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.