Study of in vitro effects of hydralazine metabolites - Comparative evaluation of products of hydroxylation, hydrolysis and conjugation

A. J. McLean, P. du Souich, K. Barron, O. Carrier, K. D. Haegele, J. L. McNay

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Abstract

K + contractures were induced in paired strips of rabbit aortic smooth muscle. The relationship between relaxant effects and the bath concentration of hydralazine acetone hydrazone (HA), 4-OH-hydralazine (HH) and phthalazine (P) was studied over the concentration range 10 -5 - 10 -3 M. All compounds were active, HA = HH > P (p < 0.05; n = 6) at concentrations in the range 10 -4 - 10 -3 M, HA > HH at a concentration of 10 -3M (p > 0.01). The activity of HA did not depend on significant reconversion to hydralazine (H) in the bath (< 0.5%). A range of H derivatives may contribute to the hypotensive effects of administered H.

Original languageEnglish
Pages (from-to)19-25
Number of pages7
JournalArchives Internationales de Pharmacodynamie et de Therapie
Volume235
Issue number1
StatePublished - 1 Dec 1978

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Hydralazine
Hydroxylation
Hydrolysis
Hydrazones
Baths
Contracture
Smooth Muscle
Rabbits
In Vitro Techniques
hydroxide ion

Cite this

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title = "Study of in vitro effects of hydralazine metabolites - Comparative evaluation of products of hydroxylation, hydrolysis and conjugation",
abstract = "K + contractures were induced in paired strips of rabbit aortic smooth muscle. The relationship between relaxant effects and the bath concentration of hydralazine acetone hydrazone (HA), 4-OH-hydralazine (HH) and phthalazine (P) was studied over the concentration range 10 -5 - 10 -3 M. All compounds were active, HA = HH > P (p < 0.05; n = 6) at concentrations in the range 10 -4 - 10 -3 M, HA > HH at a concentration of 10 -3M (p > 0.01). The activity of HA did not depend on significant reconversion to hydralazine (H) in the bath (< 0.5{\%}). A range of H derivatives may contribute to the hypotensive effects of administered H.",
author = "McLean, {A. J.} and {du Souich}, P. and K. Barron and O. Carrier and Haegele, {K. D.} and McNay, {J. L.}",
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Study of in vitro effects of hydralazine metabolites - Comparative evaluation of products of hydroxylation, hydrolysis and conjugation. / McLean, A. J.; du Souich, P.; Barron, K.; Carrier, O.; Haegele, K. D.; McNay, J. L.

In: Archives Internationales de Pharmacodynamie et de Therapie, Vol. 235, No. 1, 01.12.1978, p. 19-25.

Research output: Contribution to journalArticle

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T1 - Study of in vitro effects of hydralazine metabolites - Comparative evaluation of products of hydroxylation, hydrolysis and conjugation

AU - McLean, A. J.

AU - du Souich, P.

AU - Barron, K.

AU - Carrier, O.

AU - Haegele, K. D.

AU - McNay, J. L.

PY - 1978/12/1

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AB - K + contractures were induced in paired strips of rabbit aortic smooth muscle. The relationship between relaxant effects and the bath concentration of hydralazine acetone hydrazone (HA), 4-OH-hydralazine (HH) and phthalazine (P) was studied over the concentration range 10 -5 - 10 -3 M. All compounds were active, HA = HH > P (p < 0.05; n = 6) at concentrations in the range 10 -4 - 10 -3 M, HA > HH at a concentration of 10 -3M (p > 0.01). The activity of HA did not depend on significant reconversion to hydralazine (H) in the bath (< 0.5%). A range of H derivatives may contribute to the hypotensive effects of administered H.

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