PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 18239617-5 2008 Functionally, histamine and H(4)R agonists clobenpropit and 4-methylhistamine downregulated the production of the Th2-linked chemokine CCL2 and the Th1 cytokine IL-12 on Mo-IDEC, whereas agonists for the other histamine receptors did not. clobenpropit 43-55 histamine receptor H4 Homo sapiens 28-33 18550011-3 2008 The topical application of a histamine H3 receptor antagonist, clobenpropit, into the nasal cavities resulted in a dose-dependent increase in sneezing and nasal rubbing, and both Sch 50971 and a tachykinin NK1 receptor antagonist, L-733,060, inhibited these reactions in non-sensitized mice. clobenpropit 63-75 histamine receptor H3 Mus musculus 29-50 18239617-5 2008 Functionally, histamine and H(4)R agonists clobenpropit and 4-methylhistamine downregulated the production of the Th2-linked chemokine CCL2 and the Th1 cytokine IL-12 on Mo-IDEC, whereas agonists for the other histamine receptors did not. clobenpropit 43-55 C-C motif chemokine ligand 2 Homo sapiens 135-139 18239617-5 2008 Functionally, histamine and H(4)R agonists clobenpropit and 4-methylhistamine downregulated the production of the Th2-linked chemokine CCL2 and the Th1 cytokine IL-12 on Mo-IDEC, whereas agonists for the other histamine receptors did not. clobenpropit 43-55 negative elongation factor complex member C/D Homo sapiens 148-151 17350613-0 2007 The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons. clobenpropit 37-49 histamine receptor H3 Rattus norvegicus 4-25 17627982-7 2007 The excitatory actions of the agonists were specifically and selectively blocked by the H(1), H(2), H(3) or H(4) receptor antagonists pyrilamine, ranitidine, clobenpropit or J1-[(5-chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine (JNJ 7777120), respectively. clobenpropit 158-170 H3 clustered histone 14 Homo sapiens 100-121 17507084-7 2007 H(4)R agonists (clobenpropit and 4-methylhistamine) induce a Ca(2+) mobilization in monocytes, which could be blocked with the selective H(4)R antagonist JNJ7,777,120. clobenpropit 16-28 histamine receptor H4 Homo sapiens 0-5 17507084-7 2007 H(4)R agonists (clobenpropit and 4-methylhistamine) induce a Ca(2+) mobilization in monocytes, which could be blocked with the selective H(4)R antagonist JNJ7,777,120. clobenpropit 16-28 histamine receptor H4 Homo sapiens 137-142 17350613-0 2007 The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons. clobenpropit 37-49 protein kinase cAMP-activated catalytic subunit alpha Rattus norvegicus 136-152 17350613-2 2007 Clobenpropit reversed the neurotoxicity in a concentration-dependent manner, and showed peak protection at a concentration of 10(-7) M. This protection was antagonized by the histamine H3 receptor agonist (R)-alpha-methylhistamine, but not by the histamine H1 receptor antagonist pyrilamine or the histamine H2 receptor antagonist cimetidine. clobenpropit 0-12 histamine receptor H3 Rattus norvegicus 175-196 17350613-2 2007 Clobenpropit reversed the neurotoxicity in a concentration-dependent manner, and showed peak protection at a concentration of 10(-7) M. This protection was antagonized by the histamine H3 receptor agonist (R)-alpha-methylhistamine, but not by the histamine H1 receptor antagonist pyrilamine or the histamine H2 receptor antagonist cimetidine. clobenpropit 0-12 histamine receptor H 1 Rattus norvegicus 247-268 17350613-2 2007 Clobenpropit reversed the neurotoxicity in a concentration-dependent manner, and showed peak protection at a concentration of 10(-7) M. This protection