Dopamine Receptor Dopamine Receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS). The neurotransmitter dopamine is the primary endogenous ligand for dopamine receptors. Dopamine receptors are implicated in many neurological processes, including motivation, pleasure, cognition, memory, learning, and fine motor control, as well as modulation of neuroendocrine signaling. Abnormal dopamine receptor signaling and dopaminergic nerve function is implicated in several neuropsychiatric disorders. Thus, dopamine receptors are common neurologic drug targets; antipsychotics are often dopamine receptor antagonists while psychostimulants are typically indirect agonists of dopamine receptors. There are at least five subtypes of dopamine receptors, D1, D2, D3, D4, and D5. The D1 and D5 receptors are members of the D1-like family of dopamine receptors, whereas the D2, D3 and D4receptors are members of the D2-like family. www.MedChemExpress.com 1 Dopamine Receptor Antagonists, Agonists, Inhibitors, Modulators & Activators (+)-Dihydrexidine hydrochloride (+)-PD 128907 hydrochloride ((+)-DAR-0100 hydrochloride) Cat. No.: HY-101299 Cat. No.: HY-110000 (+)-Dihydrexidine hydrochloride ((+)-DAR-0100 (+)-PD 128907 hydrochloride is a selective hydrochloride) is a dopamine D1 receptor dopamine D2/D3 receptor agonist, with Kis of agonist with an EC50 of 72± 21 nM. 1.7, 0.84 nM for human and rat D3 receptors, 179, 770 n M for human and rat D3 receptors, respectively. Purity: >98% Purity: 98.83% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg (-)-GSK598809 (-)-Isocorypalmine (1S,5R-GSK598809) Cat. No.: HY-19654B (Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine) Cat. No.: HY-N0927 (-)-GSK598809 is an isomer of GSK598809. GSK598809 (-)-Isocorypalmine (Tetrahydrocolumbamine), is a potent and selective dopamine D3 Receptor isolated from the crude base fraction of Corydalis (DRD3) antagonist. chaerophylla, is a dopamine receptor ligand. Recombinant CYP719A21 displays strict substrate specificity and high affinity (Km=4.63 ± 0.71 μM) for (-)-Isocorypalmine. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 5 mg (Rac)-PF-06256142 (Rac)-Rotigotine hydrochloride Cat. No.: HY-119943A Cat. No.: HY-15394 (Rac)-PF-06256142 is the less effective enantiomer (Rac)-Rotigotine hydrochloride is a racemate of of PF-06256142 (HY-119943). (Rac)-PF-06256142 is Rotigotine. an agonist of D1 receptor, with an EC50 of 107 nM. (Rac)-PF-06256142 can be used for the research of schizophrenia and Parkinson's disease. Purity: >98% Purity: 97.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg (Rac)-Tavapadon (±)-Methotrimeprazine (D6) ((Rac)-PF-06649751; (Rac)-CVL-751) Cat. No.: HY-119486A (dl-Methotrimeprazine D6) Cat. No.: HY-19489S (Rac)-Tavapadon ((Rac)-PF-06649751) is a potent (±)-Methotrimeprazine (D6) is the deuterium and selective noncatechol dopamine D1 receptor labeled Methotrimeprazine, which is a D3 dopamine agonist. and Histamine H1 receptor antagonist. Purity: 99.63% Purity: >98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg 2'-O-Methylisoliquiritigenin 3-O-Methyldopa Cat. No.: HY-N1745 (3-Methoxy-L-tyrosine; 3-O-Methyl-L-DOPA) Cat. No.: HY-113468A 2'-O-Methylisoliquiritigenin, isolated from the 3-O-Methyldopa (3-Methoxy-L-tyrosine) is a Arachis species, up-regulates 5-HT, NE, DA and metabolite of L-DOPA which is formed by GABA pathways, but does not put a very catechol-O-methyltransferase (COMT). significant effect on ne NE pathway. 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine. Purity: >98% Purity: ≥98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 1 mg, 5 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] 3-O-Methyldopa D3 5-HT6/7 antagonist 1 (3-Methoxy-L-tyrosine D3; 3-O-Methyl-L-DOPA D3) Cat. No.: HY-113468AS Cat. No.: HY-101622 3-O-Methyldopa D3 (3-Methoxy-L-tyrosine D3) is 5-HT6/7 antagonist 1 is a multifunctional ligand deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa that antagonizes 5-HT6/7/2A and D2 receptors, is a metabolite of L-DOPA which is formed by without interacting with M1 receptors and hERG catechol-O-methyltransferase (COMT). channels. 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine. Purity: ≥99.