Histamine analogues. 32nd communication: synthesis and pharmacology of sopromidine, a potent and stereoselective isomer of the achiral H2-agonist impromidine

Article abstract of DOI:10.1016/0223-5234(89)90007-X

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 H₂-receptor of the guinea-pig. (R)-7 is revealed to be a full H₂-agonist with 7.4-fold potency relative to histamine, while (S)-7 is a competitive H₂-antagonist. chiral H₂-agonists / histamine H₂-receptor / impromidine analogues / α-methylhistamine