was antagonized by the histamine H3 receptor agonist (R)-alpha-methylhistamine, but not by the histamine H1 receptor antagonist pyrilamine or the histamine H2 receptor antagonist cimetidine. clobenpropit 0-12 histamine receptor H 2 Rattus norvegicus 298-319 17350613-6 2007 Furthermore, both the adenylyl cyclase inhibitor SQ-22536 and the protein kinase A (PKA) inhibitor H-89 reversed the protection and the GABA release by clobenpropit. clobenpropit 152-164 protein kinase cAMP-activated catalytic subunit alpha Rattus norvegicus 66-82 17350613-6 2007 Furthermore, both the adenylyl cyclase inhibitor SQ-22536 and the protein kinase A (PKA) inhibitor H-89 reversed the protection and the GABA release by clobenpropit. clobenpropit 152-164 protein kinase cAMP-activated catalytic subunit alpha Rattus norvegicus 84-87 17350613-8 2007 These results indicate that clobenpropit enhanced GABA release to protect against NMDA-induced excitotoxicity, which was induced through the cAMP/PKA pathway, and reduction of intracellular calcium level may also be involved. clobenpropit 28-40 protein kinase cAMP-activated catalytic subunit alpha Rattus norvegicus 146-149 15082882-7 2004 Pretreatment with histamine H(3) receptor antagonist clobenpropit (4 micromol/kg i.a.) clobenpropit 53-65 histamine receptor H3 Rattus norvegicus 18-41 14735131-4 2004 The aim of the present study was to evaluate the effects of two histamine H3 receptor antagonists, clobenpropit and thioperamide, on rewarding and neurochemical effects of methamphetamine utilizing three in vivo methodologies, drug self-administration, drug discrimination, and microdialysis in Sprague-Dawley rats. clobenpropit 99-111 histamine receptor H3 Rattus norvegicus 64-85 17346280-4 2007 Dimaprit, clobenpropit and clozapine, which are H4R agonists, dose-dependently blocked both PPD-induced interferon-gamma and Cry j1-induced interleukin-5 production by both peripheral blood mononuclear cells (PBMCs) and antigen-specific T-cell lines. clobenpropit 10-22 histamine receptor H4 Homo sapiens 48-51 17346280-4 2007 Dimaprit, clobenpropit and clozapine, which are H4R agonists, dose-dependently blocked both PPD-induced interferon-gamma and Cry j1-induced interleukin-5 production by both peripheral blood mononuclear cells (PBMCs) and antigen-specific T-cell lines. clobenpropit 10-22 interferon gamma Homo sapiens 104-120 17346280-4 2007 Dimaprit, clobenpropit and clozapine, which are H4R agonists, dose-dependently blocked both PPD-induced interferon-gamma and Cry j1-induced interleukin-5 production by both peripheral blood mononuclear cells (PBMCs) and antigen-specific T-cell lines. clobenpropit 10-22 interleukin 5 Homo sapiens 140-153 15084444-5 2004 alpha-Fluoromethylhistidine (FMH, 25 microg per site), a selective histidine decarboxylase inhibitor prevented the ameliorating effect of clobenpropit on the working memory deficits induced by MK-801. clobenpropit 138-150 histidine decarboxylase Rattus norvegicus 67-90 15179677-5 2004 H(3)receptor agonist, immepip, and histidine decarboxylase, alpha-fluoromethylhistidine reversed the ameliorating effect of clobenpropit on seizure development in a dose-dependent manner. clobenpropit 124-136 histidine decarboxylase Rattus norvegicus 35-58 15082882-13 2004 Pretreatment with histamine H(3) receptor antagonist clobenpropit (0,4 micromol i.c.v.) clobenpropit 53-65 histamine receptor H3 Rattus norvegicus 18-41 14729385-9 2004 Pretreatment with the selective histamine H3 receptor antagonist, clobenpropit (100 nM), blocked the sympathoinhibitory effect of (R)-alpha-methylhistamine on the neurogenic sympathetic vasoconstriction. clobenpropit 66-78 histamine receptor H3 Homo sapiens 32-53 12372902-1 2002 Optical difference spectroscopy was used to identify and quantify human adrenal microsomal and mitochondrial cytochrome P450 enzyme interactions with the histamine H(3) receptor antagonists thioperamide, clobenpropit and ciproxifan. clobenpropit 204-216 histamine receptor H3 Homo sapiens 154-177 12787830-7 2003 Clobenpropit (1 nM, a potent histamine H(3) receptor antagonist) "antagonised" the suppressive effect of SKF 91488 and histamine-evoked relaxation was restored. clobenpropit 0-12 histamine receptor H3 Rattus norvegicus 29-52 11752226-8 2002 The cAMP-dependent protein kinase blockers Rp-cAMPs and PKI14-22 could impair the effects of thioperamide and clobenpropit, respectively. clobenpropit 110-122 calmodulin 2, pseudogene 1 Rattus norvegicus 46-51 12235264-5 2002 Agonists selective for H(2) (dimaprit), H(3/4) (R-(-)-alpha-methylhistamine), and H(4) (clobenpropit) were capable of inducing the release of bioactive IL-16 because CD8(+) cell supernatants induced CD4(+) cell migration, which was abrogated by an anti-IL-16 antibody. clobenpropit 88-100 interleukin 16 Homo sapiens 152-157 12235264-5 2002 Agonists selective for H(2) (dimaprit), H(3/4) (R-(-)-alpha-methylhistamine), and H(4) (clobenpropit) were capable of inducing the release of bioactive IL-16 because CD8(+) cell supernatants induced CD4(+) cell migration, which was abrogated by an anti-IL-16 antibody. clobenpropit 88-100 CD8a molecule Homo sapiens 166-169 12235264-5 2002 Agonists selective for H(2) (dimaprit), H(3/4) (R-(-)-alpha-methylhistamine), and H(4) (clobenpropit) were capable of inducing the release of bioactive IL-16 because CD8(+) cell supernatants induced CD4(+) cell migration, which was abrogated by an anti-IL-16 antibody. clobenpropit 88-100 CD4 molecule Homo sapiens 199-202 12235264-5 2002 Agonists selective for H(2) (dimaprit), H(3/4) (R-(-)-alpha-methylhistamine), and H(4) (clobenpropit) were capable of inducing the release of bioactive IL-16 because CD8(+) cell supernatants induced CD4(+) cell migration, which was abrogated by an anti-IL-16 antibody. clobenpropit 88-100 interleukin 16 Homo sapiens 253-258 12359275-7 2002 Pretreatment with either of the selective histamine H(3) receptor antagonists, thioperamide and clobenpropit, blocked the sympathoinhibitory effect of (R)-alpha-methylhistamine in porcine turbinate mucosa. clobenpropit 96-108 histamine receptor H3 Homo sapiens 42-65 12503632-5 2002 Ligand-binding studies using Pfi-013 expressed in HEK-293Galpha15 cells, demonstrates specific binding to histamine with a Kd of 3.28 +/- 0.76 nM and possesses a unique rank order of potency against known histaminergic compounds in a competitive ligand-binding assay (histamine > clobenpropit > iodophenpropit > thioperamide > R-alpha-methylhistamine > cimetidine > pyrilamine). clobenpropit 283-295 histamine receptor H4 Homo sapiens 29-36 10973974-7 2000 In functional assays, not only an H3 receptor agonist, R-(alpha)-methylhistamine, but also a H3 receptor antagonist, clobenpropit, and a neuroleptic, clozapine, activated GPRv53-expressing cells. clobenpropit 117-129 histamine receptor H4 Homo sapiens 171-177 11742589-1 2001 AIM: The effect of clobenpropit on regional cerebral blood flow (rCBF) was investigated in the rat hippocampus. clobenpropit 19-31 CCAAT/enhancer binding protein zeta Rattus norvegicus 65-69 11742589-4 2001 RESULTS: Intracerebroventricular (icv) injection of clobenpropit (20, 50 microg), a representative H3-antagonist, dose-dependently and significantly increased rCBF in the hippocampus. clobenpropit 52-64 CCAAT/enhancer binding protein zeta Rattus norvegicus 159-163 11742589-5 2001 The increase of rCBF induced by clobenpropit was enhanced by metoprine (1, 2 mg/kg), a selective histamine N-methyltransferase inhibitor; however, was antagonized by an H3-agonist, (R)-alpha-methylhistamine (5 microg), an H(1)-antagonist, mepyramine (5-10 mg/kg), and an H2-antagonist, zolantidine (10 mg/kg). clobenpropit 32-44 CCAAT/enhancer binding protein zeta Rattus norvegicus 16-20 9017245-0 1996 Brain penetration of the histamine H3 receptor antagonists thioperamide and clobenpropit in rat and mouse, determined with ex vivo [125I]iodophenpropit binding. clobenpropit 76-88 histamine receptor H3 Rattus norvegicus 25-46 10556922-1 1999 1 We have investigated the binding of a novel histamine H3-receptor antagonist radioligand, [3H]- clobenpropit ([3H]-VUF9153), to guinea-pig cerebral cortex membranes. clobenpropit 117-124 histamine H3 receptor Cavia porcellus 46-67 10556922-10 1999 5 A series of histamine H3-receptor ligands expressed affinity values for sites labelled with [3H]-clobenpropit which were not significantly different from those estimated when [3H]-R-alpha-MH was used to label histamine H3-receptors in guinea-pig cerebral cortex membranes. clobenpropit 99-111 histamine H3 receptor Cavia porcellus 14-35 9874165-9 1998 In conclusion, intrahypothalamic perfusion of the histamine H3 receptor agonist, immepip and the histamine H3 receptor antagonist, clobenpropit, potently and oppositely modulated in vivo histamine release from the anterior hypothalamic area. clobenpropit 131-143 histamine receptor H3 Rattus norvegicus 97-118 9826104-0 1998 Effect of clobenpropit, a centrally acting histamine H3-receptor antagonist, on electroshock- and pentylenetetrazol-induced seizures in mice. clobenpropit 10-22 histamine receptor H3 Mus musculus 43-64 9017245-1 1996 We investigated the brain penetration of the histamine H3 receptor antagonists thioperamide and clobenpropit using ex vivo [125I]iodophenpropit binding. clobenpropit 96-108 histamine receptor H3 Rattus norvegicus 45-66 7957622-0 1994 Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in mice. clobenpropit 0-12 histamine receptor H3 Mus musculus 31-52 8982515-9 1996 The inhibitory effect of 100 microM histamine was completely prevented by the highly selective histamine H3 receptor antagonist, clobenpropit but was resistant to antagonism by triprolidine and cimetidine, antagonists at histamine H1 and H2 but not H3 receptors. clobenpropit 129-141 histamine receptor H3 Rattus norvegicus 95-116 7957622-0 1994 Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in mice. clobenpropit 14-22 histamine receptor H3 Mus musculus 31-52 7957622-4 1994 These findings suggest that the effect of clobenpropit on electrically induced convulsions is due to an increase in endogenous histamine release in the brain, which is consistent with biochemical results that clobenpropit increased brain histidine decarboxylase activity dose dependently. clobenpropit 42-54 histidine decarboxylase Mus musculus 238-261 7957622-4 1994 These findings suggest that the effect of clobenpropit on electrically induced convulsions is due to an increase in endogenous histamine release in the brain, which is consistent with biochemical results that clobenpropit increased brain histidine decarboxylase activity dose dependently. clobenpropit 209-221 histidine decarboxylase Mus musculus 