PMID-sentid Pub_year Sent_text comp_official_name comp_offset protein_name organism prot_offset 29558203-9 2018 Increasing adenosine levels, as well as stimulating the adenosine receptors A2A and A2B, exhibited strong prodegenerative effects, whereas conversely, lowering adenosine levels by inhibition of CD73 resulted in protective effects against degeneration. Adenosine 56-65 immunoglobulin kappa variable 2D-29 Homo sapiens 76-87 29857029-4 2018 At cellular level, Rhes interferes with adenosine A2A- and dopamine D1 receptor-dependent cAMP/PKA pathway, upstream of the activation of the heterotrimeric G protein complex. Cyclic AMP 90-94 immunoglobulin kappa variable 2D-29 Homo sapiens 50-79 29880250-0 2018 Identification of novel thiazolo[5,4-d]pyrimidine derivatives as human A1 and A2A adenosine receptor antagonists/inverse agonists. Thiazolo[5,4-d]pyrimidine 24-49 immunoglobulin kappa variable 2D-29 Homo sapiens 78-81 30044380-0 2018 Comparative Study of Carborane- and Phenyl-Modified Adenosine Derivatives as Ligands for the A2A and A3 Adenosine Receptors Based on a Rigid in Silico Docking and Radioligand Replacement Assay. carborane 21-30 immunoglobulin kappa variable 2D-29 Homo sapiens 93-96 30044380-0 2018 Comparative Study of Carborane- and Phenyl-Modified Adenosine Derivatives as Ligands for the A2A and A3 Adenosine Receptors Based on a Rigid in Silico Docking and Radioligand Replacement Assay. Adenosine 52-61 immunoglobulin kappa variable 2D-29 Homo sapiens 93-96 29533161-1 2018 OBJECTIVE: Polydeoxyribonucleotide as adenosine receptor (A2A) agonist has been used in plastic surgery and dermatology related to its regenerative property. Polydeoxyribonucleotides 11-34 immunoglobulin kappa variable 2D-29 Homo sapiens 58-61 27915051-2 2017 This review makes the point that caffeine is - in low doses - an antagonist of adenosine acting at A1, A2A and A2B receptors. Caffeine 33-41 immunoglobulin kappa variable 2D-29 Homo sapiens 103-106 28114825-0 2017 The role of 5-arylalkylamino- and 5-piperazino- moieties on the 7-aminopyrazolo[4,3-d]pyrimidine core in affecting adenosine A1 and A2A receptor affinity and selectivity profiles. 7-aminopyrazolo(4,3-d)pyrimidine 64-96 immunoglobulin kappa variable 2D-29 Homo sapiens 132-135 28114825-1 2017 New 7-amino-2-phenylpyrazolo[4,3-d]pyrimidine derivatives, substituted at the 5-position with aryl(alkyl)amino- and 4-substituted-piperazin-1-yl- moieties, were synthesized with the aim of targeting human (h) adenosine A1 and/or A2A receptor subtypes. 7-amino-2-phenylpyrazolo[4,3-d]pyrimidine 4-45 immunoglobulin kappa variable 2D-29 Homo sapiens 229-232 28734062-4 2018 Therefore, a series of 3-phenylcarboxamidocoumarins were synthesized and their affinity for the human AR subtypes was screened by radioligand binding assays for A1 , A2A and A3 receptors and for A2B by adenylyl cyclase assay. 3-phenylcarboxamidocoumarins 23-51 immunoglobulin kappa variable 2D-29 Homo sapiens 166-169 27915051-2 2017 This review makes the point that caffeine is - in low doses - an antagonist of adenosine acting at A1, A2A and A2B receptors. Adenosine 79-88 immunoglobulin kappa variable 2D-29 Homo sapiens 103-106 26796668-5 2016 Using extensive multiscale computer modelling, we find a marked propensity of DHA for interaction with both A2A and D2 receptors, which leads to an increased rate of receptor oligomerisation. Docosahexaenoic Acids 78-81 immunoglobulin kappa variable 2D-29 Homo sapiens 108-118 27216633-0 2016 Discovery of potent adenosine A2a antagonists as potential anti-Parkinson disease agents. Adenosine 20-29 immunoglobulin kappa variable 2D-29 Homo sapiens 30-33 27216633-3 2016 In this study, we combined extensive pharmacophore modeling and quantitative structure-activity relationship (QSAR) analysis to explore the structural requirements for potent Adenosine A2A antagonists. Adenosine 175-184 immunoglobulin kappa variable 2D-29 Homo sapiens 185-188 27216633-6 2016 Best QSAR models and their associated pharmacophore hypotheses were validated by identification of several novel Adenosine A2A antagonist leads retrieved from the National Cancer Institute (NCI) structural database. Adenosine 113-122 immunoglobulin kappa variable 2D-29 Homo sapiens 123-126 27161878-0 2016 Exploring the 2- and 5-positions of the pyrazolo[4,3-d]pyrimidin-7-amino scaffold to target human A1 and A2A adenosine receptors. pyrazolo[4,3-d]pyrimidin-7-amino 40-72 immunoglobulin kappa variable 2D-29 Homo sapiens 105-108 27161878-4 2016 In particular, the 2-(2-methoxybenzyl)-5-(5-methylfuran-2-yl) derivative 25 possessed the highest hA2A and hA1 AR affinities (Ki=3.62nM and 18nM, respectively) and behaved as potent antagonist at both these receptors (cAMP assays). 2-(2-methoxybenzyl)-5-(5-methylfuran-2-yl 19-60 immunoglobulin kappa variable 2D-29 Homo sapiens 98-102 27161878-4 2016 In particular, the 2-(2-methoxybenzyl)-5-(5-methylfuran-2-yl) derivative 25 possessed the highest hA2A and hA1 AR affinities (Ki=3.62nM and 18nM, respectively) and behaved as potent antagonist at both these receptors (cAMP assays). Cyclic AMP 218-222 immunoglobulin kappa variable 2D-29 Homo sapiens 98-102 27161878-5 2016 Its 2-(2-hydroxybenzyl) analog 26 also showed a high affinity for the hA2A AR (Ki=5.26nM) and was 22-fold selective versus the hA1 subtype. hydroxybenzyl 9-22 immunoglobulin kappa variable 2D-29 Homo sapiens 70-74 26873265-0 2016 Pharmacophore generation, atom-based 3D-QSAR, HQSAR and activity cliff analyses of benzothiazine and deazaxanthine derivatives as dual A2A antagonists/MAO-B inhibitors. benzothiazine 83-96 immunoglobulin kappa variable 2D-29 Homo sapiens 135-138 26873265-0 2016 Pharmacophore generation, atom-based 3D-QSAR, HQSAR and activity cliff analyses of benzothiazine and deazaxanthine derivatives as dual A2A antagonists/MAO-B inhibitors. 7-deazaxanthine 101-114 immunoglobulin kappa variable 2D-29 Homo sapiens 135-138 26796668-6 2016 Bioluminescence resonance energy transfer (BRET) experiments performed on living cells suggest that this DHA effect on the oligomerisation of A2A and D2 receptors is purely kinetic. Docosahexaenoic Acids 105-108 immunoglobulin kappa variable 2D-29 Homo sapiens 142-152 25770019-2 2015 The aim of this study was to assess the expression of CD73 and A2A in immune cells and the effect of activation of A2A by an adenosine analogue on apoptosis in patients with obesity and type 2 diabetes mellitus (T2D). Adenosine 125-134 immunoglobulin kappa variable 2D-29 Homo sapiens 115-118 25384972-0 2015 Human monocyte recognition of adenosine-based cyclic dinucleotides unveils the A2a Galphas protein-coupled receptor tonic inhibition of mitochondrially induced cell death. adenosine-based cyclic dinucleotides 30-66 immunoglobulin kappa variable 2D-29 Homo sapiens 79-82 25384972-6 2015 The blockade of basal (adenosine-free) signaling from A2a inhibits protein kinase A (PKA) activity, thereby recruiting cytosolic p53, which opens the mitochondrial permeability transition pore and impairs mitochondrial respiration, resulting in apoptosis. Adenosine 23-32 immunoglobulin kappa variable 2D-29 Homo sapiens 54-57 25384972-9 2015 Treatment with cyclic di-AMP selectively depleted A2a-expressing monocytes and their precursors via apoptosis. cyclic diadenosine phosphate 15-28 immunoglobulin kappa variable 2D-29 Homo sapiens 