d1-receptors

dopamine D1 receptor antagonist

SKF83959, a benzazepine analog, is a selective and potent partial agonist of the dopamine D1 receptor with Ki values of 1.18, 7.56, 920, and 399 nM for rat D1, D5, D2, and D3 receptors, respectively.SKF83959 is a potent variant modulator of the sigma (σ)-1 receptor, which ameliorates cognitive dysfunction for the study depression and Alzheimer's disease.

Ropinirole hydrochloride (SKF-101468A) is a selective dopamine D2 receptors agonist (Ki: 29 nM). Ropinirole hydrochloride (SKF-101468A) is the hydrochloride salt form of ropinirole, a non-ergot dopamine agonist with antiparkinsonian property.

Zuclopenthixol (cis-Clopenthixol) is a thioxanthene with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors.

Ecopipam (UNII-0X748O646K) is a potent, selective, and orally active antagonist of dopamine D1 D5 receptors, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam demonstrates more than 40-fold selectivity over D2, D4, 5-HT, and α2a receptors (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). It is used in research on schizophrenia and obesity.

Pimozide (R6238) is a diphenylbutylpiperidine derivative and a dopamine antagonist with the antipsychotic property. Pimozide selectively inhibits type 2 dopaminergic receptors in the central nervous system (CNS), thereby decreasing dopamine neurotransmission and reducing the occurrence of the motor and vocal tics and delusions of parasitosis. In addition, this agent antagonizes alpha-adrenergic and 5-HT2 receptors.

SCH-23390 hydrochloride (R-(+)-SCH23390 hydrochloride) is an effective dopamine receptor antagonist, with high affinity for the D1 (Ki=0.2 nM) and D5 (Ki=0.3 nM) receptors.

BP 897 is a potent and selective agonist of dopamine D3 receptor and it is a weak dopamine D2 receptor antagonist, with Kis of 0.92 nM and 61 nM for D3 and D2 receptors. Which shows low affinities at D1 and D4 receptors (Kis, 3 and 0.3 μM, respectively).

UCM-1306 is a potent and orally active allosteric modulator (PAM) of the human dopamine D1 receptor. It increases the maximal effect of endogenous dopamine (DA) in both human and mouse D1 receptors. UCM-1306 could improve motor symptoms and address key comorbid cognitive impairment associated with long-term Parkinson's disease (PD).

Chlorprothixene hydrochloride (Truxal hydrochloride) brings strong blocking effects by blocking the 5-HT2 D1, D2, D3, histamine H1, muscarinic and alpha1 adrenergic receptors. Chlorprothixene hydrochloride s a typical antipsychotic drug of the thioxanthene (tricyclic) class.

Quetiapine (ICI204636) is used for the therapy of schizophrenia, and for the treatment of acute manic episodes associated with bipolar I disorder. The mechanism of quetiapine' action is thought by mediated through antagonist activity at serotonin and dopamine receptors. Specifically, the D1 and D2 dopamine, the α1 adrenoreceptor and α2 adrenoreceptor, and 5-HT1A and 5-HT2 serotonin receptor subtypes are antagonized. Quetiapine also can inhibit the histamine H1 receptor.

GR 103691, a potent and selective dopamine D3 receptor antagonist (Ki: 0.4 nM), exhibits more than 100-fold selectivity for human dopamine D3 receptors over human D4 and D1 sites.

SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist, specifically targeting D1 and D5 receptors with Ki values of 0.2 nM and 0.3 nM, respectively.

Dinoxyline is a potent dopamine receptor agonist, with dissociation constants (Ki values) for D1, D2, D3, and D4 receptors being 7 nM, 6 nM, 5 nM, and 43 nM, respectively. It is utilized in neuroscience research.

Biriperone is a potential neuroinhibitor that acts by blocking D1, D2, and 5-HT2A receptors.

Rotigotine Hydrochloride (N-0924), a dopamine receptor agonist prefering for D3 receptors over D1 and D2, has effective activity of anti-Parkinsonian. Racemic rotigotine hydrochloride is about 50 times as potent as quinpirole, the gold standard D2 agonist.

Pergolide mesylate salt(LY127809) is a long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.

RS 67333 hydrochloride (RO5203648) is a potent, selective partial agonist of the 5-HT4 receptor (5-HT4R) with a pKi value of 8.7 in guinea-pig striatum. It demonstrates lower binding affinities for other receptors, including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1 and D2, and muscarinic M1-M3 receptors. Notably, RS 67333 hydrochloride exhibits neuroprotective properties, rendering it useful in Alzheimer's disease research.

NGB 2904 is a potent and selective antagonist of dopamine D3 receptor (Ki values are 1.4, 217, 223, 642, > 5000, > 10000 and > 10000 nM for D3, D2, 5-HT2, α1, D4, D1 and D5 receptors respectively). NGB2904 potently antagonizes mitogenesis stimulated by quinpirole (IC50 = 6.8 nM).

Zelandopam is a dopamine D1 agonist. Zelandopam is a potent stimulant of pancreatic exocrine secretion by acting on DA D1 receptors of the pancreas in dogs. Intravenous administration of Zelandopam produces renal vasodilating and diuretic natriuretic effe

Bt-sch is an imaging agent based on D1 and D2 receptors of dopamine.

Zicronapine( LU 31-130) is an atypical antipsychotic. Zicronapine has monoaminergic activity and multi-receptor properties. It has shown effective antagonism against dopamine D1, D2, and serotonin 5HT2A receptors in vitro and in vivo.

Zuclopenthixol dihydrochloride is an D1 and D2 dopamine receptors antagonist.

Clopenthixol is a thioxanthene with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors.