human dopamine d3 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.

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.

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, and orally active dopamine D3 receptor (D3R) antagonist that crosses the blood-brain barrier, with Ki values of 10.7 nM for rodent D3R and 11.2 nM for human D3R. It is 80-100 times more selective for D3 receptors than other dopamine receptors, acting on D3 receptors (pKi: 8.0), D2 receptors (pKi: 6.0), 5-HT1B receptors (pKi < 5.2), and 5-HT1D receptors (pKi: 5.9).

L-741626 (3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole) is a selective antagonist of D2 dopamine receptor (Ki: 2.4, 100, and 220 nM for human D2, D3 and D4 receptors respectively).

RG-15 is an orally active dopamine receptor antagonist with high affinity for the human D2 receptor (pKi of 8.23) and human D3 receptor (pKi of 10.49). It inhibits dopamine-stimulated [35S]GTPγS binding with IC50 values of 21.2 nM in rat striatal membranes, 36.7 nM in mouse A9 cells expressing human D2L receptors, and 7.2 nM in CHO cells expressing human D3 receptors. RG-15 enhances dopamine turnover and synthesis in the striatum and olfactory bulb of mice, exhibiting antipsychotic activity.

L 741742 is an effective and highly selective antagonist of the D4 dopamine receptor (Ki: 1700, 770, and 3.5 nM at cloned human D2, D3, and D4 receptors).

Mesdopetam (IRL790), a dopamine D3 receptor antagonist with a Ki of 90 nM and an IC50 of 9.8 μM for the human recombinant D3 receptor, exhibits psychomotor stabilizing properties and is used in the study of motor and psychiatric complications associated with Parkinson's disease.

A-381393 is a selective and brain penetrate dopamine D4 receptor antagonist (Kis: 1.9/1.5/1.6 nM for human dopamine D4.2/D4.4/D4.7 receptor).

N-Despropyl ropinirole is an active metabolite of the dopamine D2 receptor agonist ropinirole. It increases extracellular acidification rates in CHO cells expressing human dopamine D2, D3, and D4 receptors (EC50s = 0.63, 0.063, and 1.23 µM, respectively). N-Despropyl ropinirole is also a potential impurity found in commercial preparations of ropinirole.

6-Hydroxy Buspirone, an active metabolite of the anxiolytic compound buspirone, is produced via the cytochrome P450 (CYP) isoform CYP3A4. This compound exhibits affinity for the serotonin (5-HT) receptor subtype 5-HT1A, demonstrating efficacy in the rat hippocampus and dorsal raphe with half-maximal effective concentrations (EC50s) of 4 and 1 µM, respectively. Furthermore, 6-Hydroxy Buspirone acts as a potent antagonist against dopamine D2, D3, and D4 receptors with half-maximal inhibitory concentrations (IC50s) of 3.1, 4.9, and 0.85 µM, respectively, and inhibits the organic cation transporters 1 (OCT1), OCT2, and OCT3 in S2 proximal tubule cells expressing human transporters, showcasing a concentration-dependent mechanism.

CELT-426 is a potent, partially selective fluorescent antagonist of the human D2 dopamine receptor, exhibiting Ki values of 89.3 nM, 194.8 nM, and 263.6 nM for D2, D3, and D4 dopamine receptors, respectively, in radioligand binding assays. This compound serves as an effective fluorescent probe for dopamine receptors, facilitating its application in a range of techniques including fluorescence binding assays, live cell imaging, flow cytometry, and fluorescence polarization assays. It provides an alternative to GPCR radiolabeling ligands. CELT-426 possesses excitation and emission maxima (λ) of 560 nm and 571 nm, respectively, making it suitable for use as an acceptor dye in Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) assays in conjunction with the CoraFluor1 TR-FRET donor.

Mesdopetam hemitartrate (IRL790 hemitartrate) is an antagonist of dopamine D3 receptor (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor). It has psychomotor stabilizing properties.

Desmethyl cariprazine-d8 is the deuterium-labeled form of Desmethyl cariprazine. Desmethyl cariprazine is a primary active metabolite of cariprazine, exhibiting activity at human dopamine receptors and serotonin receptors, with human D2 receptor pEC50 = 8.90, D3 receptor pEC50 = 8.09, and 5-HT1A receptor pEC50 = 6.28. It inhibits forskolin-induced cAMP production at D2, D3, and 5-HT1A receptors and serotonin-induced Ca2+ release at 5-HT2B receptors. Desmethyl cariprazine is applicable in studies related to schizophrenia, bipolar I disorder, and bipolar disorders.