in allergic rhinitis.	azelastine	0-10	dual specificity phosphatase 1	Homo sapiens	74-79
25060977-6	2015	We found azelastine significantly inhibited cytokine-induced ICAM-1 upregulation, which is reversed by MKP-1 silencing.	azelastine	9-19	intercellular adhesion molecule 1	Homo sapiens	61-67
25060977-6	2015	We found azelastine significantly inhibited cytokine-induced ICAM-1 upregulation, which is reversed by MKP-1 silencing.	azelastine	9-19	dual specificity phosphatase 1	Homo sapiens	103-108
25060977-7	2015	Azelastine and budesonide additively increased MKP-1 expression and inhibited ICAM-1 expression in vitro.	azelastine	0-10	dual specificity phosphatase 1	Homo sapiens	47-52
25060977-7	2015	Azelastine and budesonide additively increased MKP-1 expression and inhibited ICAM-1 expression in vitro.	azelastine	0-10	intercellular adhesion molecule 1	Homo sapiens	78-84
25060977-8	2015	After treatment for two consecutive weeks, combined azelastine and budesonide nasal spray significantly decreased nasal ICAM-1 level and TNSS in six uncontrolled AR patients.	azelastine	52-62	intercellular adhesion molecule 1	Homo sapiens	120-126
25060977-9	2015	Our findings suggested that azelastine is able to additively enhance the anti-inflammatory effect of budesonide by modulating MKP-1 expression, which may implicate in the treatment of uncontrolled severe AR.	azelastine	28-38	dual specificity phosphatase 1	Homo sapiens	126-131
26130469-7	2015	Other agents effective in treating nonallergic rhinitis (NAR) such as azelastine have been demonstrated to exhibit TRPV1 channel activity through the modulation of Ca(2+) signaling on sensory neurons and in nasal epithelial cells.	azelastine	70-80	transient receptor potential cation channel subfamily V member 1	Homo sapiens	115-120
26600671-8	2015	In HaCaT keratinocytes histamine and TNF-alpha induced IL-8 and MMP-1 expression was reduced by amarogentin to a similar extent as with azelastine.	azelastine	136-146	tumor necrosis factor	Homo sapiens	37-46
23657985-5	2013	Among the eight drugs studied, prednisone, desloratadine, and azelastine exhibited the highest binding affinity (K(d) = 1.65, 2.05, and 8.47 muM, respectively) toward DNA photolyase.	azelastine	62-72	latexin	Homo sapiens	141-144
24980233-0	2014	Azelastine desensitization of transient receptor potential vanilloid 1: a potential mechanism explaining its therapeutic effect in nonallergic rhinitis.	azelastine	0-10	transient receptor potential cation channel, subfamily V, member 1	Mus musculus	30-70
24980233-3	2014	This study was designed to determine, using in vitro cell lines, whether topical therapies including azelastine have activity on TRPV1 ion channels similar to capsaicin.	azelastine	101-111	transient receptor potential cation channel, subfamily V, member 1	Mus musculus	129-134
24980233-6	2014	As azelastine has previously been found clinically effective in NAR, additional experiments were performed to determine its ability to desensitize TRPV1 ion channels and its effect on regulating intracellular calcium homeostasis.	azelastine	3-13	transient receptor potential cation channel, subfamily V, member 1	Mus musculus	147-152
24980233-7	2014	RESULTS: Cath.a cells treated with azelastine, bepotastine, or capsaicin showed a significant increase in TRPV1-dependant (Ca(2+)) specific cytosolic fluorescence.	azelastine	35-45	transient receptor potential cation channel, subfamily V, member 1	Mus musculus	106-111
24980233-8	2014	Continuous treatment with azelastine or capsaicin resulted in desensitization of TRPV1 channels.	azelastine	26-36	transient receptor potential cation channel, subfamily V, member 1	Mus musculus	81-86
24980233-10	2014	CONCLUSION: Azelastine, similar to capsaicin, exhibits direct activity on TRPV1 ion channels that may represent a novel mechanistic pathway explaining its clinical efficacy in NAR.	azelastine	12-22	transient receptor potential cation channel, subfamily V, member 1	Mus musculus	74-79
24005046-1	2013	Azelastine is a second generation histamine H1-receptor antagonist used as an anti-asthmatic and anti-allergic drug that can induce QT prolongation and torsades de pointes.	azelastine	0-10	histamine receptor H1	Homo sapiens	34-55
24005046-4	2013	We examined the effects of azelastine on the hERG channels expressed in Xenopus oocytes and HEK293 cells using two-microelectrode voltage-clamp and patch-clamp techniques.	azelastine	27-37	ETS transcription factor ERG	Homo sapiens	45-49
24005046-5	2013	Azelastine induced a concentration-dependent decrease of the hERG current amplitude at the end of the voltage steps and tail currents.	azelastine	0-10	ETS transcription factor ERG	Homo sapiens	61-65
24005046-6	2013	The IC50 for the azelastine-induced block of the hERG currents expressed in HEK293 cells was 11.43 nM, while the drug inhibited I(Ca,L) and I(Ca,T) with IC50 values of 7.60 and 26.21 muM, respectively.	azelastine	17-27	ETS transcription factor ERG	Homo sapiens	49-53
24005046-8	2013	These results suggest that azelastine is a potent blocker of hERG channels rather than I(Ca,L) or I(Ca,T), providing molecular mechanisms for the arrhythmogenic side effects during the clinical administration of azelastine.	azelastine	27-37	ETS transcription factor ERG	Homo sapiens	61-65
24005046-8	2013	These results suggest that azelastine is a potent blocker of hERG channels rather than I(Ca,L) or I(Ca,T), providing molecular mechanisms for the arrhythmogenic side effects during the clinical administration of azelastine.	azelastine	212-222	ETS transcription factor ERG	Homo sapiens	61-65
24127660-8	2014	Azelastine, an H1 receptor antagonist approved for the treatment of seasonal allergic rhinitis, nonallergic vasomotor rhinitis, and ocular conjunctivitis, was subsequently confirmed as a selective inhibitor of IL-6-induced pSTAT3 activation that also reduced the growth of HNSCC cell lines.	azelastine	0-10	interleukin 6	Homo sapiens	210-214
24274229-0	2013	Effect of intranasal azelastine on substance P release in perennial nonallergic rhinitis patients.	azelastine	21-31	tachykinin precursor 1	Homo sapiens	35-46
24274229-4	2013	Assessment of changes in the concentration of substance P (SP) in nasal lavage fluid before and after saline hypertonic challenge may be a means of assessing the effect of intranasal azelastine on neuropeptide release and severity of rhinitis symptoms.	azelastine	183-193	tachykinin precursor 1	Homo sapiens	46-57
24274229-11	2013	After azelastine treatment, significantly greater concentrations of SP were seen in nasal lavage fluid 15 minutes after hypertonic saline challenge in the untreated patients (56.8 +- 13.8 pg/mL) in comparison with azelastine-treated patients (44.5 +- 16.5 pg/mL; p < 0.05).	azelastine	6-16	tachykinin precursor 1	Homo sapiens	68-70
24274229-13	2013	CONCLUSION: Azelastine intranasal spray reduces SP release into nasal lavage fluid of NAR patients immediately after hypertonic nasal saline challenge.	azelastine	12-22	tachykinin precursor 1	Homo sapiens	48-50
15631542-9	2005	Some topical multiple-action histamine H(1)-receptor antagonists (olopatadine, ketotifen, azelastine and epinastine) have been shown to prevent activation of neutrophils, eosinophils and macrophages, or inhibit release of leukotrienes, platelet-activating factors and other inflammatory mediators.	azelastine	90-100	histamine receptor H1	Homo sapiens	29-52
20502763-1	2010	BACKGROUND: Azelastine hydrochloride is a histamine receptor-1 (H(1)) antagonist with anti-inflammatory properties that is available in the United States as Astelin Nasal Spray for rhinitis patients who are suffering from sneezing and rhinorrhea.	azelastine	12-36	H1.5 linker histone, cluster member	Homo sapiens	42-68
20502763-1	2010	BACKGROUND: Azelastine hydrochloride is a histamine receptor-1 (H(1)) antagonist with anti-inflammatory properties that is available in the United States as Astelin Nasal Spray for rhinitis patients who are suffering from sneezing and rhinorrhea.	azelastine	157-164	H1.5 linker histone, cluster member	Homo sapiens	42-68
22347894-7	2010	Among them, azelastine and mizolastine are predicted to be effluxed via ABCB1-mediated transport, whereas aripiprazole, clozapine, cyproheptadine, iloperidone, olanzapine, and ziprasidone are likely to be non-effluxed.	azelastine	12-22	ATP binding cassette subfamily B member 1	Homo sapiens	72-77
17499203-2	2007	The cells were cultured for 24 h with IgE treatment in the presence of azelastine or epinastine at the concentration of 10(-5) M. The FcepsilonRIalpha mRNA expression was determined by northern blot analysis.	azelastine	71-81	Fc epsilon receptor Ia	Rattus norvegicus	134-150
17499203-6	2007	The inhibitory effect of azelastine on the IgE-mediated expression of FcepsilonRIgamma protein is not due to their inhibition of mRNA and protein expression, but due to abrogating phosphorylation of the gamma chains, which is important for initiation of FcepsilonRI signaling cascade elicited by IgE interaction.	azelastine	25-35	Fc epsilon receptor Ig	Rattus norvegicus	70-86
17239638-3	2008	We, therefore, assessed the effect of clinically recommended doses of azelastine and montelukast alone and in combination on EAR and LAR.	azelastine	70-80	protein tyrosine phosphatase receptor type F	Homo sapiens	133-136
17239638-6	2008	RESULTS: Azelastine, montelukast and their combination protected against both EAR and LAR (p<0.004, each) by 46% and 43%, 76% and 59%, and 89% and 78%, respectively.	azelastine	9-19	protein tyrosine phosphatase receptor type F	Homo sapiens	86-89
16996482-12	2006	The anti-histamine azelastine inhibited TNF-alpha release dose dependently.	azelastine	19-29	tumor necrosis factor	Homo sapiens	40-49
