BETAHISTINE, ITS METABOLITES AND VASCULAR RESPONSES IN THE FORELIMB OF THE DOG
HERIBERT KONZETT, ROBERT G. BOST, FAYE J. BOWMAN, EDWARD R. BOWMAN and HERBERT McKENNIS JR.
Journal of Pharmacology and Experimental Therapeutics July 1971, 178 (1) 122-129;
HERIBERT KONZETT
ROBERT G. BOST
FAYE J. BOWMAN
EDWARD R. BOWMAN
HERBERT McKENNIS JR.
Betahistine, and two of its putative metabolites, 2-(2-aminoethyl) pyridine and 2-(2-hydroxyethyl) pyridine have been compared for effects (at constant blood-flow rate) on vascular resistance in the forelimb of the dog. Betahistine and its N-demethyl derivative, 2-(2-aminoethyl) pyridine, were of equal or similar potency in decreasing vascular resistance at a dose range of 0.22 to 2.2 µmol/min. In contrast, 2-(2-hydroxyethyl) pyridine at doses up to 22 µmol/min and 2-pyridylacetic acid, a urinary metabolite of betahistine in the dog, at doses up to 22 µmol/min produced no demonstrable change in vascular resistance. After p.o. administration of betahistine (15 mg/kg b.wt. for eight days) the urine of male mongrel dogs contained acidic metabolitea in amounts corresponding by spectrophotometricestimate to 45% of betahistine administered. The presence of 2-pyridylacetate in the acidic metabolic fraction was demonstrated by chemical preparation of methyl 2-pyridylacetate picrate, which was compared with an authentic sample of synthetic compound.
Accepted March 8, 1971.
© 1971, by The Williams & Wilkins Company
You are going to email the following BETAHISTINE, ITS METABOLITES AND VASCULAR RESPONSES IN THE FORELIMB OF THE DOG
HERIBERT KONZETT, ROBERT G. BOST, FAYE J. BOWMAN, EDWARD R. BOWMAN and HERBERT McKENNIS
Journal of Pharmacology and Experimental Therapeutics July 1, 1971, 178 (1) 122-129;
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