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg A-381393 A-437203 Cat. No.: HY-116941 (Lu201640; A37203) Cat. No.: HY-U00185 A-381393 is a potent, selective, brain penetrate A-437203 is a selective D3 receptor antagonist dopamine D4 receptor antagonist, with Kis of with Ki of 71, 1.6, and 6220 nM for D2, D3, and 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4 receptors, respectively. D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. Purity: 99.96% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 1 mg, 5 mg Abaperidone ABT-670 Cat. No.: HY-101619 Cat. No.: HY-19483 Abaperidone is a potent antagonist of ABT-670 is a selective, oral bioavailable agonist 5-HT2Areceptor and dopamine D2 receptor of dopamine D4 receptor, with EC50 of 89 with IC50s of 6.2 and 17 nM. nM, 160 nM, and 93 nM for humanD4, ferretD4, and ratD4, respectively. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg ABT-724 ABT-724 trihydrochloride Cat. No.: HY-14330 Cat. No.: HY-103409 ABT-724 is a potent and highly selective ABT-724 trihydrochloride is a potent and highly dopamine D4 receptor agonist with an EC50 selective dopamine D4 receptor agonist with of 12.4 nM for human dopamine D4 receptor. an EC50 of 12.4 nM for human dopamine D4 ABT-724 is a potent partial agonist at the rat receptor. D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). Purity: >98% Purity: 99.12% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg Adoprazine Alizapride hydrochloride (SLV313) Cat. No.: HY-14782 Cat. No.: HY-A0125A Adoprazine (SLV313) is a full 5-HT1A receptor Alizapride hydrochloride is a dopamine agonist with a pEC50 of 9 at cloned h5-HT1A receptor antagonist with prokinetic and receptors. Adoprazine (SLV313) is a full D2 and antiemetic effects which can also be used in the treatment of nausea and vomiting, including D3 receptor antagonist with pA2s of 9.3 and postoperative nausea and vomiting. 8.9 at hD2 and hD3 receptors, respectively. Purity: 98.10% Purity: 99.95% Clinical Data: Phase 1 Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 50 mg, 100 mg www.MedChemExpress.com 3 Amisulpride Amisulpride hydrochloride (DAN 2163) Cat. No.: HY-14545 (DAN 2163 hydrochloride) Cat. No.: HY-14545A Amisulpride is a dopamine D2/D3 receptor Amisulpride hydrochloride is a dopamine D2/D3 antagonist with Kis of 2.8 and 3.2 nM for human receptor antagonist with Kis of 2.8 and 3.2 nM dopamine D2 and D3, respectively. for human dopamine D2 and D3, respectively. Purity: 99.96% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 100 mg, 200 mg, 500 mg Size: 1 mg, 5 mg Ansofaxine hydrochloride Asenapine (LY03005; LPM570065) Cat. No.: HY-U00096 (Org 5222) Cat. No.: HY-10121 Ansofaxine hydrochloride (LY03005; LPM570065) is a Asenapine (Org 5222), an atypical antipsychotic, triple reuptake inhibitor; inhibits serotonin, is an antagonist of serotonin receptors (pKi: dopamine and norepinephrine reuptake with IC50 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), values of 723, 491 and 763 nM, respectively. dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Purity: 99.85% Purity: 98.81% Clinical Data: Phase 1 Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 20 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Asenapine hydrochloride Asimilobine Cat. No.: HY-16567 Cat. No.: HY-N7512 Asenapine hydrochloride, an antipsychotic, is a Asimilobine is an aporphine isoquinoline alkaloid 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and isolated from plant species of Magnolia obobata Dopamine (D2, D3, D4) receptor antagonist with Thun. Asimilobine is a dopamine biosynthesis Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, inhibitor and a serotonergic receptor antagonist. 1.1 nM for Dopamine receptor, respectively. Asimilobine shows an antimalarial and anti-cancer activity. Purity: 98.76% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg Azaperone Benzamide Derivative 1 (R-1929) Cat. No.: HY-B1470 Cat. No.: HY-U00415 Azaperone (R-1929) acts as a dopamine antagonist Benzamide Derivative 1 is a benzamide derivative but also has some antihistaminic and from patent EP0213775A1, compound 18. Benzamide anticholinergic properties. Derivative 1 may be useful in treatment of gastrointestinal disorders. Purity: 99.77% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 1 mg, 5 mg Benztropine mesylate (Benzatropine mesylate; Benzotropine BGC20-761 mesylate; Benztropine methanesulfonate) Cat.