dopamine d3 receptor

Dopamine D3 receptor ligand-6 (Compound 196476) is a selective antagonist of the dopamine D3 receptor (D3). It holds potential for research in substance use disorders, including opioid and psychostimulant addiction.

Dopamine D3 receptor antagonist-3 is a selective positive allosteric modulator-antagonist (PAM-antagonist) of the D3 dopamine receptor (D3R) that can cross the blood-brain barrier. It demonstrates antagonistic activity in D3R-mediated β-arrestin recruitment assays with an IC50 of 2.5 μM and Kb of 0.49 μM, and in D3R-mediated Go-BRET assays with an IC50 of 0.34 μM. Dopamine D3 receptor antagonist-3 is applicable for the study of neuropsychiatric disorders, including substance use disorders.

Dopamine D3 receptor ligand is a potent, selective, high-affinity compound with 89 times greater selectivity for D3 receptors (Ki: 8 nM) compared to D2 receptors (Ki: 715 nM).

Dopamine D3 receptor antagonist-2 is a dopamine D3 receptor-selective compound (Ki=2.16 nM) that exhibits potential therapeutic effects in CNS disorders.

Dopamine D3 receptor antagonist-1 is a dopamine D3 receptor-selective or multi-targeting ligand with a Ki value of 1.58 nM, showing therapeutic potential for central nervous system disorders.

Dopamine D3 receptor agonist 13a selectively targets the dopamine D3 receptor over dopamine D1, D2, and D4 receptors, with affinities (Ki values) of 0.14, 4,600, 2.85, and 756 nM, respectively. It also interacts with serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT2A, 5-HT2B, and 5-HT2C, with Ki values of 6, 54, 1.47, and 252 nM, respectively. While acting as a partial agonist at dopamine D2 receptors (EC50 = 2.26 nM in a G protein recruitment assay), it serves as an antagonist at dopamine D3 receptors (IC50 = 4.62 nM). Additionally, Dopamine D3 receptor agonist 13a, at a dose of 3 mg/kg, has been shown to reduce cocaine self-administration in rats.

Cariprazine D6 (RGH-188 D6) is a deuterium-labeled Cariprazine. Cariprazine is an antipsychotic agent (D3 receptors, Ki: 0.085 nM; D2 receptors, Ki: 0.49 nM).

Cabergoline (FCE-21336) is an ergot derived-dopamine D2-like receptor agonist. It has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).Cabergoline permits rapid and effective hormonal and tumor control by normalizing prolactin-producing pituitary adenomas levels.

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.

L-745870 hydrochloride has excellent brain penetration. L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 receptor affinity with a Ki of 960 nM and D3 receptor affinity with a Ki of 2300 nM. 

L-745870 is an orally active, selective, and efficient dopamine D4 receptor antagonist that crosses the blood-brain barrier. It also inhibits D2 receptors, 5-HT2 receptors, and α-adrenergic receptors, useful in neurological disease studies.

FAUC-312 is a potent and selective agonist of the dopamine D4 receptor.

SK609 HCl (SK609 hydrochloride) is a dopamine D3 receptor (D3R) selective agonist that inhibits norepinephrine transporter proteins and can be used to study Parkinson's disease and cognitive disorders.

SUN-1334H free base, an orally active histamine H1 receptor inhibitor, exhibits a K_i of 9.7 nM and an IC 50 of 20.3 nM. Additionally, it effectively prevents histamine-induced contractions in isolated guinea-pig ileum with an IC 50 of 0.198 μM. The compound also blocks histamine-induced bronchoconstriction and skin wheals in guinea pigs and beagle dogs, respectively, and mitigates ovalbumin-induced rhinitis in guinea pigs.

PF-592379 is a potent agonist of dopamine D3 receptor (EC50: 21 nM).

A-437203 (Lu201640) is A kind of based on 1 h - pyrimidin - 2 - one sca ff old, selective, new powerful d3 receptor antagonist, on D2, d3, and D4 receptor, Ki value 71, respectively 1.6 and 6220 nM.

PNU-177864 hydrochloride is a potent, selective, and orally active dopamine D3 receptor antagonist that is structurally consistent with a cationic amphiphilic drug (CAD). It induces phospholipidosis in vivo and exhibits antischizophrenic activity.

SB-277011 (SB-277011A) is a specific antagonist of the dopamine D3 receptor with pKi values of 8.0, 6.0, 5.0, and <5.2 for D3 receptor, D2 receptor, 5-HT1D, and 5-HT1B respectively.

Didesmethyl cariprazine, a metabolite of Cariprazine, is the major cyclic active part. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a potent D3 preference D3/D2 receptor partial agonist of dopamine for the treatment of schizophrenia, bipolar mania, and depression, with a high affinity for d3 and d2 receptors and a moderate affinity for 5-HT 1A receptors.

NGD 94-1 is a selective D4 receptor antagonist with an affinity of 3 nM for the D4 receptor and greater than 2 pM for the D1, D2, D3, and D5 receptors.NGD 94-1 can be used in the study of cognitive disorders and other psychiatric disorders.

BP14979 is a dopamine D3 receptor agonist that can be used to study neurological disorders.

Aplindore Fumarate (DAB-452) is a small molecule dopamine D2 receptor partial agonist.Aplindore Fumarate exhibits high affinity for dopamine D2 and D3 receptors, and low affinity for dopamine D4, 5-hydroxytryptophan (5-HT2), and α1-adrenergic receptors.Aplindore Fumarate is used in the study of Parkinson's disease and schizophrenia. Fumarate can be used to study Parkinson's and schizophrenia.

Trazpiroben (TAK-906) is a selective dopamine D2/D3 receptor antagonist utilized in gastroparesis research.

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.