16925996-8	2006	Cepsilon and AID mRNA levels were lower on the treatment with 10(-5) M azelastine than those on the treatment with vehicle, but were not decreased on the treatment with 10(-5) M epinastine.	azelastine	71-81	activation-induced cytidine deaminase	Rattus norvegicus	13-16
16925996-10	2006	Azelastine at 10(-5) M, but not epinastine, reduced DNA binding activity of NF-kappaB and also diminished IkappaBalpha phosphorylation, leading to sustaining IkappaBalpha protein levels.	azelastine	0-10	NFKB inhibitor alpha	Rattus norvegicus	106-118
16925996-10	2006	Azelastine at 10(-5) M, but not epinastine, reduced DNA binding activity of NF-kappaB and also diminished IkappaBalpha phosphorylation, leading to sustaining IkappaBalpha protein levels.	azelastine	0-10	NFKB inhibitor alpha	Rattus norvegicus	158-170
16614391-10	2006	Enhanced pulmonary vascular permeability induced by UCN was markedly inhibited by pretreatment with the mast-cell stabilizer cromolyn and histamine-1 (H1) receptor antagonist azelastine respectively, but not by the leukotriene receptor antagonist montelukast.	azelastine	175-185	urocortin	Rattus norvegicus	52-55
15806111-1	2005	1 To clarify the mechanism of mast cell TNF secretion, especially its release process after being produced, we utilized an antiallergic drug, azelastine (4-(p-chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1-(2H)- phthalazinone), which has been reported to inhibit TNF release without affecting its production in ionomycin-stimulated RBL-2H3 cells.	azelastine	142-152	tumor necrosis factor	Rattus norvegicus	40-43
15806111-1	2005	1 To clarify the mechanism of mast cell TNF secretion, especially its release process after being produced, we utilized an antiallergic drug, azelastine (4-(p-chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1-(2H)- phthalazinone), which has been reported to inhibit TNF release without affecting its production in ionomycin-stimulated RBL-2H3 cells.	azelastine	142-152	tumor necrosis factor	Rattus norvegicus	270-273
15806111-1	2005	1 To clarify the mechanism of mast cell TNF secretion, especially its release process after being produced, we utilized an antiallergic drug, azelastine (4-(p-chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1-(2H)- phthalazinone), which has been reported to inhibit TNF release without affecting its production in ionomycin-stimulated RBL-2H3 cells.	azelastine	154-232	tumor necrosis factor	Rattus norvegicus	40-43
15806111-1	2005	1 To clarify the mechanism of mast cell TNF secretion, especially its release process after being produced, we utilized an antiallergic drug, azelastine (4-(p-chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1-(2H)- phthalazinone), which has been reported to inhibit TNF release without affecting its production in ionomycin-stimulated RBL-2H3 cells.	azelastine	154-232	tumor necrosis factor	Rattus norvegicus	270-273
15806111-9	2005	6 These results suggest that (alpha)PKC mediates the TNF release process and azelastine inhibits TNF release by selectively interfering with the recruitment of (alpha)PKC in the pathway activated by ionomycin in RBL-2H3 cells.	azelastine	77-87	tumor necrosis factor	Rattus norvegicus	97-100
15978303-1	2005	BACKGROUND: Azelastine nasal spray and oral cetirizine are selective histamine H(1)-receptor antagonists that are approved in the United States for the treatment of seasonal allergic rhinitis (SAR).	azelastine	12-22	histamine receptor H1	Homo sapiens	69-92
14646384-0	2003	Azelastine inhibits secretion of IL-6, TNF-alpha and IL-8 as well as NF-kappaB activation and intracellular calcium ion levels in normal human mast cells.	azelastine	0-10	interleukin 6	Homo sapiens	33-37
14646384-0	2003	Azelastine inhibits secretion of IL-6, TNF-alpha and IL-8 as well as NF-kappaB activation and intracellular calcium ion levels in normal human mast cells.	azelastine	0-10	tumor necrosis factor	Homo sapiens	39-48
14646384-0	2003	Azelastine inhibits secretion of IL-6, TNF-alpha and IL-8 as well as NF-kappaB activation and intracellular calcium ion levels in normal human mast cells.	azelastine	0-10	C-X-C motif chemokine ligand 8	Homo sapiens	53-57
14646384-3	2003	METHODS: We investigated the effect of azelastine on the secretion of IL-6, TNF-alpha and IL-8 from hCBMC, as well as its possible mechanism of action.	azelastine	39-49	interleukin 6	Homo sapiens	70-74
14646384-3	2003	METHODS: We investigated the effect of azelastine on the secretion of IL-6, TNF-alpha and IL-8 from hCBMC, as well as its possible mechanism of action.	azelastine	39-49	tumor necrosis factor	Homo sapiens	76-85
14646384-3	2003	METHODS: We investigated the effect of azelastine on the secretion of IL-6, TNF-alpha and IL-8 from hCBMC, as well as its possible mechanism of action.	azelastine	39-49	C-X-C motif chemokine ligand 8	Homo sapiens	90-94
