D1 receptor 选择性抑制剂 | 激动剂 | 拮抗剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S4618 Fenoldopam mesylate

Fenoldopam是一种选择性的多巴胺受体(dopamine-1 receptor)激动剂,具有利尿特性。它可以通过小动脉的血管舒张降低血压。

Selective
S4151 Penfluridol

Penfluridol是一种高效的,第一代二苯丁哌啶类抗精神病药物。

Selective Dopamine receptor, Ki: 1.6 μM
S5949 Metoclopramide hydrochloride hydrate

Metoclopramide hydrochloride (Clorpa, Gimoti, Maxolon, Reglan) hydrate is primarily a Dopamine receptor antagonist, with 5HT3 receptor antagonist and 5HT4 receptor agonist activity, and used as an antiemetic and gastroprokinetic.

Selective
S5862 Metoclopramide

Metoclopramide is a dopamine antagonist used for the treatment of nausea and vomiting.

Selective
S2456 Chlorpromazine HCl

Chlorpromazine HCl是一种多巴胺和钾离子通道抑制剂,对内向整流钾电流和与时间无关的外向电流IC50分别为6.1和16 μM。

Selective
S2529 Dopamine HCl

Dopamine HCl 是一种广泛存在于各种动物的儿茶酚胺类神经递质,是多巴胺D1-5受体激动剂。

Selective
S1724 Paliperidone

Paliperidone,作为 Risperidone主要的活性代谢物,是一种高效的serotonin-2Adopamine-2 receptor 拮抗剂,用于治疗精神分裂症。

Selective
S1444 Ziprasidone HCl

Ziprasidone HCl 是一类有效的dopamineserotonin (5-HT) receptor的拮抗剂,用于精神分裂症以及双向性障碍的治疗。

Selective
S4257 Alizapride HCl

Alizapride在以外消旋混合物服用时,作为多巴胺拮抗剂促肠胃运动和止吐治疗癌症化疗引起的恶心和呕吐。

Selective
S4274 Rotigotine

Rotigotine是一种dopamine receptor的激动剂,用于帕金森氏症和不宁腿综合征的治疗。

Selective
S4219 Azaperone

Azaperone 是一种吡啶哌嗪和丁酰苯类抗精神病药,具有镇静和止吐的效果,主要是在兽医上用作镇静剂。它是Dopamine receptors的拮抗剂,能够透过血脑屏障,结合D1和D2受体。

Selective
S2451 Amantadine HCl

Amantadine HCl用于治疗或预防某些病毒引起的呼吸道感染。

Selective
S1280 Amisulpride

Amisulpride是一种非典型的抗精神病药物,用于治疗精神病的精神分裂症和双相情感障碍的躁狂发作。

Selective
S1726 Levodopa

Levodopa 是多巴胺,,肾上腺素以及去甲肾上腺素的前体,具有抗帕金森病的特性。

Selective
S6887 Clozapine N-oxide

Clozapine N-oxide (CNO) is a metabolite of Clozapine (GLXC-06516) and an agonist of human muscarinic designer receptors (Designer Receptors Exclusively Activated by Designer Drugs, DREADDs). Clozapine is a potent dopamine (DA) antagonist and a selective muscarinic M4 receptor agonist.

Selective
S1763 Quetiapine (ICI-204636) fumarate

Quetiapine Fumarate是一种非典型抗精神病药物,用于治疗精神分裂症,双相I型躁狂,双相II型抑郁症,双相I型抑郁症。对多种神经递质受体如serotonin, dopamine, histamineadrenergic receptors有亲和力。

Selective
S2452 Amfebutamone (Bupropion) HCl

Amfebutamone (Bupropion) HCl是一种选择性去甲肾上腺素-多巴胺再摄取的抑制剂,IC50分别为6.5和3.4μM。

Selective
S0476 SCH-23390 hydrochloride

SCH-23390 hydrochloride is a potent and selective antagonist of dopamine D1-like receptor with Ki of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist of human 5-HT2C receptor with Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.

Pan D1 dopamine receptor, Ki: 0.2 nM
S1771 Chlorprothixene

Chlorprothixene与多巴胺和组织胺受体(如D1, D2, D3, D5, H1, 5-HT2, 5-HT6和5-HT7)具有强结合力, Ki值分别为18nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM和5.6 nM。

Pan D1 receptor, Ki: 18 nM
S4086 Loxapine Succinate

Loxapine Succinate是D2DR和D4DR抑制剂,5-羟色胺受体拮抗剂,也是Dibenzoxazepine类的抗精神病试剂。

Pan D2 receptor (human), Ki: 24 nM; D2 receptor (Human), Ki: 24 nM; D1 receptor (human), Ki: 26 nM; D1 receptor (bovine), Ki: 62 nM
S2437 Rotundine

Rotundine是一种选择性多巴胺D1受体拮抗剂, IC50为166 nM。

Pan D1 receptor, IC50: 166 nM
S3913 Pimethixene maleate

Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.

Pan Dopamine D1 Receptor, pKi: 6.37
S4358 Pimozide

Pimozide is an antipsychotic drug of the diphenylbutylpiperidine class, which is a strong inhibitor of CYP2D6.

Pan Dopamine D1 receptor, Ki: 6600 nM
S7993 SKF38393 HCl

SKF38393 HCl是一种选择性dopamine D1/D5 receptor激动剂。

Pan