A2aR antagonists/MAO-B inhibitors(University of Parma)(A2aR antagonists/MAO-B inhibitors(University of Parma)) - 药物靶点：A2aR x MAO-B_在研适应症：帕金森病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

(E)-6-(4-chlorostyryl)-1,3,5,-trimethyl-1H-pyrrolo[3,2-d]pyrimidine-2,4-(3H,5H)-dione (17f)

靶点

A2aR x MAO-B

作用机制

A2aR拮抗剂(腺苷A2a受体拮抗剂)、MAO-B抑制剂(单胺氧化酶B抑制剂)

治疗领域

神经系统疾病内分泌与代谢疾病

在研适应症

帕金森病

非在研适应症-

原研机构

University of Parma

在研机构

University of Parma

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C17H16ClN3O2

InChIKeyCUWBKAWUQFYRQI-RMKNXTFCSA-N

CAS号1419403-68-1

关联

100 项与 A2aR antagonists/MAO-B inhibitors(University of Parma) 相关的临床结果

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100 项与 A2aR antagonists/MAO-B inhibitors(University of Parma) 相关的转化医学

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100 项与 A2aR antagonists/MAO-B inhibitors(University of Parma) 相关的专利（医药）

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1

项与 A2aR antagonists/MAO-B inhibitors(University of Parma) 相关的文献（医药）

2005-05-01·European Journal of Pharmacology3区 · 医学

Antidepressant-like effect of the selective 5-HT1B receptor agonist CP 94253: A possible mechanism of action

3区 · 医学

Article

作者: Lucyna Antkiewicz-Michaluk ; Katarzyna Stachowicz ; Ewa Chojnacka-Wójcik ; Ewa Tatarczyńska ; Aleksandra Kłodzińska

The mechanism of the antidepressant-like activity of the selective 5-hydroxytryptamine(1B) (5-HT(1B)) receptor agonist 5-propoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-pyrrolo[3,2-b]pyridine (CP 94253) was studied in the forced swimming test in mice. CP 94253 administered intraperitoneally at a single dose of 5 mg/kg potently shortened the immobility time of mice. The anti-immobility effect of CP 94253 was wholly blocked by the selective 5-HT(1B) receptor antagonist N-[3-(2-dimethylamino)ethoxy-4-methoxyphenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-(1,1'-biphenyl)-4-carboxamide (SB 216641, 5 mg/kg), the dopamine D2-like receptor antagonist sulpiride (50 mg/kg) and the alpha(2)-adrenoceptor antagonist idazoxan (2 mg/kg), but was not modified in animals with a lesion of the 5-HT system produced by p-chlorophenylalanine (p-CPA, 3 x 300 mg/kg). The obtained results suggest that the anti-immobility effect of CP 94253 is mediated by activation of 5-HT(1B) receptors-most probably located postsynaptically and/or as heteroreceptors, and that the dopamine and the noradrenaline systems are involved in this action.

100 项与 A2aR antagonists/MAO-B inhibitors(University of Parma) 相关的药物交易

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