Biological Activity
bms-193885 is a potent and selective neuropeptide y1 receptor antagonist with ic50 of 5.9nm.neuropeptide y receptor 1 is g-protein coupled receptors and implicated in the modulation of food intake and energy homeostasis. neuropeptide y1 is expressed in many tissues including the hippocampus, hypothalamus, amygdala and the cortex of the brain as well as in peripheral tissues heart, kidney, skeletal muscle. the localization and expression suggests their involvement in the regulation of food intake and body weight.in cellular culture, bms-193885 displayed functional antagonism of neuropeptide y1 in aforskolin-stimulated c-amp production assay using cho cells expressing the human y(1) receptor 1.
in vivo
administration of bms-193885 at a dosage of 10mg/kg leads to 1h neuropeptide y-induced food intake in rat and the spontaneous overnight food consumpetion 2 . chronic administration of bms-193885 (10 mg/kg) i.p. for 44 days significantly reduced food intake and the rate of body weight gain as compared to their control without developing tolerance or affecting water intake 2.
References
1. poindexter gs, bruce ma, leboulluec kl, et al. dihydropyridine neuropeptide y y(1) receptor antagonists. bioorganic & medicinal chemistry letters. 2002;12(3):379-382.2. antal-zimanyi i, bruce ma, leboulluec kl, et al. pharmacological characterization and appetite suppressive properties of bms-193885, a novel and selective neuropeptide y(1) receptor antagonist. european journal of pharmacology. 2008;590(1-3):224-232.
