European journal of medicinal chemistry

Histamine analogues. 32nd communication: synthesis and pharmacology of sopromidine, a potent and stereoselective isomer of the achiral H 2-agonist impromidine

S Elz, G Gerhard, W Schunack

Index: Elz, Sigurd; Gerhard, Guenter; Schunack, Walter European Journal of Medicinal Chemistry, 1989 , vol. 24, p. 259 - 262

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Citation Number: 9

Abstract

Abstract Synthesis and pharmacology of sopromidine ((R)-7) and (S)-7, 2 position isomers of impromidine derived from the enantiomeric α-methylhistamines, are reported. The enantiomers of 7 show high stereoselectivity at the atrial H 2-receptor of the guinea-pig.(R)-7 is revealed to be a full H 2-agonist with 7.4-fold potency relative to histamine, while (S)-7 is a competitive H 2-antagonist.