Impromidine (SK&F 92676) is a very potent and specific agonist for histamine H2 receptors

PREVIOUSLY described selective agonists for histamine H 2 receptors are 4-methylhistamine 1 , related congeners 2–6 and dimaprit 7 ; these compounds are generally less potent than histamine. We have now found that N -[3-(imidazol-4-yl)-propyl]- N′ -{2-[(5-methylimidazol-4-yl) methylthio]ethyl}-guani...

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Veröffentlicht in:	Nature (London) 1978-11, Vol.276 (5686), p.403-405
Hauptverfasser:	DURANT, G. J., DUNCAN, W. A. M., GANELLIN, C. R., PARSONS, M. E., BLAKEMORE, R. C., RASMUSSEN, A. C.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Blood Pressure - drug effects Dogs Gastric Juice - metabolism Guanidines - pharmacology Guinea Pigs Heart Rate - drug effects Humanities and Social Sciences Imidazoles - pharmacology letter multidisciplinary Receptors, Histamine - drug effects Receptors, Histamine H2 - drug effects Science Science (multidisciplinary) Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	PREVIOUSLY described selective agonists for histamine H 2 receptors are 4-methylhistamine 1 , related congeners 2–6 and dimaprit 7 ; these compounds are generally less potent than histamine. We have now found that N -[3-(imidazol-4-yl)-propyl]- N′ -{2-[(5-methylimidazol-4-yl) methylthio]ethyl}-guanidine (impromidine, SK&F 92676 (I)) is extremely potent as an H 2 -receptor agonist and briefly report its properties here.
ISSN:	0028-0836 1476-4687
DOI:	10.1038/276403a0