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. 1988 Oct;95(2):473–484. doi: 10.1111/j.1476-5381.1988.tb11668.x

An examination of the postjunctional alpha-adrenoceptor subtypes for (-)-noradrenaline in several isolated blood vessels from the rabbit.

C J Daly 1, J C McGrath 1, V G Wilson 1
PMCID: PMC1854181  PMID: 2852522

Abstract

1. Postjunctional alpha-adrenoceptors in several isolated blood vessels from the rabbit have been characterized on the basis of the relative potency of the agonists noradrenaline (NA, non-selective), phenylephrine (alpha 1-selective) and UK-14304 (alpha 2-selective), and the potency of antagonists rauwolscine (alpha 2-selective) and corynanthine (alpha 1-selective) against contractions elicited by NA. In addition, the potency of prazosin against NA was also assessed in the venous preparations. 2. The thoracic aorta, ear artery and left renal vein appear to possess alpha 1-adrenoceptors since the agonist potency order was NA greater than phenylephrine greater than UK-14304, while corynanthine was 3-10 fold more potent than rauwolscine. 3. The ear vein appears to possess alpha 2-adrenoceptors. The rank order of agonist potency was UK-14304 greater than NA much greater than phenylephrine and all three agonists elicited responses of similar magnitude. Furthermore, rauwolscine was 30 fold more potent than corynanthine while prazosin failed to produce a concentration-dependent inhibition. 4. The saphenous vein and the plantaris vein appear to possess a mixture of both subtypes since the rank order of agonist potency was UK-14304 greater than NA much greater than phenylephrine, while responses elicited by UK-14304 were smaller than those to the other agonists. However, although rauwolscine was 20 to 100 fold more potent than corynanthine in both preparations, suggestive of predominantly alpha 2-adrenoceptors, prazosin was either potent (saphenous vein) or relatively inactive (plantaris vein). 5. The characteristics of postjunctional alpha 1- and alpha 2-adrenoceptors on isolated blood vessels from the rabbit are discussed in relation to the value of both the agonists, particularly NA, and the antagonists used in this study.

