D1 receptor 选择性抑制剂 | 激动剂 | 拮抗剂

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.

Fenoldopam mesylate

Fenoldopam (SKF 82526, Corlopam) is a selective dopamine-1 receptor (DA1) agonist with natriuretic/diuretic properties. It lowers blood pressure through arteriolar vasodilation.

Fenoldopam

Fenoldopam (SKF 82526) is a selective dopamine-1 (DA1) receptor agonist with natriuretic/diuretic properties with EC50 of 55.5 nM in stimulating cAMP accumulation in LLC-PK1 cells, which is more potent than DA .

Ansofaxine hydrochloride

Ansofaxine hydrochloride (LY03005, LPM570065), a triple reuptake inhibitor, inhibits serotonin, dopamine and norepinephrine reuptake with IC50 values of 723, 491 and 763 nM, respectively.

Penfluridol

Penfluridol (TLP-607,R-16341) is a highly potent, first generation diphenylbutylpiperidine antipsychotic.

Azaperone

Azaperone (NSC 170976) crosses the blood-brain barrier and binds to both DI and D2 receptors, being an antagonist of Dopamine receptors with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.

Amantadine HCl

Amantadine HCl (1-adamantanamine) is used to treat or prevent infections of the respiratory tract caused by a certain virus.

CNO (Clozapine N-oxide)

CNO (Clozapine N-oxide) 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.Solutions are unstable and should be fresh-prepared.

Quetiapine (ICI-204636) fumarate

Quetiapine Fumarate (ICI-204636) is an atypical antipsychotic used in the treatment of schizophrenia, bipolar I mania, bipolar II depression, bipolar I depression and shows affinity for various neurotransmitter receptors including serotonin, dopamine, histamine, and adrenergic receptors.

Amfebutamone (Bupropion) HCl

Amfebutamone (Bupropion) HCl(Wellbutrin) is a selective norepinephrine-dopamine reuptake inhibitor with IC50 of 6.5 and 3.4 μM for the reuptake of dopamine and norepinephrine, respectively.

Ziprasidone HCl

Ziprasidone HCl (CP-88059) is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder.

Metoclopramide

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

Rotigotine

Rotigotine(N-0923) is a dopamine receptor agonist, used in the treatment of Parkinson's disease and restless legs syndrome.

Amisulpride

Amisulpride (DAN-2163) is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder.

Dopamine HCl

Dopamine HCl(ASL279, NSC 173182) is a catecholamine neurotransmitter present in a wide variety of animals,And a dopamine D1-5 receptors agonist.

Alizapride HCl

Alizapride HCl(Alizapride hydrochloride) is a dopamine receptor antagonist used for the theropy of nausea and vomiting.

Levodopa

Levodopa(L-DOPA) is the precursor to the neurotransmitters dopamine, norepinephrine (noradrenaline), and epinephrine (adrenaline), used to treat Parkinson's symptoms.

Chlorpromazine HCl

Chlorpromazine HCl (Sonazine) is a dopamine and potassium channel inhibitor with IC50 of 6.1 and 16 μM for inward-rectifying K+ currents and time-independent outward currents.

Paliperidone

Paliperidone, the main active metabolite of Risperidone, is a potent serotonin-2A and dopamine-2 receptor antagonist, used in the treatment of schizophrenia.

SCH-23390 hydrochloride

SCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.

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 K_i of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM and 5.6 nM, respectively.

Loxapine Succinate

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

Rotundine

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

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.

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.

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.

SKF38393 HCl

SKF38393 HCl is a selective dopamine D1/D5 receptor agonist.