50-53 25384972-10 2015 Thus, monocyte recognition of cyclic dinucleotides unravels a novel proapoptotic pathway: the A2a Galphas protein-coupled receptor (GPCR)-driven tonic inhibitory signaling of mitochondrion-induced cell death. cyclic dinucleotides 30-50 immunoglobulin kappa variable 2D-29 Homo sapiens 94-97 25175458-6 2014 Special emphasis is given to in vivo microdialysis findings demonstrating the functional role putative A2A/D2 heteromers on striato-pallidal GABA neurons play in the modulation of this pathway, in which A2A receptors inhibit D2 receptor signaling. gamma-Aminobutyric Acid 141-145 immunoglobulin kappa variable 2D-29 Homo sapiens 103-109 25393959-10 2014 In addition, SQ22536 (an adenylate cyclase inhibitor) and ZM241385 (a potent adenosine receptor A2A antagonist) attenuated the effect of adenosine on platelet aggregation induced by ADP and intraplatelet level of cAMP. ZM 241385 58-66 immunoglobulin kappa variable 2D-29 Homo sapiens 96-99 25393959-10 2014 In addition, SQ22536 (an adenylate cyclase inhibitor) and ZM241385 (a potent adenosine receptor A2A antagonist) attenuated the effect of adenosine on platelet aggregation induced by ADP and intraplatelet level of cAMP. Adenosine 77-86 immunoglobulin kappa variable 2D-29 Homo sapiens 96-99 25393959-10 2014 In addition, SQ22536 (an adenylate cyclase inhibitor) and ZM241385 (a potent adenosine receptor A2A antagonist) attenuated the effect of adenosine on platelet aggregation induced by ADP and intraplatelet level of cAMP. Adenosine Diphosphate 182-185 immunoglobulin kappa variable 2D-29 Homo sapiens 96-99 25393959-13 2014 Docking of adenosine and inosine inside A2A showed that the main difference is the formation by adenosine of an additional hydrogen bond between the NH2 of the adenine group and the residues Asn253 in H6 and Glu169 in EL2 of the A2A receptor. Adenosine 11-20 immunoglobulin kappa variable 2D-29 Homo sapiens 40-43 25393959-13 2014 Docking of adenosine and inosine inside A2A showed that the main difference is the formation by adenosine of an additional hydrogen bond between the NH2 of the adenine group and the residues Asn253 in H6 and Glu169 in EL2 of the A2A receptor. Adenosine 11-20 immunoglobulin kappa variable 2D-29 Homo sapiens 229-232 25393959-13 2014 Docking of adenosine and inosine inside A2A showed that the main difference is the formation by adenosine of an additional hydrogen bond between the NH2 of the adenine group and the residues Asn253 in H6 and Glu169 in EL2 of the A2A receptor. Inosine 25-32 immunoglobulin kappa variable 2D-29 Homo sapiens 40-43 25393959-13 2014 Docking of adenosine and inosine inside A2A showed that the main difference is the formation by adenosine of an additional hydrogen bond between the NH2 of the adenine group and the residues Asn253 in H6 and Glu169 in EL2 of the A2A receptor. Inosine 25-32 immunoglobulin kappa variable 2D-29 Homo sapiens 229-232 25393959-13 2014 Docking of adenosine and inosine inside A2A showed that the main difference is the formation by adenosine of an additional hydrogen bond between the NH2 of the adenine group and the residues Asn253 in H6 and Glu169 in EL2 of the A2A receptor. Adenosine 96-105 immunoglobulin kappa variable 2D-29 Homo sapiens 40-43 25393959-13 2014 Docking of adenosine and inosine inside A2A showed that the main difference is the formation by adenosine of an additional hydrogen bond between the NH2 of the adenine group and the residues Asn253 in H6 and Glu169 in EL2 of the A2A receptor. Adenosine 96-105 immunoglobulin kappa variable 2D-29 Homo sapiens 229-232 25393959-13 2014 Docking of adenosine and inosine inside A2A showed that the main difference is the formation by adenosine of an additional hydrogen bond between the NH2 of the adenine group and the residues Asn253 in H6 and Glu169 in EL2 of the A2A receptor. Hydrogen 123-131 immunoglobulin kappa variable 2D-29 Homo sapiens 40-43 25393959-13 2014 Docking of adenosine and inosine inside A2A showed that the main difference is the formation by adenosine of an additional hydrogen bond between the NH2 of the adenine group and the residues Asn253 in H6 and Glu169 in EL2 of the A2A receptor. Hydrogen 123-131 immunoglobulin kappa variable 2D-29 Homo sapiens 229-232 25393959-13 2014 Docking of adenosine and inosine inside A2A showed that the main difference is the formation by adenosine of an additional hydrogen bond between the NH2 of the adenine group and the residues Asn253 in H6 and Glu169 in EL2 of the A2A receptor. Adenine 160-167 immunoglobulin kappa variable 2D-29 Homo sapiens 40-43 25393959-13 2014 Docking of adenosine and inosine inside A2A showed that the main difference is the formation by adenosine of an additional hydrogen bond between the NH2 of the adenine group and the residues Asn253 in H6 and Glu169 in EL2 of the A2A receptor. Adenine 160-167 immunoglobulin kappa variable 2D-29 Homo sapiens 229-232 24652540-0 2014 Human monocytes respond to extracellular cAMP through A2A and A2B adenosine receptors. Cyclic AMP 41-45 immunoglobulin kappa variable 2D-29 Homo sapiens 54-57 24652540-8 2014 The effects of extracellular cAMP on monocytes are mediated by CD73 ecto-5"-nucleotidase and A2A and A2B adenosine receptors, as selective antagonists could reverse its effects. Cyclic AMP 29-33 immunoglobulin kappa variable 2D-29 Homo sapiens 93-96 24595664-16 2014 We conclude that (a) A1AR is unnecessary for LAD2 degranulation or AR enhancement; (b) A2A, A2B, and A3 ARs all contribute to pharmacologic AR enhancement of LAD2 and BMMC degranulation; and (c) LAD2 cells depend on microenvironmental adenosine to trigger AR modulation. Adenosine 235-244 immunoglobulin kappa variable 2D-29 Homo sapiens 87-90 24483158-2 2014 Polydeoxyribonucleotide (PDRN), an adenosine A2A receptor agonist, improves wound healing in diabetic mice. Polydeoxyribonucleotides 0-23 immunoglobulin kappa variable 2D-29 Homo sapiens 45-48 24024783-3 2014 Adenosine acts via specific GPCRs to either stimulate cyclic AMP formation, as exemplified by Gs -protein-coupled adenosine receptors (A2A and A2B ), or inhibit AC activity, in the case of Gi/o -coupled adenosine receptors (A1 and A3 ). Adenosine 0-9 immunoglobulin kappa variable 2D-29 Homo sapiens 135-146 23917951-6 2013 Thus adenosine A2A antagonists, safinamide, and the antiepileptic agent zonisamide can extend the duration of action of levodopa. Adenosine 5-14 immunoglobulin kappa variable 2D-29 Homo sapiens 15-18 23917951-6 2013 Thus adenosine A2A antagonists, safinamide, and the antiepileptic agent zonisamide can extend the duration of action of levodopa. Levodopa 120-128 immunoglobulin kappa variable 2D-29 Homo sapiens 15-18 23917951-11 2013 Noradrenergic alpha2A antagonism using fipamezole can potentially reduce dyskinesia. fipamezole 39-49 immunoglobulin kappa variable 2D-29 Homo sapiens 14-21 23741498-6 2013 A2A and A3ARs were able to modulate cAMP production and cell proliferation. Cyclic AMP 36-40 immunoglobulin kappa variable 2D-29 Homo sapiens 0-3 23699177-0 2013 Protective effects of pentoxifylline in pulmonary inflammation are adenosine receptor A2A dependent. Pentoxifylline 22-36 immunoglobulin kappa variable 2D-29 Homo sapiens 86-89 23699177-4 2013 Therefore, we studied the association between A2A and PTX in a murine model of LPS-induced pulmonary inflammation. Pentoxifylline 