238-261 7957622-5 1994 The anticonvulsive effect of clobenpropit was antagonized by mepyramine, a histamine H1 receptor antagonist, but not by zolantidine, a histamine H2 receptor antagonist, indicating that histamine released by the anticonvulsant effect of clobenpropit interacts with histamine H1 receptors of postsynaptic neurons. clobenpropit 29-41 histamine receptor H1 Mus musculus 75-96 30536350-0 2018 Histamine H3 receptor antagonist Clobenpropit protects propofol-induced apoptosis of hippocampal neurons through PI3K/AKT pathway. clobenpropit 33-45 histamine receptor H3 Rattus norvegicus 0-21 34942919-1 2021 Clobenpropit (CLO), an antagonist on histamine H3 receptors (HH3R), has been shown to protect NMDA-induced neuronal necrosis in cortical neuronal cell culture from rats. clobenpropit 0-12 histamine receptor H3 Rattus norvegicus 37-59 34942919-1 2021 Clobenpropit (CLO), an antagonist on histamine H3 receptors (HH3R), has been shown to protect NMDA-induced neuronal necrosis in cortical neuronal cell culture from rats. clobenpropit 0-12 histamine receptor H3 Rattus norvegicus 61-65 34942919-1 2021 Clobenpropit (CLO), an antagonist on histamine H3 receptors (HH3R), has been shown to protect NMDA-induced neuronal necrosis in cortical neuronal cell culture from rats. clobenpropit 14-17 histamine receptor H3 Rattus norvegicus 37-59 34942919-1 2021 Clobenpropit (CLO), an antagonist on histamine H3 receptors (HH3R), has been shown to protect NMDA-induced neuronal necrosis in cortical neuronal cell culture from rats. clobenpropit 14-17 histamine receptor H3 Rattus norvegicus 61-65 30536350-10 2018 CONCLUSIONS: Clobenpropit protects propofol-induced neuronal apoptosis through activating PI3K/AKT pathway. clobenpropit 13-25 AKT serine/threonine kinase 1 Rattus norvegicus 95-98 8119312-0 1993 Pharmacological activity of VUF 9153, an isothiourea histamine H3 receptor antagonist. clobenpropit 28-36 histamine receptor H3 Rattus norvegicus 53-74 8119312-1 1993 The pharmacological activity of the histamine H3 receptor antagonist VUF 9153 (S-[3-(4(5)-imidazolyl)]propyl-N-(4-chlorobenzyl)isothiourea) has been investigated in vitro and in vivo. clobenpropit 69-77 histamine receptor H3 Rattus norvegicus 36-57 8119312-1 1993 The pharmacological activity of the histamine H3 receptor antagonist VUF 9153 (S-[3-(4(5)-imidazolyl)]propyl-N-(4-chlorobenzyl)isothiourea) has been investigated in vitro and in vivo. clobenpropit 79-138 histamine receptor H3 Rattus norvegicus 36-57 30536350-0 2018 Histamine H3 receptor antagonist Clobenpropit protects propofol-induced apoptosis of hippocampal neurons through PI3K/AKT pathway. clobenpropit 33-45 AKT serine/threonine kinase 1 Rattus norvegicus 118-121 30536350-1 2018 OBJECTIVE: The aim of the study was to explore whether histamine H3 receptor antagonist Clobenpropit could protect propofol-induced neurotoxicity in hippocampal neurons. clobenpropit 88-100 histamine receptor H3 Rattus norvegicus 55-76 30536350-8 2018 Protein expressions of cleaved-caspase-3 and Bax/Bcl2 were remarkably downregulated in neurons treated with Clobenpropit. clobenpropit 108-120 BCL2 associated X, apoptosis regulator Rattus norvegicus 45-48 30536350-8 2018 Protein expressions of cleaved-caspase-3 and Bax/Bcl2 were remarkably downregulated in neurons treated with Clobenpropit. clobenpropit 108-120 BCL2, apoptosis regulator Rattus norvegicus 49-53 30536350-9 2018 LY294002 induction remarkably reverses the protective role of Clobenpropit in neuronal apoptosis, manifesting as downregulated PI3K and p-AKT after LY294002 