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Selected References

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  1. ARUNLAKSHANA O., SCHILD H. O. Some quantitative uses of drug antagonists. Br J Pharmacol Chemother. 1959 Mar;14(1):48–58. doi: 10.1111/j.1476-5381.1959.tb00928.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Agrawal D. K., Triggle C. R., Daniel E. E. Pharmacological characterization of the postsynaptic alpha adrenoceptors in vascular smooth muscle from canine and rat mesenteric vascular beds. J Pharmacol Exp Ther. 1984 Jun;229(3):831–838. [PubMed] [Google Scholar]
  3. Bentley S. M., Drew G. M., Whiting S. B. Evidence for two distinct types of postsynaptic alpha-adrenoceptor [proceedings]. Br J Pharmacol. 1977 Sep;61(1):116P–117P. [PMC free article] [PubMed] [Google Scholar]
  4. Bou J., Massingham R. Effect of diltiazem upon contractile responses to phenylephrine, cirazoline, Sgd 101/75, St 587 and B-HT 920 in rabbit aorta and dog saphenous vein preparations. Eur J Pharmacol. 1986 Mar 4;121(3):319–325. doi: 10.1016/0014-2999(86)90252-9. [DOI] [PubMed] [Google Scholar]
  5. Bousquet P., Feldman J., Schwartz J. Central cardiovascular effects of alpha adrenergic drugs: differences between catecholamines and imidazolines. J Pharmacol Exp Ther. 1984 Jul;230(1):232–236. [PubMed] [Google Scholar]
  6. Cambridge D. UK-14,304, a potent and selective alpha2-agonist for the characterisation of alpha-adrenoceptor subtypes. Eur J Pharmacol. 1981 Jul 10;72(4):413–415. doi: 10.1016/0014-2999(81)90588-4. [DOI] [PubMed] [Google Scholar]
  7. Chiu A. T., McCall D. E., Thoolen M. J., Timmermans P. B. Ca++ utilization in the constriction of rat aorta to full and partial alpha-1 adrenoceptor agonists. J Pharmacol Exp Ther. 1986 Jul;238(1):224–231. [PubMed] [Google Scholar]
  8. Coates J., Weetman D. F. Occurrence of alpha 1s-adrenoceptors in the mouse but not in the rabbit isolated anococcygeus preparations. Br J Pharmacol. 1983 Jan;78(1):117–122. doi: 10.1111/j.1476-5381.1983.tb09370.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Daly C. J., McGrath J. C., Wilson V. G. Evidence that the population of postjunctional-adrenoceptors mediating contraction of smooth muscle in the rabbit isolated ear vein is predominantly alpha 2. Br J Pharmacol. 1988 Aug;94(4):1085–1090. doi: 10.1111/j.1476-5381.1988.tb11626.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. Daly C. J., McGrath J. C., Wilson V. G. Pharmacological analysis of postjunctional alpha-adrenoceptors mediating contractions to (-)-noradrenaline in the rabbit isolated lateral saphenous vein can be explained by interacting responses to simultaneous activation of alpha 1- and alpha 2-adrenoceptors. Br J Pharmacol. 1988 Oct;95(2):485–500. doi: 10.1111/j.1476-5381.1988.tb11669.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Docherty J. R., Constantine J. W., Starke K. Smooth muscle of rabbit aorta contains alpha 1-but not alpha 2-adrenoceptors. Naunyn Schmiedebergs Arch Pharmacol. 1981 Aug;317(1):5–7. doi: 10.1007/BF00506248. [DOI] [PubMed] [Google Scholar]
  12. Doxey J. C., Lane A. C., Roach A. G., Virdee N. K. Comparison of the alpha-adrenoceptor antagonist profiles of idazoxan (RX 781094), yohimbine, rauwolscine and corynanthine. Naunyn Schmiedebergs Arch Pharmacol. 1984 Feb;325(2):136–144. doi: 10.1007/BF00506193. [DOI] [PubMed] [Google Scholar]
  13. Drew G. M., Whiting S. B. Evidence for two distinct types of postsynaptic alpha-adrenoceptor in vascular smooth muscle in vivo. Br J Pharmacol. 1979 Oct;67(2):207–215. doi: 10.1111/j.1476-5381.1979.tb08668.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Flavahan N. A., McGrath J. C. Blockage by yohimbine of prazosin-resistant pressor effects of adrenaline in the pithed rat. Br J Pharmacol. 1980 Jul;69(3):355–357. doi: 10.1111/j.1476-5381.1980.tb07021.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. Flavahan N. A., Rimele T. J., Cooke J. P., Vanhoutte P. M. Characterization of postjunctional alpha-1 and alpha-2 adrenoceptors activated by exogenous or nerve-released norepinephrine in the canine saphenous vein. J Pharmacol Exp Ther. 1984 Sep;230(3):699–705. [PubMed] [Google Scholar]
  16. Flavahan N. A., Vanhoutte P. M. Effect of cooling on alpha-1 and alpha-2 adrenergic responses in canine saphenous and femoral veins. J Pharmacol Exp Ther. 1986 Jul;238(1):139–147. [PubMed] [Google Scholar]
  17. Fuder H., Nelson W. L., Miller D. D., Patil P. N. Alpha adrenoreceptors of rabbit aorta and stomach fundus. J Pharmacol Exp Ther. 1981 Apr;217(1):1–9. [PubMed] [Google Scholar]
