New antihypertensive cannabinoids

A number of azacannabinoids containing hydroxyacyl and aminoacetyl substituents on the nitrogen atom were synthesized. The hydroxyacetyl and gamma-hydroxybutyryl derivatives were potent antihypertensive agents (minimum effective dose, 3-5 mg/kg, orally) of the same order of activity as the highly CN...

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Veröffentlicht in:Journal of medicinal chemistry 1983-02, Vol.26 (2), p.214-217
Hauptverfasser: Zaugg, Harold E, Kyncl, Jaroslav
Format: Artikel
Sprache:eng
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Zusammenfassung:A number of azacannabinoids containing hydroxyacyl and aminoacetyl substituents on the nitrogen atom were synthesized. The hydroxyacetyl and gamma-hydroxybutyryl derivatives were potent antihypertensive agents (minimum effective dose, 3-5 mg/kg, orally) of the same order of activity as the highly CNS-active N-propargyl derivatives Ia and Ib. Furthermore, 4a showed weak stimulant properties at hypotensive dose levels, in contrast to the strongly CNS-depressant action characteristic of the N-propargyl analogues.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00356a017