54-57 immunoglobulin kappa variable 2D-29 Homo sapiens 46-49 23699177-9 2013 Further, oxidative burst of human PMNs was A2A-dependently reduced by 53% after PTX treatment. Pentoxifylline 80-83 immunoglobulin kappa variable 2D-29 Homo sapiens 43-46 23699177-10 2013 In summary, PTX exhibits its anti-inflammatory effects in LPS-induced lung injury through an A2A-dependent pathway. Pentoxifylline 12-15 immunoglobulin kappa variable 2D-29 Homo sapiens 93-96 23631427-5 2013 The best derivative was N-(4-oxo-4H-3,1-benzothiazin-2-yl)-4-phenylbutanamide (17, Ki human A2A, 39.5 nM; IC50 human MAO-B, 34.9 nM; selective versus other AR subtypes and MAO-A), which inhibited A2AAR-induced cAMP accumulation and showed competitive, reversible MAO-B inhibition. N-(4-oxo-4H-3,1-benzothiazin-2-yl)-4-phenylbutanamide 24-77 immunoglobulin kappa variable 2D-29 Homo sapiens 92-95 23631427-5 2013 The best derivative was N-(4-oxo-4H-3,1-benzothiazin-2-yl)-4-phenylbutanamide (17, Ki human A2A, 39.5 nM; IC50 human MAO-B, 34.9 nM; selective versus other AR subtypes and MAO-A), which inhibited A2AAR-induced cAMP accumulation and showed competitive, reversible MAO-B inhibition. Cyclic AMP 210-214 immunoglobulin kappa variable 2D-29 Homo sapiens 92-95 23741498-8 2013 In human chondrocyte and osteoblast cell lines, the inhibitory effect of A2A and A3AR stimulation on the release of prostaglandin E2 (PGE2), an important lipid inflammatory mediator, was observed. Dinoprostone 116-132 immunoglobulin kappa variable 2D-29 Homo sapiens 73-76 23741498-8 2013 In human chondrocyte and osteoblast cell lines, the inhibitory effect of A2A and A3AR stimulation on the release of prostaglandin E2 (PGE2), an important lipid inflammatory mediator, was observed. Dinoprostone 134-138 immunoglobulin kappa variable 2D-29 Homo sapiens 73-76 22474168-4 2012 Unexpectedly, A2A and beta2AR agonists also synergize with melphalan, lenalidomide, bortezomib, and doxorubicin. Melphalan 59-68 immunoglobulin kappa variable 2D-29 Homo sapiens 14-17 20087854-5 2010 The endocannabinoid system is involved in the psychoactive effects of many compounds, and adenosine A2A receptors (the main receptor target of caffeine) elicit a permissive effect towards CB1 receptors, thus suggesting that A2A-CB1 receptor interaction plays a major role in the generation and maintenance of caffeine reinforcing behavior. Caffeine 143-151 immunoglobulin kappa variable 2D-29 Homo sapiens 224-231 22474168-4 2012 Unexpectedly, A2A and beta2AR agonists also synergize with melphalan, lenalidomide, bortezomib, and doxorubicin. Lenalidomide 70-82 immunoglobulin kappa variable 2D-29 Homo sapiens 14-17 22474168-4 2012 Unexpectedly, A2A and beta2AR agonists also synergize with melphalan, lenalidomide, bortezomib, and doxorubicin. Bortezomib 84-94 immunoglobulin kappa variable 2D-29 Homo sapiens 14-17 22474168-4 2012 Unexpectedly, A2A and beta2AR agonists also synergize with melphalan, lenalidomide, bortezomib, and doxorubicin. Doxorubicin 100-111 immunoglobulin kappa variable 2D-29 Homo sapiens 14-17 22142423-0 2012 Structure-activity relationships of truncated C2- or C8-substituted adenosine derivatives as dual acting A2A and A3 adenosine receptor ligands. Adenosine 68-77 immunoglobulin kappa variable 2D-29 Homo sapiens 105-108 22033526-6 2012 Putative physical and functional interactions between the A2A and cannabinoid receptors were respectively assessed by co-immuno-precipitation and co-incubating the cells with the unselective cannabinoid agonist WIN55,212-2, and the selective A2A antagonist ZM-241385. win55 211-216 immunoglobulin kappa variable 2D-29 Homo sapiens 58-61 22033526-6 2012 Putative physical and functional interactions between the A2A and cannabinoid receptors were respectively assessed by co-immuno-precipitation and co-incubating the cells with the unselective cannabinoid agonist WIN55,212-2, and the selective A2A antagonist ZM-241385. ZM 241385 257-266 immunoglobulin kappa variable 2D-29 Homo sapiens 58-61 20087854-5 2010 The endocannabinoid system is involved in the psychoactive effects of many compounds, and adenosine A2A receptors (the main receptor target of caffeine) elicit a permissive effect towards CB1 receptors, thus suggesting that A2A-CB1 receptor interaction plays a major role in the generation and maintenance of caffeine reinforcing behavior. Caffeine 309-317 immunoglobulin kappa variable 2D-29 Homo sapiens 224-231 19652957-11 2009 Since A2A, D2, and CB1 receptors coexpress on brain GABAergic neurons and reductions in markers of GABA neurotransmission have been identified in schizophrenia, a lower density of CB1 receptor induced by antipsychotics could represent an adaptative mechanism that reduces the endocannabinoid-mediated suppression of GABA release, contributing to the normalization of cognitive functions in the disorder. gamma-Aminobutyric Acid 52-56 immunoglobulin kappa variable 2D-29 Homo sapiens 6-9 21309106-3 2010 Additionally, findings on the adenosine receptor 2A (A2A) gene, which has been reported to be associated with panic disorder and also with anxiety levels after caffeine administration in a gene--environment interactional model, will be discussed. Caffeine 160-168 immunoglobulin kappa variable 2D-29 Homo sapiens 30-57 19019012-0 2009 A1 and A2a receptors mediate inhibitory effects of adenosine on the motor activity of human colon. Adenosine 51-60 immunoglobulin kappa variable 2D-29 Homo sapiens 7-10 20021407-5 2009 Six antagonists, Bromocriptine, Cabergoline, Etilevodopa, Lysuride, Melevodopa and Pramipexole, were found more potent for binding and the active amino acids residues were identified (http://www.rcsb.org/pdb/) in A2A receptor. Pramipexole 83-94 immunoglobulin kappa variable 2D-29 Homo sapiens 213-216 20021407-5 2009 Six antagonists, Bromocriptine, Cabergoline, Etilevodopa, Lysuride, Melevodopa and Pramipexole, were found more potent for binding and the active amino acids residues were identified (http://www.rcsb.org/pdb/) in A2A receptor. Bromocriptine 17-30 immunoglobulin kappa variable 2D-29 Homo sapiens 213-216 20021407-5 2009 Six antagonists, Bromocriptine, Cabergoline, Etilevodopa, Lysuride, Melevodopa and Pramipexole, were found more potent for binding and the active amino acids residues were identified (http://www.rcsb.org/pdb/) in A2A receptor. Cabergoline 32-43 immunoglobulin kappa variable 2D-29 Homo sapiens 213-216 20021407-5 2009 Six antagonists, Bromocriptine, Cabergoline, Etilevodopa, Lysuride, Melevodopa and Pramipexole, were found more potent for binding and the active amino acids residues were identified (http://www.rcsb.org/pdb/) in A2A receptor. etilevodopa 45-56 immunoglobulin kappa variable 2D-29 Homo sapiens 213-216 20021407-5 2009 Six antagonists, Bromocriptine, Cabergoline, Etilevodopa, Lysuride, Melevodopa and Pramipexole, were found more potent for binding and the active amino acids residues were identified (http://www.rcsb.org/pdb/) in A2A receptor. Lisuride 58-66 immunoglobulin kappa variable 2D-29 Homo sapiens 213-216 20021407-5 2009 Six antagonists, Bromocriptine, Cabergoline, Etilevodopa, Lysuride, Melevodopa and Pramipexole, were found more potent for binding and the active amino acids residues were identified (http://www.rcsb.org/pdb/) in A2A receptor. levodopa methyl ester 68-78 immunoglobulin kappa variable 2D-29 Homo