  18. Guimarães S., Paiva M. Q. Two distinct adrenoceptor-biophases in the vasculature: one for alpha- and the other for beta-agonists. Naunyn Schmiedebergs Arch Pharmacol. 1981 Jun;316(3):195–199. doi: 10.1007/BF00505649. [DOI] [PubMed] [Google Scholar]
  19. Henseling M. Kinetic constants for uptake and metabolism of 3H-(-)noradrenaline in rabbit aorta. Possible falsification of the constants by diffusion barriers within the vessel wall. Naunyn Schmiedebergs Arch Pharmacol. 1983 Jun;323(1):12–23. doi: 10.1007/BF00498822. [DOI] [PubMed] [Google Scholar]
  20. Hieble J. P., Sarau H. M., Foley J. J., Demarinis R. M., Pendleton R. G. Comparison of central and peripheral alpha 1-adrenoceptors. Naunyn Schmiedebergs Arch Pharmacol. 1982 Mar;318(4):267–273. doi: 10.1007/BF00501164. [DOI] [PubMed] [Google Scholar]
  21. Holck M. I., Jones C. H., Haeusler G. Differential interactions of clonidine and methoxamine with the postsynaptic alpha-adrenoceptor of rabbit main pulmonary artery. J Cardiovasc Pharmacol. 1983 Mar-Apr;5(2):240–248. doi: 10.1097/00005344-198303000-00013. [DOI] [PubMed] [Google Scholar]
  22. Honda K., Takenaka T., Miyata-Osawa A., Terai M., Shiono K. Studies on YM-12617: a selective and potent antagonist of postsynaptic alpha 1-adrenoceptors. Naunyn Schmiedebergs Arch Pharmacol. 1985 Jan;328(3):264–272. doi: 10.1007/BF00515552. [DOI] [PubMed] [Google Scholar]
  23. Hooker C. S., Calkins P. J., Fleisch J. H. On the measurement of vascular and respiratory smooth muscle responses in vitro. Blood Vessels. 1977;14(1):1–11. doi: 10.1159/000158110. [DOI] [PubMed] [Google Scholar]
  24. Johnson S. M., de la Lande I. S. Action of deoxycorticosterone acetate on the central artery of the rabbit ear. Blood Vessels. 1978;15(4):231–246. doi: 10.1159/000158169. [DOI] [PubMed] [Google Scholar]
  25. McGrath J. C. Alpha-adrenoceptor antagonism by apoyohimbine and some observations on the pharmacology of alpha-adrenoceptors in the rat anococcygeus and vas deferens. Br J Pharmacol. 1984 Aug;82(4):769–781. doi: 10.1111/j.1476-5381.1984.tb16473.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  26. McGrath J. C. Evidence for more than one type of post-junctional alpha-adrenoceptor. Biochem Pharmacol. 1982 Feb 15;31(4):467–484. doi: 10.1016/0006-2952(82)90147-2. [DOI] [PubMed] [Google Scholar]
  27. Medgett I. C., Langer S. Z. Heterogeneity of smooth muscle alpha adrenoceptors in rat tail artery in vitro. J Pharmacol Exp Ther. 1984 Jun;229(3):823–830. [PubMed] [Google Scholar]
  28. Purdy R. E., Ashbrook D. W., Stupecky G. L., Watanabe M. Y. Qualitative and quantitative differences between the postsynaptic alpha adrenoceptors of rabbit ear artery and thoracic aorta. J Pharmacol Exp Ther. 1983 Mar;224(3):543–551. [PubMed] [Google Scholar]
  29. Purdy R. E., Krueger C. G., Young S. Evidence for nonclassical alpha adrenoceptor blockade by prazosin in isolated rabbit blood vessels. Life Sci. 1980 Dec 8;27(23):2187–2195. doi: 10.1016/0024-3205(80)90383-5. [DOI] [PubMed] [Google Scholar]
  30. Ruffolo R. R., Jr, Rosing E. L., Waddell J. E. Receptor interactions of imidazolines. I. Affinity and efficacy for alpha adrenergic receptors in rat aorta. J Pharmacol Exp Ther. 1979 Jun;209(3):429–436. [PubMed] [Google Scholar]
  31. Schulz J. C., Westfall D. P. A pharmacological analysis of the alpha-adrenoceptor antagonism by prazosin in arteries and veins. Blood Vessels. 1982;19(2):79–87. doi: 10.1159/000158375. [DOI] [PubMed] [Google Scholar]
  32. Schümann H. J., Lues I. Postjunctional alpha-adrenoceptors in the isolated saphenous vein of the rabbit. Characterization and influence of angiotensin. Naunyn Schmiedebergs Arch Pharmacol. 1983 Aug;323(4):328–334. doi: 10.1007/BF00512471. [DOI] [PubMed] [Google Scholar]
  33. Shoji T., Tsuru H., Shigei T. A regional difference in the distribution of postsynaptic alpha-adrenoceptor subtypes in canine veins. Naunyn Schmiedebergs Arch Pharmacol. 1983 Dec;324(4):246–255. doi: 10.1007/BF00502619. [DOI] [PubMed] [Google Scholar]
  34. 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]
  35. Weiss R. J., Webb R. C., Smith C. B. Alpha-2 adrenoreceptors on arterial smooth muscle: selective labeling by [3H]clonidine. J Pharmacol Exp Ther. 1983 Jun;225(3):599–605. [PubMed] [Google Scholar]
  36. 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 Aug;308(2):127–136. doi: 10.1007/BF00499054. [DOI] [PubMed] [Google Scholar]
  37. Wilffert B., Timmermans P. B., van Zwieten P. A. Extrasynaptic location of alpha-2 and noninnervated beta-2 adrenoceptors in the vascular system of the pithed normotensive rat. J Pharmacol Exp Ther. 1982 Jun;221(3):762–768. [PubMed] [Google Scholar]

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