14646384-7	2003	Preincubation for 5 min resulted in almost maximal inhibition with 6 microM azelastine for TNF-alpha (80%), with 24 microM for IL-6 (83%) and 60 microM for IL-8 (99%); the vehicle solution at the same concentrations as Optivar had no effect.	azelastine	76-86	tumor necrosis factor	Homo sapiens	91-100
14646384-9	2003	CONCLUSION: Azelastine inhibited hCBMC secretion of IL-6, TNF-alpha and IL-8, possibly by inhibiting intracellular Ca2+ ions and NF-kappaB activation.	azelastine	12-22	interleukin 6	Homo sapiens	52-56
14646384-9	2003	CONCLUSION: Azelastine inhibited hCBMC secretion of IL-6, TNF-alpha and IL-8, possibly by inhibiting intracellular Ca2+ ions and NF-kappaB activation.	azelastine	12-22	tumor necrosis factor	Homo sapiens	58-67
14646384-9	2003	CONCLUSION: Azelastine inhibited hCBMC secretion of IL-6, TNF-alpha and IL-8, possibly by inhibiting intracellular Ca2+ ions and NF-kappaB activation.	azelastine	12-22	C-X-C motif chemokine ligand 8	Homo sapiens	72-76
11948533-3	2002	Because we previously clarified that azelastine, an antiallergy and antiasthmatic drug, is N-demethylated by CYP1A2, CYP2D6, and CYP3A4 in humans, the reaction was used as a model.	azelastine	37-47	cytochrome P450 family 1 subfamily A member 2	Homo sapiens	109-115
12969771-7	2003	significantly inhibited the development of nasal obstruction when sensitized guinea pigs were repeatedly challenged via inhalation with Japanese cedar pollen, whereas the histamine H1-receptor antagonist, azelastine (1 mg/kg, p.o.	azelastine	205-215	histamine H1 receptor	Cavia porcellus	171-192
12722967-8	2003	RESULTS: Azelastine, in comparison to placebo, significantly reduced symptom scores, number of inflammatory cells, and intercellular adhesion molecule-1 expression during the early- and late-phase reaction.	azelastine	9-19	intercellular adhesion molecule 1	Homo sapiens	119-152
12776442-2	2003	Azelastine has established antiallergic and anti-inflammatory effects that are unrelated to H1-receptor antagonism, including inhibitory effects on the synthesis of leukotrienes, kinins, and cytokines; the generation of superoxide free radicals; and the expression of the intercellular adhesion molecule 1.	azelastine	0-10	intercellular adhesion molecule 1	Homo sapiens	272-305
12660427-11	2003	Intradermal injection of CRH or Ucn induced substantial Evan"s blue extravasation that was inhibited by pretreatment with azelastine (24 microM) and olopatadine (133 microM).	azelastine	122-132	corticotropin releasing hormone	Rattus norvegicus	25-28
12673950-4	2003	In RBL-2H3 mast cells, anti-allergic drugs including azelastine inhibited the release of TNF more potently than degranulation in response to antigen or ionomycin.	azelastine	53-63	tumor necrosis factor-like	Rattus norvegicus	89-92
12027072-0	2002	Azelastine is more potent than olopatadine n inhibiting interleukin-6 and tryptase release from human umbilical cord blood-derived cultured mast cells.	azelastine	0-10	interleukin 6	Homo sapiens	56-69
12027072-11	2002	CONCLUSIONS: These results indicate that azelastine and olopatadine can inhibit CHMCs activation and release of IL-6, tryptase, and histamine.	azelastine	41-51	interleukin 6	Homo sapiens	112-116
12607189-8	2002	The antiH-1, emedastine, significantly reduced H-induced production of IL-1, IL-6 and IL-8, while azelastine reduced only IL-1.	azelastine	98-108	interleukin 1 alpha	Homo sapiens	122-126
11948533-3	2002	Because we previously clarified that azelastine, an antiallergy and antiasthmatic drug, is N-demethylated by CYP1A2, CYP2D6, and CYP3A4 in humans, the reaction was used as a model.	azelastine	37-47	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	117-123
11948533-3	2002	Because we previously clarified that azelastine, an antiallergy and antiasthmatic drug, is N-demethylated by CYP1A2, CYP2D6, and CYP3A4 in humans, the reaction was used as a model.	azelastine	37-47	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	129-135
11858803-0	2002	Inhibitory effects of azelastine on substance P-induced itch-associated response in mice.	azelastine	22-32	tachykinin 1	Mus musculus	36-47
11858803-3	2002	Substance P-induced scratching was dose dependently suppressed by azelastine (3-30 mg/kg), but not by chlorpheniramine (10 and 30 mg/kg).	azelastine	66-76	tachykinin 1	Mus musculus	0-11
11858803-4	2002	Azelastine (30 mg/kg) inhibited the substance P-induced production of leukotriene B4, but not prostaglandin E2, in the skin.	azelastine	0-10	tachykinin 1	Mus musculus	36-47
9827354-0	1998	Influence of the anti-allergic agent, azelastine, on tumor necrosis factor-alpha (TNF-alpha) secretion from cultured mouse mast cells.	azelastine	38-48	tumor necrosis factor	Mus musculus	53-80
11894734-2	2002	Azelastine and olopatadine are histamine 1 receptor (H-1R) antagonists with antiallergic effects present in the ophthalmic solutions Optivar and Patanol, respectively.	azelastine	0-10	histamine receptor H1	Homo sapiens	53-57
