Biological Activity
mdl 72832 hydrochloride is a potent and selective ligand for 5-ht1a receptor with pic50 value of 9.1 [1].the 5-ht1a receptor is a g protein-coupled receptor for endogenous neurotransmitter serotonin (5-ht) and mediates inhibitory neurotransmission.mdl 72832 hydrochloride is a potent and selective ligand for 5-ht1a receptor [1]. also, mdl 72832 exhibited affinity with pkd values of 6.32 and 6.34 for 5-ht1c and 5-ht1d receptors, respectively [1].in rats, mdl 72832 inhibited 8-oh-dpat-induced cardiovascular effects. in guinea-pigs, 8-oh-dpat inhibited the contraction of the field-stimulated guinea-pig ileum in a concentration-dependent way. while mdl 72832 inhibited 8-oh-dpat-induced neuronal inhibition. mdl 72832 is a ligand for 5-ht1a receptor with mixed antagonist and agonist properties [1]. in pre-satiated rats, (+) -mdl 72832 (1.0 mg/kg) stimulated food intake and (-) -mdl 72832 (0.03 mg/kg) significantly increased food intake [2]. in rats, mdl 72832 increased postsynaptic 5-ht1a receptors mediating hypothermia and exhibited agonist property [3].
References
[1]. mir ak, hibert m, tricklebank md, et al. mdl 72832: a potent and stereoselective ligand at central and peripheral 5-ht1a receptors. eur j pharmacol, 1988, 149(1-2): 107-120.
[2]. neill jc, cooper sj. mdl 72832, a selective 5-ht1a receptor ligand, stereospecifically increases food intake. eur j pharmacol, 1988, 151(2): 329-332.
[3]. millan mj, rivet jm, canton h, et al. induction of hypothermia as a model of 5-hydroxytryptamine1a receptor-mediated activity in the rat: a pharmacological characterization of the actions of novel agonists and antagonists. j pharmacol exp ther, 1993, 264(3): 1364-1376.
