Histamine analogues. 32nd communication: synthesis and pharmacology of sopromidine, a potent and stereoselective isomer of the achiral H2-agonist impromidine
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
Elz, Sigurd,Gerhard, Guenter,Schunack, Walter
p. 259 - 262
(2007/10/02)
Structure-activity relationships of histamine analogues, XX: absolute configuration and histamine-like activity of the enantiomeric alpha-methylhistamines
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Gerhard,Schunack
p. 709 - 714
(2007/10/02)
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