sb242084 dihydrochloride

SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, which closely resembled its corresponding receptor binding affinity [1].in vivo: SB 242084 potently inhibited m-chlorophenylpiperazine (mCPP, 7 mgkg i.p. 20 min pre-test)-induced hypolocomotion in rats, a model of in vivo central 5-HT2C receptor function, with an ID50 of 0.11 mg kg i.p., and 2.0 mg kg p.o. SB 242084 (0.1-1 mg kg i.p.) exhibited an anxiolytic-like profile in the rat social interaction test, increasing time spent in social interaction, but having no effect on locomotion. SB 242084 (0.1-1 mg kg i.p.) also markedly increased punished responding in a rat Geller-Seifter conflict test of anxiety, but had no consistent effect on unpunished responding [1].

SB-747651A dihydrochloride is a chemical compound that serves as an ATP-competitive inhibitor for mitogen- and stress-activated kinase 1 (MSK1), featuring an IC50 of 11 nM. Additionally, this compound effectively inhibits PRK2, RSK1, p70S6K, and ROCK-II, showcasing its potential in inflammation research [1].

SB 699551 dihydrochloride is a 5-ht5a receptor antagonist.

SB 242084 dihydrochloride hydrate is a psychoactive drug and research chemical which acts as a selective antagonist for the 5HT2C receptor.

SB 243213 dihydrochloride is an orally active, selective, and high-affinity antagonist of the 5-hydroxytryptamine (5-HT)2C receptor, with a pKi of 9.37 and a pKb of 9.8 for the human 5-HT2C receptor.

SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate antagonist of dopamine D3 receptor(pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively).

SB-772077B dihydrochloride is an aminofurazan-based Rho kinase inhibitor with IC50 values of 5.6 nM for ROCK1 and 6 nM for ROCK2.

SB 242084 monohydrochloride is a selective, competitive, and high-affinity 5-HT2C receptor antagonist (pKi=9.0) that can cross the blood-brain barrier. This compound enhances the basal activity of dopaminergic neurons in the ventral tegmental area (VTA) and increases dopamine release in the nucleus accumbens. Additionally, SB 242084 monohydrochloride boosts the expression of mitochondrial genes and oxidative metabolism via the 5-HT2A receptor. Its potential for research in anxiety, depression, negative symptoms of schizophrenia, and acute organ damage is significant.