sapiens 213-216 19140664-0 2009 N-[6-amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A receptor antagonists with improved drug like properties and in vivo efficacy. n-[6-amino-2-(heteroaryl)pyrimidin-4-yl]acetamides 0-50 immunoglobulin kappa variable 2D-29 Homo sapiens 54-57 19140664-1 2009 In the present article, we report on a strategy to improve the physical properties of a series of small molecule human adenosine 2A (hA2A) antagonists. Adenosine 119-128 immunoglobulin kappa variable 2D-29 Homo sapiens 133-137 19066414-1 2008 In the present study, the involvement of the selective adenosine A1 (CPA) and A2A (CGS 21680) and non-selective adenosine A1/A2A (NECA) receptor agonists on the development of hypersensitivity to acute morphine injection given during opiate withdrawal was investigated. Morphine 202-210 immunoglobulin kappa variable 2D-29 Homo sapiens 98-128 18758473-1 2008 Adenosine is a key endogenous molecule that regulates tissue function by activating four G-protein-coupled adenosine receptors: A1, A2A, A2B and A3. Adenosine 0-9 immunoglobulin kappa variable 2D-29 Homo sapiens 132-135 18249548-1 2008 A collection of 25 2-(2"-furyl)-1,2,4-triazolo[1,5-a]quinoxalines incorporating different substitution patterns at position 4 have been synthesized and their binding affinity towards human adenosine receptors (hA(1), hA(2A), hA(2B) and hA(3)) was determined. 2-(2"-furyl)-1,2,4-triazolo[1,5-a]quinoxalines 19-65 immunoglobulin kappa variable 2D-29 Homo sapiens 217-222 19356442-0 2008 Effects of age, gender, obesity, and diabetes on the efficacy and safety of the selective A2A agonist regadenoson versus adenosine in myocardial perfusion imaging integrated ADVANCE-MPI trial results. regadenoson 102-113 immunoglobulin kappa variable 2D-29 Homo sapiens 90-93 18226909-1 2008 A large series of piperazin-, piperidin- and tetrahydroisoquinolinamides of 4-(1,3-dialkyl-9-deazaxanthin-8-yl)phenoxyacetic acid were prepared through conventional or multiple parallel syntheses and evaluated for their binding affinity at the recombinant human adenosine receptors, chiefly at the hA(2B) and hA(2A) receptor subtypes. piperazin-, piperidin- and tetrahydroisoquinolinamides 18-72 immunoglobulin kappa variable 2D-29 Homo sapiens 309-315 18226909-4 2008 A number of selected ligands tested in functional assays in vitro showed very interesting antagonist activities and efficacies at both A(2A) and A(2B) receptor subtypes, with pA(2) values close to the corresponding pK(i)s. Structure-affinity and structure-selectivity relationships suggested that the binding potency at the hA(2B) receptor may be increased by lipophilic substituents at the N4-position of piperazinamides and that an ortho-methoxy substituent at the 8-phenyl ring and alkyl groups at N1 larger than the ones at N3, in the 9-deazaxanthine ring, may strongly enhance the hA(2A)/hA(2B) SI. piperazinamides 406-421 immunoglobulin kappa variable 2D-29 Homo sapiens 135-140 18226909-4 2008 A number of selected ligands tested in functional assays in vitro showed very interesting antagonist activities and efficacies at both A(2A) and A(2B) receptor subtypes, with pA(2) values close to the corresponding pK(i)s. Structure-affinity and structure-selectivity relationships suggested that the binding potency at the hA(2B) receptor may be increased by lipophilic substituents at the N4-position of piperazinamides and that an ortho-methoxy substituent at the 8-phenyl ring and alkyl groups at N1 larger than the ones at N3, in the 9-deazaxanthine ring, may strongly enhance the hA(2A)/hA(2B) SI. 9-deazaxanthine 539-554 immunoglobulin kappa variable 2D-29 Homo sapiens 135-140 18215030-7 2008 Finally, 3D-QSAR and LBHM strategies have been utilized to predict the binding affinity of five new human A2A pyrazolo-triazolo-pyrimidine antagonists finding a good agreement between the theoretical and the experimental predictions. Pyrazolotriazolopyrimidine 110-138 immunoglobulin kappa variable 2D-29 Homo sapiens 106-109 16765381-2 2006 Dual probe microdialysis was used to study A2A/D2 receptor interactions in the striato-pallidal GABA pathway in a model of Parkinson"s Disease. gamma-Aminobutyric Acid 96-100 immunoglobulin kappa variable 2D-29 Homo sapiens 43-49 18307293-2 2008 Previously we have described a series of novel A 2A receptor antagonists with excellent water solubility. Water 88-93 immunoglobulin kappa variable 2D-29 Homo sapiens 47-51 17310264-7 2007 SCH58261 was the most potent antagonist of the human A2A with a K(i) value of 4 nM, whereas Biogen-34 was the most potent antagonist of the rat A2A with a K(i) value of 1.2 nM. 5-amino-7-(2-phenylethyl)-2-(2-furyl)pyrazolo(4,3-e)-1,2,4-triazolo(1,5-c)pyrimidine 0-8 immunoglobulin kappa variable 2D-29 Homo sapiens 53-56 16765381-8 2006 L-dopa induced dyskinesias could be caused by changes in the balance of A2A/D2 heteromers vs A2A homomers expressed at the surface membrane, where A2A homomers dominate with abnormal increases in A2A signaling. Levodopa 0-6 immunoglobulin kappa variable 2D-29 Homo sapiens 72-78 15149696-3 2004 Based on the analysis of H-bond donor/acceptor capabilities of the isomeric triazolopyridine pairs it can be concluded that the H-bond donor strength of the free amino functionality is the main determinant for hA2a inhibitory activity and hA1 selectivity. CP-808844 76-92 immunoglobulin kappa variable 2D-29 Homo sapiens 210-214 16867213-1 2006 Antagonism of the A2A adenosine function has proved beneficial in the treatment of Parkinson"s disease, in that it increases L-dopa therapeutical effects without concomitant worsening of its side-effects. Adenosine 22-31 immunoglobulin kappa variable 2D-29 Homo sapiens 18-21 16867213-1 2006 Antagonism of the A2A adenosine function has proved beneficial in the treatment of Parkinson"s disease, in that it increases L-dopa therapeutical effects without concomitant worsening of its side-effects. Levodopa 125-131 immunoglobulin kappa variable 2D-29 Homo sapiens 18-21 16867213-2 2006 In this paper we describe a preferential A2A adenosine antagonist, ST 1535, with long-lasting pharmacodynamic effects. Adenosine 45-54 immunoglobulin kappa variable 2D-29 Homo sapiens 41-44 16867213-3 2006 It competitively antagonizes the effects of the A2A adenosine agonist NECA on cAMP in cells cloned with the human A2A adenosine receptor (IC50=353+/-30 nM), and the effects of the A1 adenosine agonist CHA on cAMP in cells cloned with the human A1 adenosine receptor (IC50=510+/-38 nM). Cyclic AMP 78-82 immunoglobulin kappa variable 2D-29 Homo sapiens 48-51 16867213-3 2006 It competitively antagonizes the effects of the A2A adenosine agonist NECA on cAMP in cells cloned with the human A2A adenosine receptor (IC50=353+/-30 nM), and the effects of the A1 adenosine agonist CHA on cAMP in cells cloned with the human A1 adenosine receptor (IC50=510+/-38 nM). Cyclic AMP 78-82 immunoglobulin kappa variable 2D-29 Homo sapiens 114-117 16867213-3 2006 It competitively antagonizes the effects of the A2A adenosine agonist NECA on cAMP in cells cloned with the human A2A adenosine receptor (IC50=353+/-30 nM), and the effects of the A1 adenosine agonist CHA on cAMP in cells cloned with the human A1 adenosine receptor (IC50=510+/-38 nM). Adenosine 52-61 immunoglobulin kappa variable 2D-29 Homo sapiens 48-51 16867213-4 2006 ST 1535, at oral doses of 5 and 10 mg/kg, antagonizes catalepsy induced by intracerebroventricular administration of the A2A adenosine agonist CGS 21680 (10 microg/5 microl) in mice. Adenosine 125-134 immunoglobulin kappa variable 2D-29 Homo sapiens 121-124 16867213-4 2006 ST 1535, at oral doses of 5 and 10 mg/kg, antagonizes catalepsy induced by intracerebroventricular administration of the A2A adenosine agonist CGS 21680 (10 microg/5 microl) in mice. cysteinylglycine 143-146 immunoglobulin kappa variable 2D-29 Homo sapiens 121-124 16501051-6 2006 The inhibitory effects of CGS-21680 and histamine on PAF biosynthesis were prevented by the protein kinase A inhibitor H-89, supporting roles for the Gs -coupled receptors A2A and H2, respectively, and cyclic adenosine monophosphate in the inhibitory mechanism. 