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J Med Chem ; 26(2): 214-7, 1983 Feb.
Article in English | MEDLINE | ID: mdl-6827538

ABSTRACT

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.


Subject(s)
Antihypertensive Agents , Cannabinoids/chemical synthesis , Animals , Blood Pressure/drug effects , Cannabinoids/pharmacology , Heart Rate/drug effects , Hypertension/physiopathology , Indicators and Reagents , Magnetic Resonance Spectroscopy , Rats , Structure-Activity Relationship
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