human d4 receptor

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-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).

Iloperidone (HP 873) is an atypical antipsychotic agent that is used for treatment of schizophrenia.

Sonepiprazole (PNU-101387G) is a chemical compound known for its selective antagonistic properties toward D4 dopamine receptors, exhibiting dissociation constants (Kis) of 3.6 nM and 10.1 nM for rat D4 (rD4) and human D4.2 (hD4.2) dopamine receptors, respectively; it shows significantly less affinity for rat D2 (rD2) dopamine and Histamine-H1 receptors, with Kis of 5147 nM and 7430 nM, respectively.

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 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).

Verlukast (MK-0679) is a selective, orally active leukotriene D4 receptor antagonist for use in bronchial asthma research.

Dopamine D4 receptor ligand 3 (Compound 16) functions as a dopamine D4 receptor (D4R) antagonist with a pKi of 8.86. In HEK-293T cells, it shows pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 sensors, respectively. This compound inhibits the activity of human glioma cell lines U87 MG, T98G, and U251 MG, and it induces ROS production and mitochondrial dysfunction in these glioma cells.

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).

ABT 724 trihydrochloride is an effective and selective agonist of the D4 receptor (EC50 = 12.4 nM, 14.3 nM, and 23.2 nM for human, rat and ferret, respectively). ABT-724 trihydrochloride can be used in erectile dysfunction studies.

Iloperidone hydrochloride is a D(2)/5-HT(2) receptor antagonist. It is also an atypical antipsychotic for the treatment of schizophrenia symptoms.

L 741742 hydrochloride is a selective, high-affinity human D4 receptor antagonist with good oral bioavailability and brain penetration, suitable for studying neurological disorders.

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

SV-156 is a highly selective antagonist of dopamine receptor 2 (D2).

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).

Ropinirole (SKF 101468) is an orally active and potent D3/D2 receptor agonist with anti-amyotrophic lateral sclerosis effects. Ropinirole is used in the study of Parkinson's disease.

Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear leukocytes (PMN) with IC50 values of 29 and 14 µM, respectively. Flufenamic acid also activates various ion channels, including transient receptor potential canonical 6 (TRPC6) and the large-conductance calcium-activated potassium channel (KCa1.1). It also inhibits various ion channels, including TRPC3 and the cystic fibrosis transmembrane conductance regulator (CFTR). Flufenamic acid (20 mg/kg) reduces increases in intestinal fluid secretion and intestinal barrier disruption in mice ......

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.