2-(4-(2-carboxyethyl)phenethylamino)-5'-N-ethylcarboxamidoadenosine 26-35 immunoglobulin kappa variable 2D-29 Homo sapiens 172-182 16501051-6 2006 The inhibitory effects of CGS-21680 and histamine on PAF biosynthesis were prevented by the protein kinase A inhibitor H-89, supporting roles for the Gs -coupled receptors A2A and H2, respectively, and cyclic adenosine monophosphate in the inhibitory mechanism. Histamine 40-49 immunoglobulin kappa variable 2D-29 Homo sapiens 172-182 16501051-6 2006 The inhibitory effects of CGS-21680 and histamine on PAF biosynthesis were prevented by the protein kinase A inhibitor H-89, supporting roles for the Gs -coupled receptors A2A and H2, respectively, and cyclic adenosine monophosphate in the inhibitory mechanism. Platelet Activating Factor 53-56 immunoglobulin kappa variable 2D-29 Homo sapiens 172-182 16501051-6 2006 The inhibitory effects of CGS-21680 and histamine on PAF biosynthesis were prevented by the protein kinase A inhibitor H-89, supporting roles for the Gs -coupled receptors A2A and H2, respectively, and cyclic adenosine monophosphate in the inhibitory mechanism. N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide 119-123 immunoglobulin kappa variable 2D-29 Homo sapiens 172-182 16353217-6 2006 In particular, discrepancies in mutational divergence between the Inuit populations and their putative source mtDNA pool in Siberia/Alaska for the two predominant haplotype clusters, A2a and A2b, are more consistent with the possibility that expanding Thule groups encountered and interbred with existing Dorset populations in Canada and Greenland. thule 252-257 immunoglobulin kappa variable 2D-29 Homo sapiens 183-186 15294291-2 2004 The A2a-GFP protein was able to bind adenosine analogs indicating that the GFP tag did not alter the ligand binding activity of the receptor. Adenosine 37-46 immunoglobulin kappa variable 2D-29 Homo sapiens 4-7 14663020-0 2003 Progress in pursuit of therapeutic A2A antagonists: the adenosine A2A receptor selective antagonist KW6002: research and development toward a novel nondopaminergic therapy for Parkinson"s disease. istradefylline 100-106 immunoglobulin kappa variable 2D-29 Homo sapiens 35-38 11592813-6 2001 The receptors that transduce adenosine action include A1, A2a, A2b, and A3 adenosine receptors. Adenosine 29-38 immunoglobulin kappa variable 2D-29 Homo sapiens 58-61 12671949-1 2003 Piribedil is a non-ergot D2/D3 agonist with a significant antagonist action on alpha2A and alpha2C adrenergic receptor subtypes. Piribedil 0-9 immunoglobulin kappa variable 2D-29 Homo sapiens 79-86 11739107-3 2002 The A(2A) adenosine receptor (A(2A)-AR) is a member of the family of guanine nucleotide binding proteins and has become a focus of major interest primarily because of its ability to broadly inactivate the inflammatory cascade. Guanine Nucleotides 69-87 immunoglobulin kappa variable 2D-29 Homo sapiens 30-38 11906291-4 2002 1,8-disubstituted xanthine derivatives were equipotent to or more potent than 1,3,8-trisubstituted xanthines at A2B ARs, but generally less potent at A1 and A2A, and much less potent at A3 ARs. 1,8-disubstituted xanthine 0-26 immunoglobulin kappa variable 2D-29 Homo sapiens 157-160 11906291-10 2002 1-Butyl-8-p-carboxyphenylxanthine (10), another polar analogue bearing a carboxylate function, exhibited a K(i) value of 24 nM for A2B ARs, 49-fold selectivity versus human and 20-fold selectivity versus rat A1 ARs, and greater than 150-fold selectivity versus human A2A and A3 ARs. 1-butyl-8-p-carboxyphenylxanthine 0-33 immunoglobulin kappa variable 2D-29 Homo sapiens 267-270 11296702-1 2001 On the basis of earlier suggested unitary mechanism of synaptic plasticity opposite effects of adenosine and dopamine on the cAMP concentration in striatal spinal cells can emphasize the well known antagonistic interactions between A2A and D2 receptors on striatopallidal cells and between A1 and D1 receptors on striatonigral cells. Adenosine 95-104 immunoglobulin kappa variable 2D-29 Homo sapiens 232-242 11296702-1 2001 On the basis of earlier suggested unitary mechanism of synaptic plasticity opposite effects of adenosine and dopamine on the cAMP concentration in striatal spinal cells can emphasize the well known antagonistic interactions between A2A and D2 receptors on striatopallidal cells and between A1 and D1 receptors on striatonigral cells. Dopamine 109-117 immunoglobulin kappa variable 2D-29 Homo sapiens 232-242 11296702-1 2001 On the basis of earlier suggested unitary mechanism of synaptic plasticity opposite effects of adenosine and dopamine on the cAMP concentration in striatal spinal cells can emphasize the well known antagonistic interactions between A2A and D2 receptors on striatopallidal cells and between A1 and D1 receptors on striatonigral cells. Cyclic AMP 125-129 immunoglobulin kappa variable 2D-29 Homo sapiens 232-242 8750371-4 1995 Plasma antifactor IIa (aIIa) activity levels after the 30- and 60-U/kg doses of ardeparin were too low to reliably characterize the disposition of the drug. ardeparin 80-89 immunoglobulin kappa variable 2D-29 Homo sapiens 23-27 9914161-2 1999 Many of the adenosine actions seem to be mediated by specific surface receptors positively coupled to adenylate cyclase: A2A and A2B. Adenosine 12-21 immunoglobulin kappa variable 2D-29 Homo sapiens 121-132 9756374-8 1998 Small but statistically significant inhibitions of the adenosine-(50 microM)-stimulated increase in chloride efflux were elicited by the A1 receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine (CPX, 100 nM) and the A2 receptor antagonist 3,7-dimethyl-1-propylargylxanthine (DMPX, 10 microM). Adenosine 55-64 immunoglobulin kappa variable 2D-29 Homo sapiens 217-219 9756374-8 1998 Small but statistically significant inhibitions of the adenosine-(50 microM)-stimulated increase in chloride efflux were elicited by the A1 receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine (CPX, 100 nM) and the A2 receptor antagonist 3,7-dimethyl-1-propylargylxanthine (DMPX, 10 microM). Chlorides 100-108 immunoglobulin kappa variable 2D-29 Homo sapiens 217-219 9756374-8 1998 Small but statistically significant inhibitions of the adenosine-(50 microM)-stimulated increase in chloride efflux were elicited by the A1 receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine (CPX, 100 nM) and the A2 receptor antagonist 3,7-dimethyl-1-propylargylxanthine (DMPX, 10 microM). 