10772385-4	2000	All antihistamines caused a dose-dependent inhibition of TNF-alpha release from HMC-1 cells, with maximal effects at 10(-12) M for azelastine, 10(-9) M for loratadine and cetirizine, and 10(-8) M for ranitidine.	azelastine	131-141	tumor necrosis factor	Homo sapiens	57-66
10570018-0	1999	Azelastine N-demethylation by cytochrome P-450 (CYP)3A4, CYP2D6, and CYP1A2 in human liver microsomes: evaluation of approach to predict the contribution of multiple CYPs.	azelastine	0-10	peptidylprolyl isomerase G	Homo sapiens	48-51
10570018-0	1999	Azelastine N-demethylation by cytochrome P-450 (CYP)3A4, CYP2D6, and CYP1A2 in human liver microsomes: evaluation of approach to predict the contribution of multiple CYPs.	azelastine	0-10	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	57-63
10570018-0	1999	Azelastine N-demethylation by cytochrome P-450 (CYP)3A4, CYP2D6, and CYP1A2 in human liver microsomes: evaluation of approach to predict the contribution of multiple CYPs.	azelastine	0-10	cytochrome P450 family 1 subfamily A member 2	Homo sapiens	69-75
10570018-3	1999	In microsomes from human B-lymphoblast cells, recombinant cytochrome P-450 (CYP)2D6 and CYP1A1 exhibited higher azelastine N-demethylase activity than did other CYP enzymes.	azelastine	112-122	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	58-83
10570018-3	1999	In microsomes from human B-lymphoblast cells, recombinant cytochrome P-450 (CYP)2D6 and CYP1A1 exhibited higher azelastine N-demethylase activity than did other CYP enzymes.	azelastine	112-122	cytochrome P450 family 1 subfamily A member 1	Homo sapiens	88-94
10570018-3	1999	In microsomes from human B-lymphoblast cells, recombinant cytochrome P-450 (CYP)2D6 and CYP1A1 exhibited higher azelastine N-demethylase activity than did other CYP enzymes.	azelastine	112-122	peptidylprolyl isomerase G	Homo sapiens	76-79
10570018-4	1999	On the other hand, recombinant CYP3A4 and CYP1A2 as well as CYP1A1 and CYP2D6 in microsomes from baculovirus-infected insect cells were active in azelastine N-demethylation.	azelastine	146-156	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	31-37
10570018-4	1999	On the other hand, recombinant CYP3A4 and CYP1A2 as well as CYP1A1 and CYP2D6 in microsomes from baculovirus-infected insect cells were active in azelastine N-demethylation.	azelastine	146-156	cytochrome P450 family 1 subfamily A member 2	Homo sapiens	42-48
10570018-4	1999	On the other hand, recombinant CYP3A4 and CYP1A2 as well as CYP1A1 and CYP2D6 in microsomes from baculovirus-infected insect cells were active in azelastine N-demethylation.	azelastine	146-156	cytochrome P450 family 1 subfamily A member 1	Homo sapiens	60-66
10570018-4	1999	On the other hand, recombinant CYP3A4 and CYP1A2 as well as CYP1A1 and CYP2D6 in microsomes from baculovirus-infected insect cells were active in azelastine N-demethylation.	azelastine	146-156	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	71-77
10570018-11	1999	Our data suggested that the approach using RAF(CL) (RAF as the ratio of clearance) is most predictive of the N-demethylation clearance of azelastine because it best reflects the observed N-demethylation clearance in human liver microsomes.	azelastine	138-148	zinc fingers and homeoboxes 2	Homo sapiens	43-46
10570018-11	1999	Our data suggested that the approach using RAF(CL) (RAF as the ratio of clearance) is most predictive of the N-demethylation clearance of azelastine because it best reflects the observed N-demethylation clearance in human liver microsomes.	azelastine	138-148	zinc fingers and homeoboxes 2	Homo sapiens	52-55
10570018-12	1999	Summarizing the results, azelastine N-demethylation in humans liver microsomes is catalyzed mainly by CYP3A4 and CYP2D6, and CYP1A2 to a small extent (in average, 76.6, 21.8, and 3.9%, respectively), although the percent contribution of each isoform varied among individuals.	azelastine	25-35	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	102-108
10570018-12	1999	Summarizing the results, azelastine N-demethylation in humans liver microsomes is catalyzed mainly by CYP3A4 and CYP2D6, and CYP1A2 to a small extent (in average, 76.6, 21.8, and 3.9%, respectively), although the percent contribution of each isoform varied among individuals.	azelastine	25-35	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	113-119
10570018-12	1999	Summarizing the results, azelastine N-demethylation in humans liver microsomes is catalyzed mainly by CYP3A4 and CYP2D6, and CYP1A2 to a small extent (in average, 76.6, 21.8, and 3.9%, respectively), although the percent contribution of each isoform varied among individuals.	azelastine	25-35	cytochrome P450 family 1 subfamily A member 2	Homo sapiens	125-131