treatment. clobenpropit 62-74 AKT serine/threonine kinase 1 Rattus norvegicus 138-141 29414147-0 2018 Clobenpropit, a histamine H3 receptor antagonist/inverse agonist, inhibits [3H]-dopamine uptake by human neuroblastoma SH-SY5Y cells and rat brain synaptosomes. clobenpropit 0-12 histamine receptor H3 Homo sapiens 16-37 30071054-11 2018 Furthermore, it was found that the premedication with prazosin, yohimbine, 6-hydroxydopamine and the vasopressin V1a receptor antagonist blocked the effects of clobenpropit. clobenpropit 160-172 arginine vasopressin receptor 1A Rattus norvegicus 101-125 29414147-7 2018 Clobenpropit inhibited [3H]-dopamine uptake (maximum inhibition 82.7+-2.8%, IC50 490nM), and the effect was reproduced by the H3R antagonist/inverse agonist iodophenpropit, but not by the agonists R-alpha-methylhistamine and immepip or the antagonists/inverse agonists ciproxifan and A-331440. clobenpropit 0-12 histamine receptor H3 Homo sapiens 126-129 29414147-1 2018 BACKGROUND: Clobenpropit, a potent antagonist/inverse agonist at the histamine H3 receptor (H3R), reduced the cytotoxic action of 6-hydroxydopamine (6-OHDA) in neuroblastoma SH-SY5Y cells transfected with the human H3R. clobenpropit 12-24 histamine receptor H3 Homo sapiens 69-90 29414147-9 2018 Modeling of the human NET and DAT obtained by homology from the crystal of Drosophila melanogaster DAT showed that clobenpropit can bind to a site also recognized in both transporters by nisoxetine, a potent NET inhibitor. clobenpropit 115-127 solute carrier family 6 member 3 Homo sapiens 30-33 29414147-1 2018 BACKGROUND: Clobenpropit, a potent antagonist/inverse agonist at the histamine H3 receptor (H3R), reduced the cytotoxic action of 6-hydroxydopamine (6-OHDA) in neuroblastoma SH-SY5Y cells transfected with the human H3R. clobenpropit 12-24 histamine receptor H3 Homo sapiens 92-95 29414147-9 2018 Modeling of the human NET and DAT obtained by homology from the crystal of Drosophila melanogaster DAT showed that clobenpropit can bind to a site also recognized in both transporters by nisoxetine, a potent NET inhibitor. clobenpropit 115-127 Dopamine transporter Drosophila melanogaster 99-102 29414147-1 2018 BACKGROUND: Clobenpropit, a potent antagonist/inverse agonist at the histamine H3 receptor (H3R), reduced the cytotoxic action of 6-hydroxydopamine (6-OHDA) in neuroblastoma SH-SY5Y cells transfected with the human H3R. clobenpropit 12-24 histamine receptor H3 Homo sapiens 215-218 29414147-4 2018 Clobenpropit binding to the human norepinephrine (NET) and dopamine (DAT) transporters was analyzed by molecular modeling. clobenpropit 0-12 solute carrier family 6 member 3 Homo sapiens 69-72 26907350-6 2016 At week 18, feeding with the diets containing cimetidine (Hrh2 antagonist) and clobenpropit (Hrh3 antagonist/inverse agonist) significantly lowered the multiplicity of colonic adenocarcinoma. clobenpropit 79-91 histamine receptor H3 Mus musculus 93-97 26907350-9 2016 Because clobenpropit is also known to be a Hrh4 receptor agonist, Hrh2, Hrh3 and Hrh4 may be involved in inflammation-related colorectal carcinogenesis. clobenpropit 8-20 histamine receptor H4 Mus musculus 43-47 26907350-9 2016 Because clobenpropit is also known to be a Hrh4 receptor agonist, Hrh2, Hrh3 and Hrh4 may be involved in inflammation-related colorectal carcinogenesis. clobenpropit 8-20 histamine receptor H2 Mus musculus 66-70 26907350-9 2016 Because clobenpropit is also known to be a Hrh4 receptor agonist, Hrh2, Hrh3 and Hrh4 may be involved in inflammation-related colorectal carcinogenesis. clobenpropit 