Guanoclor is an antihypertensive agent that binds to non-adrenergic sites in pig kidney membranes (IC50 = 10 nM).1,2 It inhibits the Na+/H+ exchanger in pig kidney membranes (IC50 = 1 μM) and cell-free bovine dopamine β-hydroxylase (IC50 = 90 μM). Guanoclor inhibits electrically stimulated norepinephrine release from spleen.1 It decreases norepinephrine levels in dog heart, spleen, hypothalamus, and adrenal gland when administered at a dose of 10 mg/kg per day for six weeks. It decreases adrenal catecholamine levels in rats when administered at a dose of 20 mg/kg per day for six weeks. Guanoclor (20 mg/kg) decreases experimentally induced hypertension and the tyramine-induced pressor response and increases the norepinephrine-induced pressor response in non-anesthetized dogs.
|1. Lawrie, T.D., Lorimer, A.R., McAlpine, S.G., et al. Clinical trial and pharmacological study of compound 1029. ("Vatensol"). Br. Med. J. 1(5380), 402-406 (1964).|2. Vigne, P., Lazdunski, M., and Frelin, C. Guanabenz, guanochlor, guanoxan and idazoxan bind with high affinity to non-adrenergic sites in pig kidney membranes. Eur. J. Pharmacol. 160(2), 295-298 (1989).