dopamine 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 D2 receptor agonist-2 (Dopamine D2 Receptor) is a ligand targeting the dopamine D2 receptor.

Dopamine D4 receptor antagonist-1 can be used in schizophrenia study. Dopamine D4 receptor antagonist-1 is a selective antagonist of Dopamine D4 receptor (DRD4). The Ki value of Dopamine D4 receptor antagonist-1 for Hd4.2 is 9.0 nM [1].

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.

5-HT1A modulator 1 exhibits high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

Pentiapine (CGS 10746) is a novel inhibitor of dopamine release.

ONC206, an analogue of the TRAIL inducer ONC201, acts as a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations and possesses broad-spectrum anti-tumor activity.

MPTP hydrochloride is a dopamine neurotoxin and the precursor of MPP⁺. It can induce apoptosis and has the ability to cross the blood-brain barrier. MPTP hydrochloride is toxic to dopaminergic neurons and is commonly used for the construction of Parkinson's disease animal models.

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

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.

(Rac)-AMXT-1501 4HCl is a polyamine transport inhibitor that inhibits polyamine transport and acts synergistically with cisplatin in HNSCC. (Rac)-AMXT-1501 4HCl has potential antimicrobial activity and inhibits neuroblastoma cell proliferation and pneumococcal pod biosynthesis by targeting ornithine decarboxylase and polyamine transport.

Carmoxirole hydrochloride (EMD 45609 hydrochloride) is a selective dopamine D2 receptor agonist with in vivo antihypertensive activity.

Dopamine D2 Receptor Antagonist-1 functions as a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R), demonstrating sub-millimolar affinity.

NMI 8739 (n-docosahexaenoyl dopamine) is an agonist of D2 autoreceptor. NMI 8739 reduces NO production and elicits concentration-dependent suppression of CCL-20, MCP-1 and IL-6 release.

JNJ-37822681 has potential for the treatment of schizophrenia and bipolar disorder.JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D2 receptor antagonist with a moderate binding affinity for the dopamine D2

PD 168568 dihydrochloride (PD 168568 (dihydrochloride)) is an orally active and selective antagonist of D4 dopamine receptor(Ki of 8.8 nM).

Piperidine-MO-1 is a dopamine receptor modulator, with an ED50 of 68 μmol/kg on increase of DOPAC in the rat striatum.

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.