1,3-dipropyl-8-cyclopentylxanthine 196-199 immunoglobulin kappa variable 2D-29 Homo sapiens 217-219 9453355-7 1998 Both KF17837 (selective A2 antagonist) and DPSPX (A1/A2 antagonist), but not DPCPX (selective A1 antagonist), blocked the antimitogenic effects of 2-chloroadenosine, EHNA, and dipyridamole on DNA and collagen synthesis, suggesting the involvement of A2A and/or A2B, but excluding the participation of A1, receptors. KF 17837 5-12 immunoglobulin kappa variable 2D-29 Homo sapiens 250-253 9453355-7 1998 Both KF17837 (selective A2 antagonist) and DPSPX (A1/A2 antagonist), but not DPCPX (selective A1 antagonist), blocked the antimitogenic effects of 2-chloroadenosine, EHNA, and dipyridamole on DNA and collagen synthesis, suggesting the involvement of A2A and/or A2B, but excluding the participation of A1, receptors. 1,3-dipropyl-8-(4-sulfophenyl)xanthine 43-48 immunoglobulin kappa variable 2D-29 Homo sapiens 250-253 10714510-1 2000 A series of N6,2-disubstituted adenosine analogues have been synthesized and their functional activity measured against A2a and A1 receptors. n6,2-disubstituted adenosine 12-40 immunoglobulin kappa variable 2D-29 Homo sapiens 120-123 1851342-1 1991 In six healthy volunteers we have estimated the pharmacokinetic parameters of the anti factor Xa (AXa) and anti factor IIa (AIIa) activities of a LMW heparin, Logiparin. Heparin, Low-Molecular-Weight 146-157 immunoglobulin kappa variable 2D-29 Homo sapiens 124-128 7739005-0 1995 2-Aralkynyl and 2-heteroalkynyl derivatives of adenosine-5"-N-ethyluronamide as selective A2a adenosine receptor agonists. 2-aralkynyl 0-11 immunoglobulin kappa variable 2D-29 Homo sapiens 90-93 7739005-0 1995 2-Aralkynyl and 2-heteroalkynyl derivatives of adenosine-5"-N-ethyluronamide as selective A2a adenosine receptor agonists. 2-heteroalkynyl 16-31 immunoglobulin kappa variable 2D-29 Homo sapiens 90-93 7739005-0 1995 2-Aralkynyl and 2-heteroalkynyl derivatives of adenosine-5"-N-ethyluronamide as selective A2a adenosine receptor agonists. Adenosine-5'-(N-ethylcarboxamide) 47-76 immunoglobulin kappa variable 2D-29 Homo sapiens 90-93 7739005-8 1995 From these data and those previously reported, the structure-activity relationships derived for the 2-alkynyl-substituted ribose uronamides would indicate that potentiation of A2a receptor affinity could be obtained by aromatic rings not conjugated with the triple bond or by heteroaromatic groups. 2-alkynyl-substituted ribose uronamides 100-139 immunoglobulin kappa variable 2D-29 Homo sapiens 176-179 7731018-1 1995 Synthesis and A1 and A2a adenosine binding activities of some 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c] pyrazol-4-ones, 1-aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]quinolin-4- ones, and 1-aryl-1H-imidazo[4,5-b]quinoxalines. Adenosine 25-34 immunoglobulin kappa variable 2D-29 Homo sapiens 21-24 7731018-1 1995 Synthesis and A1 and A2a adenosine binding activities of some 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c] pyrazol-4-ones, 1-aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]quinolin-4- ones, and 1-aryl-1H-imidazo[4,5-b]quinoxalines. 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c] pyrazol-4-ones 62-125 immunoglobulin kappa variable 2D-29 Homo sapiens 21-24 7731018-1 1995 Synthesis and A1 and A2a adenosine binding activities of some 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c] pyrazol-4-ones, 1-aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]quinolin-4- ones, and 1-aryl-1H-imidazo[4,5-b]quinoxalines. 1-aryl-4,9-dihydro-3-methyl-1h-pyrazolo[3,4-b]quinolin-4- ones 127-189 immunoglobulin kappa variable 2D-29 Homo sapiens 21-24 7731018-2 1995 The syntheses and A1 and A2a adenosine binding activities of some new 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c]pyrazol-4-ones, 1-aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]-quinolin-4-ones, and 1-aryl-1H-imidazo[4,5-b]quinoxalines are reported. Adenosine 29-38 immunoglobulin kappa variable 2D-29 Homo sapiens 25-28 7731018-2 1995 The syntheses and A1 and A2a adenosine binding activities of some new 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c]pyrazol-4-ones, 1-aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]-quinolin-4-ones, and 1-aryl-1H-imidazo[4,5-b]quinoxalines are reported. 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c]pyrazol-4-ones 70-132 immunoglobulin kappa variable 2D-29 Homo sapiens 25-28 7731018-2 1995 The syntheses and A1 and A2a adenosine binding activities of some new 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c]pyrazol-4-ones, 1-aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]-quinolin-4-ones, and 1-aryl-1H-imidazo[4,5-b]quinoxalines are reported. 1-aryl-4,9-dihydro-3-methyl-1h-pyrazolo[3,4-b]-quinolin-4-ones 134-196 immunoglobulin kappa variable 2D-29 Homo sapiens 25-28 7731018-2 1995 The syntheses and A1 and A2a adenosine binding activities of some new 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c]pyrazol-4-ones, 1-aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]-quinolin-4-ones, and 1-aryl-1H-imidazo[4,5-b]quinoxalines are reported. 1-aryl-1h-imidazo[4,5-b]quinoxalines 202-238 immunoglobulin kappa variable 2D-29 Homo sapiens 25-28 1851342-1 1991 In six healthy volunteers we have estimated the pharmacokinetic parameters of the anti factor Xa (AXa) and anti factor IIa (AIIa) activities of a LMW heparin, Logiparin. Logiparin 159-168 immunoglobulin kappa variable 2D-29 Homo sapiens 124-128 34319736-6 2021 For the first time, falcarinol (1a) and its analogue (R)-2i were found to have potential L-type calcium channel-blocking activity, as recorded using a manual patch clamp technique on HEK-293 cells stably expressing hCav1.2 (alpha1C/beta2a/alpha2delta1). falcarinol 20-30 immunoglobulin kappa variable 2D-29 Homo sapiens 232-251 33235193-1 2020 Adenosine, its interacting A1 and A2A receptors, and particularly the variant rs5751876 in the A2A gene ADORA2A have been shown to modulate anxiety, arousal, and sleep. Adenosine 0-9 immunoglobulin kappa variable 2D-29 Homo sapiens 95-98 15104468-0 2004 Efficient synthesis of an adenosine A2a agonist: glycosylation of 2-haloadenines and an N2-alkyl-6-chloroguanine. 2-haloadenines 66-80 immunoglobulin kappa variable 2D-29 Homo sapiens 36-39 15104468-0 2004 Efficient synthesis of an adenosine A2a agonist: glycosylation of 2-haloadenines and an N2-alkyl-6-chloroguanine. n2-alkyl-6-chloroguanine 88-112 immunoglobulin kappa variable 2D-29 Homo sapiens 36-39 15104468-1 2004 A convergent synthesis of adenosine A2a agonist 1 in the form of its maleate salt 2 was achieved. maleate salt 69-81 immunoglobulin kappa variable 2D-29 Homo sapiens 36-39 24687255-3 2014 Among new classes of drugs, adenosine A2A antagonists have emerged as promising candidates. Adenosine 28-37 immunoglobulin kappa variable 2D-29 Homo sapiens 38-41 24687255-5 2014 To date, the clinical research regarding A2A antagonists and their potential utilization in PD therapy continues to evolve between drugs just or previously discontinued (preladenant and vipadenant), new derivatives in development (tozadenant, PBF-509, ST1535, ST4206 and V81444) and the relatively old drug istradefylline, which has finally been licensed as an anti-parkinsonian drug in Japan. istradefylline 307-321 immunoglobulin kappa variable 2D-29 Homo sapiens 41-44 24687255-7 2014 Moreover, results from phase II and III trials also demonstrate that A2A antagonists are effective in reducing off-time, without worsening troublesome dyskinesia, and in increasing on-time with a mild increase of non-troublesome dyskinesia, in patients at an advanced stage of PD treated with L-DOPA. Levodopa 293-299 immunoglobulin kappa variable 2D-29 Homo sapiens 69-72 35224877-6 2022 BRL44408 was the most alpha2A-selective antagonist, although its alpha1A-affinity (81 nM) is only 9-fold greater than its alpha2C-affinity. BRL 44408 0-8 immunoglobulin kappa variable 2D-29 Homo sapiens 22-29 35569686-0 2022 2,3-Dihydrobenzo-dioxine piperidine derivatives as potent and selective alpha2c antagonists. 