D2 receptor 选择性抑制剂 | 激动剂 | 拮抗剂

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S4631

Prochlorperazine dimaleate salt

Prochlorperazine dimaleate (Prochlorperazin, Compazine, Capazine, Stemetil) is a dopamine (D2) receptor antagonist.

S6853

ONC206

ONC206 is a selective antagonist of DRD2/3/4 with broad-spectrum anti-tumor activity.

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.

S3201

Trifluoperazine 2HCl

Trifluoperazine (NSC-17474, RP-7623, SKF-5019) 2HCl is a dopamine D2 receptor inhibitor with IC50 of 1.1 nM. Trifluoperazine also inhibits calmodulin (CaM).

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.

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.

S3044

Lurasidone HCl

Lurasidone (SM-13496) is an atypical antipsychotic, inhibits Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C with IC50 of 1.68 nM, 2.03 nM, 0.495 nM, 6.75 nM and 10.8 nM, respectively.

S0104

Pardoprunox (SLV-308) hydrochloride

Pardoprunox hydrochloride (DU-126891, SME-308) is a potent but partial dopamine D2 receptor agonist with pEC50 of 8.0, and a partial agonist in the induction of [35S]GTPγS binding with pEC50 of 9.2 and a serotonin 5-HT1A receptor agonist, with pEC50 of 6.3, respectively.

S3189

Ropinirole HCl

Ropinirole (SKF-101468A) a selective dopamine D2 receptors agonist with Ki of 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.

S4251

Phenothiazine

Phenothiazine (ENT 38) is a dopamine-2 (D2) receptor antagonist therefore decreases the effect of dopamine in the brain.

S4655

Sulpiride

Sulpiride (Dolmatil, Dobren, Sulpyrid, Aiglonyl, Dogmatil) is a dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid.

S2493

Olanzapine

Olanzapine (LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.

S2461

Domperidone

Domperidone is an oral dopamine D2 receptor antagonist, used to treat nausea and vomiting.

S4289

Metoclopramide HCl

Metoclopramide HCl(Metoclopramide hydrochloride) is a selective dopamine D2 receptor antagonist, used for the treatment of nausea and vomiting.

S2104

Levosulpiride

Levosulpiride(RV-12309,S-(-)-Sulpiride) is a selective antagonist for D2 dopamine receptors used as an antipsychotic and prokinetic agent.

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.

S5842

Cabergoline

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

S2460

Pramipexole

Pramipexole (SND 919,Mirapexin,Sifrol,Mirapex) is a partial/full D2S, D2L, D3, D4 receptor agonist with a Ki of 3.9, 2.2, 0.5 and 5.1 nM for D2S, D2L, D3, D4 receptor, respectively.

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.

S1771

Chlorprothixene

Chlorprothixene(Minithixen,Truxal) has strong binding affinities to dopamine and histamine receptors, such as D1, D2, D3, D5, H1, 5-HT2, 5-HT6 and 5-HT7, with Ki of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM and 5.6 nM, respectively.

S4358

Pimozide

Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.

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.

S4309

Bromocriptine Mesylate

Bromocriptine mesylate is a dopamine receptor agonist with a Ki of 12.2 nM for D3 receptor and D2 receptor and a Ki of 1659 nM, 59.7 nM, 1691 nM for D1 receptor, D4 receptor, and D5 receptor, respectively. Bromocriptine mesylate is used in the treatment of Parkinson's disease, hyperprolactinemia-associated dysfunctions, and acromegaly.

S4086

Loxapine Succinate

Loxapine Succinate(NSC 759578) is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.

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.

S2437

Rotundine

Rotundine (L-tetrahydropalmatine, L-THP) is a selective dopamine D1 receptor antagonist with IC50 of 166 nM.

S2011

Pramipexole 2HCl Monohydrate

Pramipexole 2HCl Monohydrate is a novel non-ergoline dopamine (DA) agonist, used to treat Parkinson's disease.