Intra-CeA infusions of CP809101 attenuated cocaine-primed reinstatement, an effect that was prevented with concurrent administration of the 5-HT2CR antagonist SB242084 (0.1 μg/0.2 μl/side). CP809101 had no effect on cue reinstatement or anxiety-like behavior on the EPM. These ...
Reavill C, Kettle A, Holland V et al (1999) Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol 126(3):572–574PubMedCrossRef 20. Milatovich A, Hsieh CL, Bonaminio G et al (1992) Serotonin receptor 1c gene assigned to X chromosome in human ...
Of note intra-mPFC administration of the Neuropsychopharmacology 369 5-HT2C receptor in impulsivity and cocaine-seeking NC Anastasio et al 370 selective 5-HT2CR antagonist SB242084 did not significantly Anastasio NC, Lanfranco MF, Bubar MJ, Seitz PK, Stutz SJ, alter impulsive action under ...
Effects of pretreatment with the selective 5-HT 2C antagonist RS 102221 on the anxiogenic effects of mCPP on "sociability" in the social interaction test in wildtype C57BL/6J mice. Mice were given vehicle or RS 102221 1 mg/kg ip 15 min prior to vehicle or mCPP 1 mg/kg ip. RS 1022...
the antidepressantagomelatineis melatoninreceptor agonistand 5-HT2Creceptor antagonist: 5-HT2Cantagonism may lead to increased centraldopamine releaseand thus have antidepressant effects. There is also evidence for 5-HT2Creceptors editing in depression and suicidal ideation. Finally, 5-HT2Cediting (i.e.,...
we investigated the effects of systemic administration of the 5-HT2Aantagonist M100907 (0, 0.01, 0.03, and 0.1 mg/kg, i.p.) and the 5-HT2Cantagonist SB 242084 (0, 0.1, 0.3, and 1.0 mg/kg, i.p.) on the performance of an instrumental two-lever spatial discrimination and seri...
RS-102221: a novel high affinity and selective 5-HT2C receptor antagonist. Neuropharmacology 1997; 36: 621–629. Article CAS PubMed Google Scholar Nöthen MM, Cichon S, Hemmer S, Hebebrand J, Remschmidt H, Lehmkuhl G et al. Human dopamine D4 receptor gene: frequent occurrence of a ...
Competition between the agonist and antagonist binding can explain why these two mutations in the orthosteric binding site have different effects on receptor inhibition. We have observed a similar phenomenon at another class A GPCR, the adenosine A2A receptor (A2AAR), where mutation V275A7.40 ...
The term “antagonist” is intended to mean moieties that competitively bind to the receptor at the same site as agonists (for example, the endogenous ligand), but which do not activate the intracellular response initiated by the active form of the receptor, and can thereby inhibit the intracell...
and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2Creceptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insip...