N-[2-hydroxy-5-[2-(methylamino) ethyl] phenyl] methanesulfonamide. A potent agonist which releases intracellular calcium by activation of. alpha. 1-adrenoceptors

RM DeMarinis, P Lavanchy, JP Hieble…

Index: DeMarinis, Robert M.; Lavanchy, Patricia; Hieble, J, Paul; Jim, Kam F.; Matthews, William D. Journal of Medicinal Chemistry, 1985 , vol. 28, # 2 p. 245 - 248

Full Text: HTML

Citation Number: 5

Abstract

N-[2-Hydroxy-5-[2-(methylamino) ethyl] phenyl] methanesulfonamide (SK&F 102652) has been prepared and characterized pharmacologically. It is a potent agonist with an of 25 nM at al-adrenoceptors as determned in the isolated perfused rabbit ear artery. On the presynaptic a2-adrenoceptors of the guinea pig atrium it was considerably weaker, demonstrating an EC50 for inhibition of neurotransmission of 1200 nM and thus an overall ...