Assessment of Alpha-adrenergic Receptor Subtypes in Isolated Rat Aortic Segments

Overview

Journal Naunyn Schmiedebergs Arch Pharmacol

Specialty Pharmacology

Date 1984 Apr 1

PMID 6145102

Citations 9

Authors

R A Macia

W D Matthews

J Lafferty

R M DeMarinis

Affiliations

Soon will be listed here.

Abstract

The postsynaptic alpha-adrenoceptors in the isolated rat aorta have been characterized according to the sensitivity of the tissue to selective alpha 1- and alpha 2-adrenoceptor agonists and antagonists. The potency (-log EC50) order of the non-selective alpha-agonist norepinephrine and relatively selective agonists was as follows: norepinephrine (alpha 1 = alpha 2; 7.30); clonidine (alpha 2 greater than alpha 1; 7.01); phenylephrine (alpha 1 greater than alpha 2; 6.99), SK & F 89748--A (alpha 1 greater than alpha 2; 6.65); BHT-920 (alpha 2 much greater than alpha 1; 5.56) and M-7 (alpha 2 greater than alpha 1; 4.66). The isolated rat aorta was 12-200-fold more sensitive to the alpha 1-adrenoceptor agonists phenylephrine and SK & F 89748-A, than to the alpha 2-agonists, BHT-920 and M-7. Prazosin is 245-1259-fold more potent than rauwolscine as an antagonist of contractions induced by various alpha 1- and alpha 2-agonists in the rat aorta. These data indicate that constriction of the smooth muscle of the rat aorta to alpha-adrenergic agonists is mediated through alpha 1- but not alpha 2-adrenoceptors.

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References

Madjar H, Docherty J, Starke K . An examination of pre- and postsynaptic alpha-adrenoceptors in the autoperfused rabbit hindlimb. J Cardiovasc Pharmacol. 1980; 2(5):619-27. DOI: 10.1097/00005344-198009000-00011. View

Docherty J, Starke K . Postsynaptic alpha-adrenoceptor subtypes in rabbit blood vessels and rat anococcygeus muscle studied in vitro. J Cardiovasc Pharmacol. 1981; 3(4):854-66. DOI: 10.1097/00005344-198107000-00019. View

Drew G . Postsynaptic alpha 2-adrenoceptors mediate pressor responses to 2-N,N-dimethylamino-5,6-dihydroxy-1,2,3,4-tetrahydronaphthalene (M-7). Eur J Pharmacol. 1980; 65(1):85-7. DOI: 10.1016/0014-2999(80)90212-5. View

Timmermans P, van Zwieten P . Mini-review. The postsynaptic alpha 2-adrenoreceptor. J Auton Pharmacol. 1981; 1(2):171-83. DOI: 10.1111/j.1474-8673.1981.tb00509.x. View

KOBINGER W, Pichler L . Investigation into different types of post- and presynaptic alpha-adrenoceptors at cardiovascular sites in rats. Eur J Pharmacol. 1980; 65(4):393-402. DOI: 10.1016/0014-2999(80)90343-x. View

Weitzell R, Tanaka T, Starke K . Pre- and postsynaptic effects of yohimbine stereoisomers on noradrenergic transmission in the pulmonary artery of the rabbit. Naunyn Schmiedebergs Arch Pharmacol. 1979; 308(2):127-36. DOI: 10.1007/BF00499054. View

Ruffolo Jr R, Waddell J, Yaden E . Postsynaptic alpha adrenergic receptor subtypes differentiated by yohimbine in tissues from the rat. Existence of alpha-2 adrenergic receptors in rat aorta. J Pharmacol Exp Ther. 1981; 217(2):235-40. View

Docherty J, McGrath J . A comparison of pre- and post-junctional potencies of several alpha-adrenoceptor agonists in the cardiovascular system and anococcygeus muscle of the rat. Evidence for two types of post-junctional alpha-adrenoceptor. Naunyn Schmiedebergs Arch Pharmacol. 1980; 312(2):107-16. DOI: 10.1007/BF00569718. View

ARUNLAKSHANA O, SCHILD H . Some quantitative uses of drug antagonists. Br J Pharmacol Chemother. 1959; 14(1):48-58. PMC: 1481829. DOI: 10.1111/j.1476-5381.1959.tb00928.x. View

10.

DeMarinis R, Hieble J . l-1,2,3,4-Tetrahydro-8-methoxy-5-(methylthio)-2-naphthalenamine: a potent and selective agonist at alpha 1-adrenoceptors. J Med Chem. 1983; 26(9):1215-8. DOI: 10.1021/jm00363a002. View

11.

Randriantsoa A, Heitz C, STOCLET J . Functional characterization of postjunctional alpha-adrenoceptors in rat aorta. Eur J Pharmacol. 1981; 75(1):57-60. DOI: 10.1016/0014-2999(81)90345-9. View

12.

Timmermans P, Kwa H, van Zwieten P . Possible subdivision of postsynaptic alpha-adrenoceptors mediating pressor responses in the pithed rat. Naunyn Schmiedebergs Arch Pharmacol. 1979; 310(2):189-93. DOI: 10.1007/BF00500284. View

13.

Patil P, Fudge K, JACOBOWITZ D . Steric aspects of adrenergic drugs. 18. -Adrenergic receptors of mammalian aorta. Eur J Pharmacol. 1972; 19(1):79-87. DOI: 10.1016/0014-2999(72)90079-9. View

14.

Yamaguchi I, Kopin I . Differential inhibiton of alpha-1 and alpha-2 adrenoceptor-mediated pressor responses in pithed rats. J Pharmacol Exp Ther. 1980; 214(2):275-81. View

15.

Hieble J, Pendleton R . Effects of ring substitution on the pre- and postjunctional alpha-adrenergic activity of aryliminoimidazolidines. Naunyn Schmiedebergs Arch Pharmacol. 1979; 309(3):217-24. DOI: 10.1007/BF00504753. View

16.

Ruffolo Jr R, Waddell J, Yaden E . Heterogeneity of postsynaptic Alpha adrenergic receptors in mammalian aortas. J Pharmacol Exp Ther. 1982; 221(2):309-14. View

17.

Langer S, Shepperson N . Postjunctional alpha 1-adrenoceptors: preferential innervation of alpha 1-adrenoceptors and the role of neuronal uptake. J Cardiovasc Pharmacol. 1982; 4 Suppl 1:S8-13. View

18.

Hicks P, Cannon J . NN-Dialkyl derivatives of 2-amino-5,6-dihydroxy-1,2,3,4-tetrahydronaphthalene as selective agonists at presynaptic alpha-adrenoceptors in the rat. J Pharm Pharmacol. 1979; 31(7):494-6. DOI: 10.1111/j.2042-7158.1979.tb13569.x. View

19.

Langer S, Massingham R, Shepperson N . Presence of postsynaptic alpha 2-adrenoreceptors of predominantly extrasynaptic location in the vascular smooth muscle of the dog hind limb. Clin Sci (Lond). 1980; 59 Suppl 6:225s-228s. DOI: 10.1042/cs059225s. View

20.

Skarby T, Andersson K, Edvinsson L . Pharmacological characterization of postjunctional alpha-adrenoceptors in isolated feline cerebral and peripheral arteries. Acta Physiol Scand. 1983; 117(1):63-73. DOI: 10.1111/j.1748-1716.1983.tb07179.x. View