2,3-dihydrobenzo-dioxine piperidine 0-35 immunoglobulin kappa variable 2D-29 Homo sapiens 72-79 35569686-1 2022 In this manuscript, we report a series of benzodioxine methyl piperidine derivatives as highly potent and selective alpha2C antagonists by ligand design to improve the pharmacokinetics of a previous candidate molecule. benzodioxine 42-54 immunoglobulin kappa variable 2D-29 Homo sapiens 116-123 35569686-1 2022 In this manuscript, we report a series of benzodioxine methyl piperidine derivatives as highly potent and selective alpha2C antagonists by ligand design to improve the pharmacokinetics of a previous candidate molecule. methyl piperidine 55-72 immunoglobulin kappa variable 2D-29 Homo sapiens 116-123 35199177-8 2022 Chlormethine gel was given as monotherapy in 12 patients (52.17%), and in addition to systemic treatments (methotrexate and peginterferon alpha-2a) in 11 patients (47.82%). Mechlorethamine 0-12 immunoglobulin kappa variable 2D-29 Homo sapiens 138-146 35224877-7 2022 MK-912 is the highest-affinity, most alpha2C-selective antagonist (0.15 nM alpha2C-affinity) although its alpha2C-selectivity is only 13-fold greater than at alpha2A. L 657743 0-6 immunoglobulin kappa variable 2D-29 Homo sapiens 37-44 35224877-7 2022 MK-912 is the highest-affinity, most alpha2C-selective antagonist (0.15 nM alpha2C-affinity) although its alpha2C-selectivity is only 13-fold greater than at alpha2A. L 657743 0-6 immunoglobulin kappa variable 2D-29 Homo sapiens 75-82 35224877-7 2022 MK-912 is the highest-affinity, most alpha2C-selective antagonist (0.15 nM alpha2C-affinity) although its alpha2C-selectivity is only 13-fold greater than at alpha2A. L 657743 0-6 immunoglobulin kappa variable 2D-29 Homo sapiens 106-113 35464557-2 2022 On the other hand, dexmedetomidine is highly selective and has a greater affinity toward alpha2 adrenergic receptors, especially toward its alpha2a subtype, accountable for more analgesic and hypnotic effects than clonidine. Dexmedetomidine 19-34 immunoglobulin kappa variable 2D-29 Homo sapiens 140-147 2847169-5 1988 When 2-(2-methoxyethoxy)ethyl 8-(cis-2-n-octylcyclopropyl)octanoate (A2C) was added to each fraction, Na+,K+-ATPase, but not glucagon-stimulated adenylate cyclase activity, was activated in the apical fraction. 2-(2-methoxyethoxy)ethyl 8-(cis-2-n-octylcyclopropyl)octanoate 5-67 immunoglobulin kappa variable 2D-29 Homo sapiens 69-72 35224877-4 2022 Here, 3 H-rauwolscine whole cell binding was used to determine the affinity and selectivity of 99 alpha-antagonists (including antidepressants and antipsychotics) in CHO cells expressing human alpha2A, alpha2B, or alpha2C-adrenoceptors, using an identical method to beta and alpha1-adrenoceptor measurements, thus allowing direct human receptor comparisons. h-rauwolscine 8-21 immunoglobulin kappa variable 2D-29 Homo sapiens 193-200 35224877-4 2022 Here, 3 H-rauwolscine whole cell binding was used to determine the affinity and selectivity of 99 alpha-antagonists (including antidepressants and antipsychotics) in CHO cells expressing human alpha2A, alpha2B, or alpha2C-adrenoceptors, using an identical method to beta and alpha1-adrenoceptor measurements, thus allowing direct human receptor comparisons. h-rauwolscine 8-21 immunoglobulin kappa variable 2D-29 Homo sapiens 214-221 1005114-1 1976 Under the conditions that RNA ligase converts the tetranucleotide, pA-A2-A, to larger polynucleotides, no such polymerization can be detected with the derivative, pA-A2-A(MeOEt), that possesses a terminal 2"-0-(alpha-methoxyethyl) group. tetranucleotide 50-65 immunoglobulin kappa variable 2D-29 Homo sapiens 70-74 1005114-1 1976 Under the conditions that RNA ligase converts the tetranucleotide, pA-A2-A, to larger polynucleotides, no such polymerization can be detected with the derivative, pA-A2-A(MeOEt), that possesses a terminal 2"-0-(alpha-methoxyethyl) group. Polynucleotides 86-101 immunoglobulin kappa variable 2D-29 Homo sapiens 70-74 1005114-3 1976 Thus, the enzyme, together with ATP, converts equimolar quantities of A-A2-A and pA-A2-A(MeOEt) to A-A6-A(MeOEt) in 55% yield, while a similar reaction with A-A2-A and pU-U2-U(MeOEt) results in a 40% yield of A-A3-U3-U(MeOEt). Adenosine Triphosphate 32-35 immunoglobulin kappa variable 2D-29 Homo sapiens 72-76 1005114-3 1976 Thus, the enzyme, together with ATP, converts equimolar quantities of A-A2-A and pA-A2-A(MeOEt) to A-A6-A(MeOEt) in 55% yield, while a similar reaction with A-A2-A and pU-U2-U(MeOEt) results in a 40% yield of A-A3-U3-U(MeOEt). Adenosine Triphosphate 32-35 immunoglobulin kappa variable 2D-29 Homo sapiens 84-88 1005114-3 1976 Thus, the enzyme, together with ATP, converts equimolar quantities of A-A2-A and pA-A2-A(MeOEt) to A-A6-A(MeOEt) in 55% yield, while a similar reaction with A-A2-A and pU-U2-U(MeOEt) results in a 40% yield of A-A3-U3-U(MeOEt). Adenosine Triphosphate 32-35 immunoglobulin kappa variable 2D-29 Homo sapiens 84-88 1005114-9 1976 The terminal 3"-phosphate group serves equally well as a blocking group for specific ligation reactions in that the ligase converts equimolar amounts of A-A2-A and pA-A2-Ap to A-A6-Ap in 50% yield. 3"-phosphate 13-25 immunoglobulin kappa variable 2D-29 Homo sapiens 155-159 1005114-9 1976 The terminal 3"-phosphate group serves equally well as a blocking group for specific ligation reactions in that the ligase converts equimolar amounts of A-A2-A and pA-A2-Ap to A-A6-Ap in 50% yield. 3"-phosphate 13-25 immunoglobulin kappa variable 2D-29 Homo sapiens 167-172 1005114-9 1976 The terminal 3"-phosphate group serves equally well as a blocking group for specific ligation reactions in that the ligase converts equimolar amounts of A-A2-A and pA-A2-Ap to A-A6-Ap in 50% yield. a-a6-ap 176-183 immunoglobulin kappa variable 2D-29 Homo sapiens 155-159 1005114-9 1976 The terminal 3"-phosphate group serves equally well as a blocking group for specific ligation reactions in that the ligase converts equimolar amounts of A-A2-A and pA-A2-Ap to A-A6-Ap in 50% yield. a-a6-ap 176-183 immunoglobulin kappa variable 2D-29 Homo sapiens 167-172 33834710-8 2021 Brexpiprazole is a highly affine (potent) alpha2C antagonist and, therefore, also an indirect 5-HT1A agonist. brexpiprazole 0-13 immunoglobulin kappa variable 2D-29 Homo sapiens 42-49 32837981-6 2020 Further analysis demonstrated that the variation of the S protein at site 614 (QHD43416.1: p.614D>G) was a characteristic of stains in Clades A2 and A2a. qhd43416 79-87 immunoglobulin kappa variable 2D-29 Homo sapiens 149-152 32722122-3 2020 Herein, we report on the synthesis and biological evaluation of a new set of piperazine- and piperidine- containing 7-amino-2-(furan-2-yl)thiazolo[5,4-d]pyrimidine derivatives designed as human A2A AR antagonists/inverse agonists. Piperazine 77-87 immunoglobulin kappa variable 2D-29 Homo sapiens 194-197 32722122-3 2020 Herein, we report on the synthesis and biological evaluation of a new set of piperazine- and piperidine- containing 7-amino-2-(furan-2-yl)thiazolo[5,4-d]pyrimidine derivatives designed as human A2A AR antagonists/inverse agonists. piperidine 93-103 immunoglobulin kappa variable 2D-29 Homo sapiens 194-197 32722122-3 2020 Herein, we report on the synthesis and biological evaluation of a new set of piperazine- and piperidine- containing 7-amino-2-(furan-2-yl)thiazolo[5,4-d]pyrimidine derivatives designed as human A2A AR antagonists/inverse agonists. 