D2 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
S4631 Prochlorperazine dimaleate salt

Prochlorperazine是抗精神病药物中属于吩噻嗪类的多巴胺受体D2拮抗剂。

Selective
S5714 lurasidone

Lurasidone (SM-13496) is a second-generation antipsychotic agent that exhibits full antagonism at dopamine D2 and serotonin 5-HT2A receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. It also has high affinity for serotonin 5-HT7 receptors (Ki = 0.5 nM), partial agonist activity at 5-HT1A receptors (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors.

Selective D2 receptor, Ki: 1 nM
S3201 Trifluoperazine 2HCl

Trifluoperazine 2HCl是一种多巴胺D2受体抑制剂,IC50为1.1 nM。

Selective Dopamine D2 receptor, IC50: 1.1 nM
S4889 Perospirone hydrochloride

Perospirone (SM-9018) is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist.

Selective D2 receptor, Ki: 1.4 nM
S5185 Perospirone

Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively.

Selective D2 receptor, Ki: 1.4 nM
S3044 Lurasidone HCl

Lurasidone HCl是一种非典型的抗精神病药物,抑制D2, 5-HT2A5-HT7, 5-HT1A和去甲肾上腺素α2C,IC50分别为1.68 nM, 2.03 nM, 0.495 nM, 6.75 nM和10.8 nM。

Selective D2 receptor, IC50: 1.68 nM
S4358 Pimozide

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

Selective Dopamine D2 receptor, Ki: 3.0 nM
S0104 Pardoprunox (SLV-308) hydrochloride

Pardoprunox hydrochloride is a novel agonist of partial dopamine D2 and D3 receptor and serotonin 5-HT1A receptor with pKi of 8.1, 8.6 and 8.5 for D2 receptor, D3 receptor and 5-HT1A receptor, respectively.

Selective D2 receptor, pEC50: 8.0
S3189 Ropinirole HCl

Ropinirole HCl是一种选择性的D2受体抑制剂,IC50为29 nM。

Selective D2 receptor, Ki: 29 nM
S5153 Tetrahydroberberine

Tetrahydroberberine (Canadine) is an isoquinoline alkaloid with micromolar affinity for dopamine D2 (antagonist, pKi = 6.08) and 5-HT1A (agonist, pKi = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors.

Selective D2 receptor, pKi: 6.08
S4251 Phenothiazine

Phenothiazine是多巴胺-2(D2)受体拮抗剂,因此能够降低多巴胺在大脑中的作用。

Selective
S2104 Levosulpiride

Levosulpiride是一种选择性D2多巴胺受体拮抗剂,用作抗精神病药和促动力剂。

Selective
S2493 Olanzapine

Olanzapine是一种高亲和力的5-HT2 5-羟色胺和多巴胺D2受体拮抗剂。

Selective
S6853 ONC206

ONC206 is a selective antagonist of dopamine D2-like receptors (DRD2/3/4) with broad-spectrum anti-tumor activity.

Selective
S4289 Metoclopramide HCl

Metoclopramide HCl是一种选择性的 dopamine D2 receptor 拮抗剂,用于治疗恶心和呕吐。

Selective
S2461 Domperidone

Domperidone 是一种多巴胺受体抑制剂,是一种抗多巴胺试剂。

Selective
S5197 Loxapine

Loxapine (Adasuve), a typical neuroleptic, is a drug with D2/D3 receptor antagonist activity and a higher affinity for D3 than D2. Loxapine displays an extremely strong binding affinity for dopamine D4 and serotonin 5-HT2 receptors.

Selective
S4655 Sulpiride

Sulpiride是一种多巴胺D2受体拮抗剂。在临床治疗中,它被用作抗抑郁剂、安定药和助消化药。

Selective
S5481 Molindone hydrochloride

Molindone hydrochloride is the hydrochloride salt form of molindone, a conventional antipsychotic used in the therapy of schizophrenia. It is a dopamine D2/D5 receptor antagonist.

Pan
S5842 Cabergoline

Cabergoline (FCE-21336), an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor.

Pan D2 receptor, IC50: 0.7 nM
S5066 Pramipexole dihydrochloride

Pramipexole dihydrochloride (SND919) is a dopamine agonist of the non-ergoline class indicated for treating Parkinson's disease (PD) and restless legs syndrome (RLS) with Ki values of 3.9 nM, 2.2 nM, 0.5 nM and 5.1 nM for D2S receptor, D2L receptor, D3 receptor and D4 receptor.

Pan D2S Receptor, Ki: 3.9 nM; D2L Receptor, Ki: 2.2 nM
S2460 Pramipexole

Pramipexole是部分/全部D2S, D2L, D3, D4受体激动剂,作用于D2S, D2L, D3, D4受体,Ki分别为3.9, 2.2, 0.5和5.1 nM。

Pan D2S Receptor, Ki: 3.9 nM; D2L Receptor, Ki: 2.2 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 D2 receptor, Ki: 2.96 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 D2 Receptor, pKi: 8.19
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; D2 receptor (bovine), Ki: 26 nM
S3656 Piribedil

Piribedil (Trivastal, Trivastan) is a relatively selective dopamine (D2/D3) agonist with moderate antidepressant activity. It also has α2-adrenergic (α2A/α2C) antagonist properties.

Pan D2 receptor, pKi: 6.9
S2437 Rotundine

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

Pan D2 receptor, IC50: 1.47 μM
S2011 Pramipexole 2HCl Monohydrate

Pramipexole 2HCl Monohydrate 是一种部分/全部D2S, D2L, D3, D4受体激动剂,Ki为3.9, 2.2, 0.5, 5.1 nM。

Pan