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