10757040-0	1999	Suppressive effects of azelastine hydrochloride on CD40 expression in mice.	azelastine	23-47	CD40 antigen	Mus musculus	51-55
10757040-1	1999	The present study was designed to examine the influence of an anti-allergic agent, azelastine hydrochloride (AZ) on a co-stimulatory molecule, CD40 expression in actively sensitized mice.	azelastine	83-107	CD40 antigen	Mus musculus	143-147
10757040-1	1999	The present study was designed to examine the influence of an anti-allergic agent, azelastine hydrochloride (AZ) on a co-stimulatory molecule, CD40 expression in actively sensitized mice.	azelastine	109-111	CD40 antigen	Mus musculus	143-147
10757040-7	1999	These data may suggest that AZ suppresses the production of IgE through the inhibition of CD40 expression.	azelastine	28-30	CD40 antigen	Mus musculus	90-94
10654195-4	1999	Treatment of BALB/c mice with azelastine (AZ) at a dose of 50.0 micrograms/kg/day, which is the most effective therapeutic dose, for two weeks scarcely affected the expression of co-stimulatory molecules CD40, CD80 and CD86 on splenocytes, whereas a three-week treatment strongly suppressed the expression of these molecules.	azelastine	30-40	CD40 antigen	Mus musculus	204-208
10654195-4	1999	Treatment of BALB/c mice with azelastine (AZ) at a dose of 50.0 micrograms/kg/day, which is the most effective therapeutic dose, for two weeks scarcely affected the expression of co-stimulatory molecules CD40, CD80 and CD86 on splenocytes, whereas a three-week treatment strongly suppressed the expression of these molecules.	azelastine	30-40	CD80 antigen	Mus musculus	210-214
10654195-4	1999	Treatment of BALB/c mice with azelastine (AZ) at a dose of 50.0 micrograms/kg/day, which is the most effective therapeutic dose, for two weeks scarcely affected the expression of co-stimulatory molecules CD40, CD80 and CD86 on splenocytes, whereas a three-week treatment strongly suppressed the expression of these molecules.	azelastine	30-40	CD86 antigen	Mus musculus	219-223
10654195-4	1999	Treatment of BALB/c mice with azelastine (AZ) at a dose of 50.0 micrograms/kg/day, which is the most effective therapeutic dose, for two weeks scarcely affected the expression of co-stimulatory molecules CD40, CD80 and CD86 on splenocytes, whereas a three-week treatment strongly suppressed the expression of these molecules.	azelastine	42-44	CD40 antigen	Mus musculus	204-208
10654195-4	1999	Treatment of BALB/c mice with azelastine (AZ) at a dose of 50.0 micrograms/kg/day, which is the most effective therapeutic dose, for two weeks scarcely affected the expression of co-stimulatory molecules CD40, CD80 and CD86 on splenocytes, whereas a three-week treatment strongly suppressed the expression of these molecules.	azelastine	42-44	CD80 antigen	Mus musculus	210-214
10654195-4	1999	Treatment of BALB/c mice with azelastine (AZ) at a dose of 50.0 micrograms/kg/day, which is the most effective therapeutic dose, for two weeks scarcely affected the expression of co-stimulatory molecules CD40, CD80 and CD86 on splenocytes, whereas a three-week treatment strongly suppressed the expression of these molecules.	azelastine	42-44	CD86 antigen	Mus musculus	219-223
10421623-0	1999	In vitro identification of the human cytochrome P-450 enzymes involved in the N-demethylation of azelastine.	azelastine	97-107	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	37-53
10421623-2	1999	The human cytochrome P-450 (CYP) isoform responsible for azelastine N-demethylation, the major metabolic pathway for azelastine, has been examined.	azelastine	57-67	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	10-26
10421623-2	1999	The human cytochrome P-450 (CYP) isoform responsible for azelastine N-demethylation, the major metabolic pathway for azelastine, has been examined.	azelastine	57-67	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	28-31
10421623-2	1999	The human cytochrome P-450 (CYP) isoform responsible for azelastine N-demethylation, the major metabolic pathway for azelastine, has been examined.	azelastine	117-127	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	10-26
10421623-2	1999	The human cytochrome P-450 (CYP) isoform responsible for azelastine N-demethylation, the major metabolic pathway for azelastine, has been examined.	azelastine	117-127	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	28-31
10421623-4	1999	In microsomes from baculovirus-infected insect cells, recombinant CYP3A4, 2D6, 1A2, and 2C19 exhibited high azelastine N-demethylase activity.	azelastine	108-118	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	66-72
10421623-8	1999	These observations suggested that the N-demethylation of azelastine is most extensively catalyzed by the CYP2D6 and 3A4 isoforms in humans.	azelastine	57-67	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	105-111