8-20 histamine receptor H3 Mus musculus 72-76 26907350-9 2016 Because clobenpropit is also known to be a Hrh4 receptor agonist, Hrh2, Hrh3 and Hrh4 may be involved in inflammation-related colorectal carcinogenesis. clobenpropit 8-20 histamine receptor H4 Mus musculus 81-85 25024609-9 2014 Clobenpropit up-regulated E-cadherin, but down-regulated vimentin and matrix metalloproteinase 9 in real-time polymerase chain reaction. clobenpropit 0-12 cadherin 1 Homo sapiens 26-36 25762718-8 2015 RESULTS: Clobenpropit, administered systemically or directly into the hippocampus, decreased immobility during the forced swim test; systemic injections reversed memory deficits and increased hippocampal GluN2A protein levels. clobenpropit 9-21 glutamate ionotropic receptor NMDA type subunit 2A Rattus norvegicus 204-210 25762718-13 2015 Clobenpropit reverses memory deficits and increases hippocampal GluN2A expression without modifying anxiety-related phenotypes or EPSCs in CA1 pyramidal neurons. clobenpropit 0-12 glutamate ionotropic receptor NMDA type subunit 2A Rattus norvegicus 64-70 25024609-9 2014 Clobenpropit up-regulated E-cadherin, but down-regulated vimentin and matrix metalloproteinase 9 in real-time polymerase chain reaction. clobenpropit 0-12 vimentin Homo sapiens 57-65 25024609-9 2014 Clobenpropit up-regulated E-cadherin, but down-regulated vimentin and matrix metalloproteinase 9 in real-time polymerase chain reaction. clobenpropit 0-12 matrix metallopeptidase 9 Homo sapiens 70-96 25024609-10 2014 Also, clobenpropit inhibited tumor growth (gemcitabine 294 +- 46 mg vs combination 154 +- 54 mg, P = 0.02) and enhanced apoptosis in combination with gemcitabine (control 2.5%, gemcitabine 25.8%, clobenpropit 9.7% and combination 40.9%, P = 0.001) by up-regulation of E-cadherin and down-regulation of Zeb1 in Panc-1 xenograft mouse. clobenpropit 6-18 cadherin 1 Mus musculus 268-278 25024609-10 2014 Also, clobenpropit inhibited tumor growth (gemcitabine 294 +- 46 mg vs combination 154 +- 54 mg, P = 0.02) and enhanced apoptosis in combination with gemcitabine (control 2.5%, gemcitabine 25.8%, clobenpropit 9.7% and combination 40.9%, P = 0.001) by up-regulation of E-cadherin and down-regulation of Zeb1 in Panc-1 xenograft mouse. clobenpropit 6-18 zinc finger E-box binding homeobox 1 Mus musculus 302-306 25024609-10 2014 Also, clobenpropit inhibited tumor growth (gemcitabine 294 +- 46 mg vs combination 154 +- 54 mg, P = 0.02) and enhanced apoptosis in combination with gemcitabine (control 2.5%, gemcitabine 25.8%, clobenpropit 9.7% and combination 40.9%, P = 0.001) by up-regulation of E-cadherin and down-regulation of Zeb1 in Panc-1 xenograft mouse. clobenpropit 6-18 pancreas protein 1 Mus musculus 310-316 20197375-0 2010 Implementation of a fluorescence-based screening assay identifies histamine H3 receptor antagonists clobenpropit and iodophenpropit as subunit-selective N-methyl-D-aspartate receptor antagonists. clobenpropit 100-112 glutamate ionotropic receptor NMDA type subunit 1 L homeolog Xenopus laevis 153-182 23220277-4 2013 Clobenpropit is then docked into the binding pocket of H4R and two different binding modes can be identified. clobenpropit 0-12 histamine receptor H4 Homo sapiens 55-58 21272571-6 2011 Clobenpropit (histamine H(3) receptor antagonist, 1muM) canceled the alpha-methylhistamine-induced decrease in the periarterial nerve stimulation-induced vasoconstriction and noradrenaline release and periarterial nerve stimulation-induced vasodilation. clobenpropit 0-12 histamine receptor H3 Rattus norvegicus 