7-amino-2-(furan-2-yl)thiazolo[5,4-d]pyrimidine 116-163 immunoglobulin kappa variable 2D-29 Homo sapiens 194-197 32722122-5 2020 Amongst them, the 2-(furan-2-yl)-N5-(2-(4-phenylpiperazin-1-yl)ethyl)thiazolo[5,4-d]pyrimidine-5,7-diamine 11 exhibited the highest A2A AR binding affinity (Ki = 8.62 nM) as well as inverse agonist potency (IC50 = 7.42 nM). 2-(furan-2-yl)-n5-(2-(4-phenylpiperazin-1-yl)ethyl)thiazolo[5,4-d]pyrimidine-5,7-diamine 18-106 immunoglobulin kappa variable 2D-29 Homo sapiens 132-135 32764876-5 2020 Despite its approval, the clinical use of danoprevir is currently limited to its combination with peginterferon alpha-2a and ribavirin, thereby driving its development towards interferon-free, ribavirin-free regimens with improved tolerability and adherence. danoprevir 42-52 immunoglobulin kappa variable 2D-29 Homo sapiens 112-120 32015389-6 2020 DARC identifies, as functionally-congruent features linking allosterically the ATP, DNA, and clamp binding sites: residues distinctive of gamma and of gamma/delta" that mutually interact in trans, centered on the catalytic base; several gamma/delta"-residues and six gamma/delta"-covariant residue pairs within the DNA binding N-termini of helices alpha2 and alpha3; and gamma/delta"-residues associated with the alpha2 C-terminus and the clamp-binding loop. Adenosine Triphosphate 79-82 immunoglobulin kappa variable 2D-29 Homo sapiens 413-421 32764876-3 2020 Adverse events such as anemia, fatigue, fever, and headache were associated with the inclusion of peginterferon alpha-2a and ribavirin in the danoprevir-based regimen. danoprevir 142-152 immunoglobulin kappa variable 2D-29 Homo sapiens 112-120 32256718-2 2020 Dexmedetomidine is clinically effective by acting on alpha2 adrenergic receptor and the impact of the adrenoceptor alpha2A gene (ADRA2A) polymorphisms on the anesthetic and analgesic effects of dexmedetomidine is related to the clinical application of dexmedetomidine. Dexmedetomidine 194-209 immunoglobulin kappa variable 2D-29 Homo sapiens 115-122 31689542-2 2020 The aim of this study was to evaluate the effect of the de novo combination therapy including pegylated-interferon alpha-2a (PEG-IFNalpha-2a) and entecavir (ETV) in this high risk population. Polyethylene Glycols 125-128 immunoglobulin kappa variable 2D-29 Homo sapiens 115-123 31578448-0 2019 Reconstruction of apo A2A receptor activation pathways reveal ligand-competent intermediates and state-dependent cholesterol hotspots. Cholesterol 113-124 immunoglobulin kappa variable 2D-29 Homo sapiens 22-25 31578448-6 2019 Here, we reconstruct the activation pathways of the apo adenosine receptor (A2A), starting from an inactive conformation, by applying adaptive sampling MD combined with a goal-oriented scoring function. Adenosine 56-65 immunoglobulin kappa variable 2D-29 Homo sapiens 76-79 31578448-8 2019 Exploration of the apo conformational landscape of A2A reveals the existence of ligand-competent states, active intermediates and state-dependent cholesterol hotspots of relevance for drug discovery. Cholesterol 146-157 immunoglobulin kappa variable 2D-29 Homo sapiens 51-54 31009638-2 2019 In this study, we examined the inhibitory effect of guanabenz, a centrally acting alpha2-adrenoceptor agonist with high specificity for alpha2A-subtype, on HCN channels in mesencephalic trigeminal nucleus (MTN) neurons which robustly express HCN channels and have been suggested to coexpress alpha2A-adrenoceptors. Guanabenz 52-61 immunoglobulin kappa variable 2D-29 Homo sapiens 136-143 30913470-2 2019 In this work, an enlarged series of 1,2,4-triazolo[4,3-a]pyrazin-3-ones was designed to target the human (h) A2A adenosine receptor (AR) or both hA1 and hA2A ARs. 1,2,4-triazolo[4,3-a]pyrazin-3-ones 36-71 immunoglobulin kappa variable 2D-29 Homo sapiens 109-112 30913470-2 2019 In this work, an enlarged series of 1,2,4-triazolo[4,3-a]pyrazin-3-ones was designed to target the human (h) A2A adenosine receptor (AR) or both hA1 and hA2A ARs. 1,2,4-triazolo[4,3-a]pyrazin-3-ones 36-71 immunoglobulin kappa variable 2D-29 Homo sapiens 153-157 30657666-3 2019 Here, we report the development, chemical synthesis, and biological screening of a compound library that led to the identification of the beta2c- and beta2i-selective compounds LU-002c (4; IC50 beta2c: 8 nM, IC50 beta2i/beta2c: 40-fold) and LU-002i (5; IC50 beta2i: 220 nM, IC50 beta2c/beta2i: 45-fold), respectively. lu-002c 177-184 immunoglobulin kappa variable 2D-29 Homo sapiens 138-144 30657666-3 2019 Here, we report the development, chemical synthesis, and biological screening of a compound library that led to the identification of the beta2c- and beta2i-selective compounds LU-002c (4; IC50 beta2c: 8 nM, IC50 beta2i/beta2c: 40-fold) and LU-002i (5; IC50 beta2i: 220 nM, IC50 beta2c/beta2i: 45-fold), respectively. lu-002c 177-184 immunoglobulin kappa variable 2D-29 Homo sapiens 194-200 30657666-3 2019 Here, we report the development, chemical synthesis, and biological screening of a compound library that led to the identification of the beta2c- and beta2i-selective compounds LU-002c (4; IC50 beta2c: 8 nM, IC50 beta2i/beta2c: 40-fold) and LU-002i (5; IC50 beta2i: 220 nM, IC50 beta2c/beta2i: 45-fold), respectively. lu-002c 177-184 immunoglobulin kappa variable 2D-29 Homo sapiens 194-200 30657666-3 2019 Here, we report the development, chemical synthesis, and biological screening of a compound library that led to the identification of the beta2c- and beta2i-selective compounds LU-002c (4; IC50 beta2c: 8 nM, IC50 beta2i/beta2c: 40-fold) and LU-002i (5; IC50 beta2i: 220 nM, IC50 beta2c/beta2i: 45-fold), respectively. lu-002i 241-248 immunoglobulin kappa variable 2D-29 Homo sapiens 138-144 30198788-4 2019 MATERIAL AND METHODS: The human Muller cell line MIO-M1 was treated with the alpha2A-ADR agonist brimonidine in combination with inhibitors for Src-kinase, EGFR-kinase, matrix metalloproteinase (MMP) as well as small interfering RNAs (siRNAs) for the EGFR. Brimonidine Tartrate 97-108 immunoglobulin kappa variable 2D-29 Homo sapiens 77-84 30198788-6 2019 RESULTS: Our results show that human MIO-M1 cells express alpha2A-ADRs and that stimulation of these receptors caused a robust increase of ERK1/2 and protein kinase B (PKB/AKT) (Thr-308) phosphorylation in MIO-M1 cells. Threonine 178-181 immunoglobulin kappa variable 2D-29 Homo sapiens 58-65 30380560-0 2019 Tetanic Facilitation of Neuromuscular Transmission by Adenosine A2A and Muscarinic M1 Receptors is Dependent on the Uptake of Choline via High-Affinity Transporters. Choline 126-133 immunoglobulin kappa variable 2D-29 Homo sapiens 64-95