10383922-0	1999	Inhibitory effects of azelastine and its metabolites on drug oxidation catalyzed by human cytochrome P-450 enzymes.	azelastine	22-32	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	90-106
10383922-2	1999	In the present study, the inhibitory effects of azelastine and its two metabolites on human cytochrome P-450 (CYP) isoform-dependent reactions were investigated to predict the drug interactions of azelastine using microsomes from human B-lymphoblast cells expressing CYP.	azelastine	48-58	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	92-108
10383922-2	1999	In the present study, the inhibitory effects of azelastine and its two metabolites on human cytochrome P-450 (CYP) isoform-dependent reactions were investigated to predict the drug interactions of azelastine using microsomes from human B-lymphoblast cells expressing CYP.	azelastine	48-58	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	110-113
10383922-2	1999	In the present study, the inhibitory effects of azelastine and its two metabolites on human cytochrome P-450 (CYP) isoform-dependent reactions were investigated to predict the drug interactions of azelastine using microsomes from human B-lymphoblast cells expressing CYP.	azelastine	197-207	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	92-108
10383922-2	1999	In the present study, the inhibitory effects of azelastine and its two metabolites on human cytochrome P-450 (CYP) isoform-dependent reactions were investigated to predict the drug interactions of azelastine using microsomes from human B-lymphoblast cells expressing CYP.	azelastine	197-207	cytochrome P450 family 4 subfamily F member 3	Homo sapiens	110-113
10383922-5	1999	Desmethylazelastine, but not azelastine and 6-hydroxyazelastine, uncompetitively inhibited CYP2B6 activity (Ki = 32.6 +/- 4.8 microM).	azelastine	9-19	cytochrome P450 family 2 subfamily B member 6	Homo sapiens	91-97
10383922-6	1999	Azelastine, desmethylazelastine, and 6-hydroxyazelastine competitively inhibited CYP2C9 activity (Ki = 13.	azelastine	0-10	cytochrome P450 family 2 subfamily C member 9	Homo sapiens	81-87
10383922-8	1999	Azelastine and desmethylazelastine competitively inhibited CYP3A4 activity (Ki = 23.	azelastine	0-10	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	59-65
10383922-12	1999	Among the human CYPs tested, the inhibitory effects of azelastine and its two metabolites were the most potent on human CYP2D6.	azelastine	55-65	cytochrome P450 family 2 subfamily D member 6	Homo sapiens	120-126
10383922-14	1999	The inhibition of CYP2C9, CYP2C19, and CYP3A4 activity by azelastine and its two metabolites might be clinically insignificant.	azelastine	58-68	cytochrome P450 family 2 subfamily C member 9	Homo sapiens	18-24
10383922-14	1999	The inhibition of CYP2C9, CYP2C19, and CYP3A4 activity by azelastine and its two metabolites might be clinically insignificant.	azelastine	58-68	cytochrome P450 family 2 subfamily C member 19	Homo sapiens	26-33
10383922-14	1999	The inhibition of CYP2C9, CYP2C19, and CYP3A4 activity by azelastine and its two metabolites might be clinically insignificant.	azelastine	58-68	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	39-45
9950898-0	1999	Effect of azelastine on platelet-activating factor-induced microvascular leakage in rat airways.	azelastine	10-20	PCNA clamp associated factor	Rattus norvegicus	24-50
9950898-4	1999	Pretreatment with azelastine inhibited PAF-induced vascular leakage without affecting neutrophil accumulation.	azelastine	18-28	PCNA clamp associated factor	Rattus norvegicus	39-42
9950898-6	1999	PAF increased neutrophil elastase contents in bronchoalveolar lavage fluid, an effect that was inhibited by azelastine.	azelastine	108-118	PCNA clamp associated factor	Rattus norvegicus	0-3
9950898-6	1999	PAF increased neutrophil elastase contents in bronchoalveolar lavage fluid, an effect that was inhibited by azelastine.	azelastine	108-118	elastase, neutrophil expressed	Rattus norvegicus	14-33
9950898-7	1999	Therefore, azelastine attenuates PAF-induced airway mucosal microvascular leakage, probably involving inhibition of the release of neutrophil elastase from activated neutrophils.	azelastine	11-21	PCNA clamp associated factor	Rattus norvegicus	33-36
9950898-7	1999	Therefore, azelastine attenuates PAF-induced airway mucosal microvascular leakage, probably involving inhibition of the release of neutrophil elastase from activated neutrophils.	azelastine	11-21	elastase, neutrophil expressed	Rattus norvegicus	131-150
9893928-0	1998	Effects of azelastine on the level of serum interleukin-4 and soluble CD23 antigen in the treatment of nasal allergy.	azelastine	11-21	interleukin 4	Homo sapiens	44-57
9893928-0	1998	Effects of azelastine on the level of serum interleukin-4 and soluble CD23 antigen in the treatment of nasal allergy.	azelastine	11-21	Fc epsilon receptor II	Homo sapiens	70-74
