Abstract
1 When the isolated thoracic aorta of the rabbit was contracted with prostaglandin F2alpha, 5-alkylpicolinic acids produced dose-dependent relaxations. 2 Picolinic acid, 2,5-pyridinedicarboxylic acid and 5-acetylpicolinic acid which do not have the 5-alkyl residue failed to relax blood vessels. 3 The vascular relaxation was dependent on the number of carbon atoms in the 5-alkyl compounds. 4 Relaxations which occurred with 5-alkylpicolinic acids were not affected by pretreatment with either propranolol or atropine. 5 It is concluded that the 5-alkyl residue is necessary for the vascular relaxation with 5-alkylpicolinic acid and that it was not produced by stimulation of beta-adrenoceptors or cholinoceptors but rather through an activation of the basic process.
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Selected References
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- Buckner C. K., Saini R. K. On the use of functional antagonism to estimate dissociation constants for beta adrenergic receptor agonists in isolated guinea-pig trachea. J Pharmacol Exp Ther. 1975 Sep;194(3):565–574. [PubMed] [Google Scholar]
- FURCHGOTT R. F., BHADRAKOM S. Reactions of strips of rabbit aorta to epinephrine, isopropylarterenol, sodium nitrite and other drugs. J Pharmacol Exp Ther. 1953 Jun;108(2):129–143. [PubMed] [Google Scholar]
- Hidaka H., Asano M. Relaxation of isolated rabbit arteries by fusaric (5-butylpicolinic) acid. J Pharmacol Exp Ther. 1976 Dec;199(3):620–629. [PubMed] [Google Scholar]
- Hidaka H., Hara F., Harada N., Hashizume Y., Yano M. Selective inhibition of dopamine-beta-hydroxylase in the peripheral tissues by 5-dimethyldithiocarbamylpicolinic acid; its effect on stress-induced ulcer, ethanol-induced sleep and blood pressure. J Pharmacol Exp Ther. 1974 Dec;191(3):384–392. [PubMed] [Google Scholar]
- Hidaka H., Nagasaka A., Takeda A. Fusaric (5-butylpicolinic) acid: its effect on plasma growth hormone. J Clin Endocrinol Metab. 1973 Jul;37(1):145–147. doi: 10.1210/jcem-37-1-145. [DOI] [PubMed] [Google Scholar]
- Hidaka H., Nagatsu T., Takeya K., Takeuchi T., Suda H. Fusaric acid, a hypotensive agent produced by fungi. J Antibiot (Tokyo) 1969 May;22(5):228–230. doi: 10.7164/antibiotics.22.228. [DOI] [PubMed] [Google Scholar]
- Hidaka H., Shoka F., Hashizume Y., Takemoto N., Yamamoto M. Inhibition of dopamine beta-hydroxylase in blood vessels by picolinic acid derivatives in vivo and their anthypertensive effects. Jpn J Pharmacol. 1975 Oct;25(5):515–524. doi: 10.1254/jjp.25.515. [DOI] [PubMed] [Google Scholar]
- Hidaka H., Takeya K. Blood pressure decreased by halobutylpicolinic acid, an inhibitor of dopamine beta-hydroxylase. Nature. 1972 Oct 6;239(5371):334–335. doi: 10.1038/239334a0. [DOI] [PubMed] [Google Scholar]
- Suda H., Takeuchi T., Nagatsu T., Matsuzaki M., Matsumoto I., Umezawa H. Inhibition of dopamine beta-hydroxylase by 5-alkylpicolinic acid and their hypotensive effects. Chem Pharm Bull (Tokyo) 1969 Nov;17(11):2377–2380. doi: 10.1248/cpb.17.2377. [DOI] [PubMed] [Google Scholar]
- Terasawa F., Kameyama M. The clinical trial of a new hypotensive agent, "fusaric acid (5-butylpicolinic acid)": the preliminary report. Jpn Circ J. 1971 Mar;35(3):339–357. doi: 10.1253/jcj.35.339. [DOI] [PubMed] [Google Scholar]
- Toda N. The action of vasodilating drugs on isolated basilar, coronary and mesenteric arteries of the dog. J Pharmacol Exp Ther. 1974 Oct;191(1):139–146. [PubMed] [Google Scholar]
- VAN ROSSUM J. M. Cumulative dose-response curves. II. Technique for the making of dose-response curves in isolated organs and the evaluation of drug parameters. Arch Int Pharmacodyn Ther. 1963;143:299–330. [PubMed] [Google Scholar]
