d4 receptor

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.

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].

Compound 17, a dopamine D4 receptor ligand, exhibits high potency and selectivity with IC 50 values of 0.057 nM for D4, and >1000, 220, and 270 nM for D2, 5-HT1A, and α1 receptors, respectively [1].

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.

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

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.

D4R agonist-1 is a selective and potent D4R partial agonist (Ki:2.2 nM).D4R agonist-1 can be used to study neurological diseases.

BP 897 is a potent and selective agonist of dopamine D3 receptor and it is a weak dopamine D2 receptor antagonist, with Kis of 0.92 nM and 61 nM for D3 and D2 receptors. Which shows low affinities at D1 and D4 receptors (Kis, 3 and 0.3 μM, respectively).

L-745870 trihydrochloride is a highly potent and selective D4 dopamine receptor antagonist.

CP-226269 is a potent dopamine D4 receptor agonist that regulates calcium flux and has an EC50 value of 32.0 nM. CP 226269 can be used to study neurological disorders such as schizophrenia.

NRA-0160 is a selective antagonist of dopamine D4 receptor(Ki of 0.48 nM)

Pipamperone (McN-JR 3345) binds 5-HT2A closely as receptor.

Brilaroxazine (RP5063) is a potent multimodal dopamine/5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases.

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).

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.

ABT-724 is an agonist of dopamine D4 receptor(EC50: 12.4 nM)

Adoprazine (SLV313) is a potential atypical antipsychotic bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties.

Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist that acts on D2 (Ki: 0.56 nM), D3 (Ki: 0.43 nM), and 5-HT2A (Ki: 0.6 nM) receptors, and also binds Alpha-1A adrenergic receptors. It can induce apoptosis, inhibit cancer cell proliferation, and is used to study psychiatric disorders, cancer, and inflammation.

Tipelukast (KCA 757) is a novel, orally available leukotriene receptor antagonist with anti-inflammatory properties, capable of reducing fibrosis and down-regulating TIMP-1 and type 1 collagen. Tipelukast is utilized in asthma research.

Pramipexole (SND 919) is a selective dopamine receptor agonist used in the therapy of Parkinson disease. Pramipexole therapy is associated with a low rate of transient serum enzyme elevations during treatment but has not been implicated in cases of clinically apparent acute liver injury.

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

Asenapine Maleate (Org 5222 maleate) is a second generation (atypical) antipsychotic agent that is taken sublingually and used in the treatment of schizophrenia and manic or mixed episodes associated with bipolar 1 disorder. Asenapine is associated with a low rate of transient and mild serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent acute liver injury.

Flibanserin (Girosa) is a serotonergic antidepressant used to treat hypoactive sexual desire disorder. Flibanserin has been associated with a low rate of minor serum aminotransferase elevations during treatment but has not been linked to instances of clinically apparent acute liver injury.

Pramipexole dihydrochloride hydrate (Mirapex) is the hydrochloride salt of pramipexole, a benzothiazole derivative. As a nonergot dopamine agonist, pramipexole binds to D2 and D3 dopamine receptors in the striatum and substantia nigra of the brain.