D2 receptor Selective Inhibitors | Agonists | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S4631 Prochlorperazine dimaleate salt

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

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 (SKF5019) is a dopamine D2 receptor inhibitor with IC50 of 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 (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.

Selective D2 receptor, IC50: 1.68 nM
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.

Selective D2 receptor, pEC50: 8.0
S3189 Ropinirole HCl

Ropinirole (SKF-101468A) a selective dopamine D2 receptors agonist with Ki of 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
S4289 Metoclopramide HCl

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

Selective
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.

Selective
S6853 ONC206

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

Selective
S2461 Domperidone

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

Selective
S2493 Olanzapine

Olanzapine (LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.

Selective
S2104 Levosulpiride

Levosulpiride is a selective antagonist for D2 dopamine receptors used as an antipsychotic and prokinetic agent.

Selective
S4251 Phenothiazine

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

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
S2460 Pramipexole

Pramipexole (SND 919) 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.

Pan D2S Receptor, Ki: 3.9 nM; D2L Receptor, Ki: 2.2 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 D2L Receptor, Ki: 2.2 nM; D2S Receptor, Ki: 3.9 nM
S1771 Chlorprothixene

Chlorprothixene 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.

Pan D2 receptor, Ki: 2.96 nM
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 α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.

Pan Dopamine D2 receptor, Ki: 3.0 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 is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.

Pan D2 receptor (bovine), Ki: 26 nM; D2 receptor (human), Ki: 24 nM; D2 receptor (Human), Ki: 24 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 (L-tetrahydropalmatine, L-THP) is a selective dopamine D1 receptor antagonist with IC50 of 166 nM.

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

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

Pan
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.

Pan