human dopamine d4 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.

ABT-670 is a selective agonist of dopamine D4 receptor. For human D4, ferret D4, and rat D4, the EC50 values are 89 nM, 160 nM, and 93 nM , respectively.

Loxapine succinate (Loxapac), a D2DR and D4DR inhibitor, is utilized in schizophrenia.

Fananserin is an effective, selective and oral active antagonist of 5-HT2 (Ki = 0.37 nM for the rat 5-HT2A). Fananserin is an antagonist of human D4 receptor (Ki = 2.93 nM).

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).

Loxapine is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent,used primarily in the treatment of schizophrenia. The drug is a member of the dibenzoxazepine class and structurally related to clozapine (which belongs to the chemically akin class of dibenzodiazepines).

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).

SRA880 is a non-peptide somatostatin sst(1) receptor antagonist which displays a significantly lower affinity for the other human recombinant somatostatin receptors ( pK(d)= 6.0) or a wide range of neurotransmitter receptors, except for the human dopamine

SRA880 is a non-peptide antagonist of somatostatin sst1-receptor. SRA880 displayed significantly lower affinity for the other human recombinant somatostatin receptors ( pK(d) < or = 6.0). SRA880 shows a certain binding affinity to the human dopamine D4 re

U-101958 Maleate is a ligand of dopamine D4 receptor. U-101958 Maleate also binds to a large sigma1 receptor-like component in SK-N-MC neuroblastoma cells and human cerebellum with high affinity.

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.