14-37 22003888-5 2011 We have designed and synthesized a series of clobenpropit (N-(4-chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothiourea) derivatives to investigate H(4)R-ligand interactions and ligand binding orientations. clobenpropit 45-57 histamine receptor H4 Homo sapiens 147-152 22003888-6 2011 Interestingly, our studies indicate that clobenpropit (2) itself can bind to H(4)R in two distinct binding modes, while the addition of a cyclohexyl group to the clobenpropit isothiourea moiety allows VUF5228 (5) to adopt only one specific binding mode in the H(4)R binding pocket. clobenpropit 41-53 histamine receptor H4 Homo sapiens 77-82 22003888-6 2011 Interestingly, our studies indicate that clobenpropit (2) itself can bind to H(4)R in two distinct binding modes, while the addition of a cyclohexyl group to the clobenpropit isothiourea moiety allows VUF5228 (5) to adopt only one specific binding mode in the H(4)R binding pocket. clobenpropit 41-53 histamine receptor H4 Homo sapiens 260-265 20511290-1 2011 Clobenpropit, an H( 3) receptor antagonist, has been reported to modulate both the release of neurotransmitters and also the activity of histidine decarboxylase (HDC). clobenpropit 0-12 histidine decarboxylase Mus musculus 137-160 20511290-1 2011 Clobenpropit, an H( 3) receptor antagonist, has been reported to modulate both the release of neurotransmitters and also the activity of histidine decarboxylase (HDC). clobenpropit 0-12 histidine decarboxylase Mus musculus 162-165 20197375-6 2010 This strategy identified several novel modulators of NMDA receptor function, including the histamine H3 receptor antagonists clobenpropit and iodophenpropit, as well as the vanilloid receptor transient receptor potential cation channel, subfamily V, member 1 (TRPV1) antagonist capsazepine. clobenpropit 125-137 glutamate ionotropic receptor NMDA type subunit 1 L homeolog Xenopus laevis 53-66 20045936-7 2010 This vasodilation was abolished by endothelium removal and attenuated by histamine H(3) receptor antagonists, thioperamide and clobenpropit, but not by chlorpheniramine (histamine H(1) receptor antagonist) and cimetidine (histamine H(2) receptor antagonist). clobenpropit 127-139 histamine receptor H 2 Rattus norvegicus 222-245 19414267-1 2009 Previous studies have demonstrated that clobenpropit (N-(4-chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothiourea) binds to both the human histamine H(3) receptor (H(3)R) and H(4) receptor (H(4)R). clobenpropit 40-52 histamine receptor H3 Homo sapiens 139-162 19414267-1 2009 Previous studies have demonstrated that clobenpropit (N-(4-chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothiourea) binds to both the human histamine H(3) receptor (H(3)R) and H(4) receptor (H(4)R). clobenpropit 40-52 histamine receptor H4 Homo sapiens 175-196 19414267-2 2009 In this paper, we describe the synthesis and pharmacological characterization of a series of clobenpropit analogs, which vary in the functional group adjacent to the isothiourea moiety in order to study structural requirements for H(3)R and H(4)R ligands. clobenpropit 93-105 histamine receptor H3 Homo sapiens 231-246 19281909-8 2009 H(4)R agonists (clobenpropit and 4-methylhistamine) induced AP-1 in T(H)2 cells but not in T(H)1 cells. clobenpropit 16-28 JunB proto-oncogene, AP-1 transcription factor subunit Homo sapiens 60-64 18782117-8 2008 Histamine as well as the H4R agonist clobenpropit induced an enhanced chemotaxis in the skin DC migration assay. clobenpropit 37-49 histamine receptor H4 Mus musculus 25-28