9893928-3	1998	It is well known that azelastine hydrochloride (AZ, CAS 79307-93-0) suppresses symptoms of nasal allergy.	azelastine	22-46	BCAR1 scaffold protein, Cas family member	Homo sapiens	52-55
9893928-5	1998	One report states that the cytokines IL-2, IL-3, and IL-4 were suppressed by AZ in cultured cells.	azelastine	77-79	interleukin 2	Homo sapiens	37-41
9893928-5	1998	One report states that the cytokines IL-2, IL-3, and IL-4 were suppressed by AZ in cultured cells.	azelastine	77-79	interleukin 3	Homo sapiens	43-47
9893928-5	1998	One report states that the cytokines IL-2, IL-3, and IL-4 were suppressed by AZ in cultured cells.	azelastine	77-79	interleukin 4	Homo sapiens	53-57
9893928-8	1998	The results show that the levels of IL-4 and soluble CD23 were significantly reduced by the administration of AZ over a 4-week period, especially in patients with "excellent" or "good" efficacy of therapy.	azelastine	110-112	interleukin 4	Homo sapiens	36-40
9893928-8	1998	The results show that the levels of IL-4 and soluble CD23 were significantly reduced by the administration of AZ over a 4-week period, especially in patients with "excellent" or "good" efficacy of therapy.	azelastine	110-112	Fc epsilon receptor II	Homo sapiens	53-57
9865509-7	1998	Azelastine inhibited angiotensin II-, KCl- and norepinephrine-induced contractions non-specifically, while disodium cromoglycate did not affect these contractile responses.	azelastine	0-10	angiotensinogen	Homo sapiens	21-35
11894734-2	2002	Azelastine and olopatadine are histamine 1 receptor (H-1R) antagonists with antiallergic effects present in the ophthalmic solutions Optivar and Patanol, respectively.	azelastine	0-10	histamine receptor H1	Homo sapiens	31-51
11878205-3	2002	Nasal polyp cells (2 x 10(5)/ml) were sensitized with human IgE pre-incubated azelastine (CAS 58581-89-8), terfenadine (CAS 50679-08-8), levocabastine (CAS 79516-68-0) or cetirizine (CAS 83881-51-0), and stimulated with anti-human immunoglobulin E (IgE).	azelastine	78-88	immunoglobulin heavy constant epsilon	Homo sapiens	60-63
11878205-6	2002	Azelastine and terfenadine inhibited TNF alpha release with IC50 values of 6.2 mumol/l and 4.3 mumol/l, respectively.	azelastine	0-10	tumor necrosis factor	Homo sapiens	37-46
11878205-8	2002	Azelastine shows anti-inflammatory properties in therapeutically relevant concentrations as assessed by its ability to reduce TNF alpha release as well as its ability to inhibit LTC4 production in allergically stimulated human nasal polyp cells.	azelastine	0-10	tumor necrosis factor	Homo sapiens	126-135
10772385-9	2000	At the mRNA level, inhibition was only seen with KU812 cells and IL-8 in the presence of azelastine at 10-(10) M. These data show thus distinct inhibitory patterns for different antihistamines during cytokine production from human mast cells and basophils which may contribute to the anti-inflammatory effects of these drugs during treatment of allergic diseases.	azelastine	89-99	C-X-C motif chemokine ligand 8	Homo sapiens	65-69
10478514-2	1999	In addition to acting as a histamine H1-receptor antagonist, azelastine also inhibits the production or release of many chemical mediators of the allergic response such as leukotrienes, free radicals, and cytokines.	azelastine	61-71	histamine receptor H1	Homo sapiens	27-48
9827354-0	1998	Influence of the anti-allergic agent, azelastine, on tumor necrosis factor-alpha (TNF-alpha) secretion from cultured mouse mast cells.	azelastine	38-48	tumor necrosis factor	Mus musculus	82-91
9827354-1	1998	The influence of azelastine (AZ) on tumor necrosis factor-alpha (TNF-alpha) secretllon from cultured mast cells was examined.	azelastine	29-31	tumor necrosis factor	Mus musculus	36-63
9827354-5	1998	However, higher doses (5.0 and 10.0 micrograms/ml) of AZ inhibited the secretion (but not production) of TNF-alpha from mast cells.	azelastine	54-56	tumor necrosis factor	Mus musculus	105-114
9827354-6	1998	These results may suggest that some of the therapeutic effects of AZ depend on its ability to reduce the secretion of TNF-alpha from mast cells.	azelastine	66-68	tumor necrosis factor	Mus musculus	118-127
9664202-2	1998	UNLABELLED: Azelastine, a phthalazinone compound, is a second generation histamine H1 receptor antagonist which has shown clinical efficacy in relieving the symptoms of allergic rhinitis when administered as either an oral or intranasal formulation.	azelastine	12-22	histamine receptor H1	Homo sapiens	73-94
9698198-3	1998	Histamine H1 receptor antagonists having antiallergic activity (an inhibition of mast cell degranulation), such as azelastine and oxatomide and nonsedative histamine H receptor antagonists such as terfenadine, epinastine and astemizole, also showed a relatively potent effect.	azelastine	115-125	histamine receptor H1	Mus musculus	0-21