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. 1992 Jun;106(2):447–451. doi: 10.1111/j.1476-5381.1992.tb14354.x

Investigations of the subtype of alpha 2-adrenoceptor mediating contractions of the human saphenous vein.

K Smith 1, S Connaughton 1, J R Docherty 1
PMCID: PMC1907513  PMID: 1356563

Abstract

1. We have examined the effects of a series of alpha 2-adrenoceptor antagonists against isometric contractions to noradrenaline in human saphenous vein, and correlated these potencies with affinities for the alpha 2A-ligand binding site of human platelet and the alpha 2B-ligand binding site of rat kidney. 2. The alpha 2B-selective adrenoceptor antagonists, prazosin, ARC 239 and HV 723 showed high, and the alpha 2A-selective antagonist BRL 44408 showed low, potency in human saphenous vein. 3. Potency in human saphenous vein correlated better with affinity for the alpha 2B-ligand binding site (r = 0.71, n = 12, P less than 0.01) than with affinity for the alpha 2A-ligand binding site (r = 0.56, n = 12, non significant). 4. It is concluded that the postjunctional alpha 2-adrenoceptor of human saphenous vein resembles an alpha 2B-ligand binding site more than an alpha 2A-ligand binding site.

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Selected References

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  1. Borton M., Connaughton S., Docherty J. R. Actions of 8-hydroxy-2-(N-dipropylamino) tetralin (8-OH-DPAT) at alpha 2-adrenoceptors. J Auton Pharmacol. 1991 Aug;11(4):247–253. doi: 10.1111/j.1474-8673.1991.tb00322.x. [DOI] [PubMed] [Google Scholar]
  2. Bylund D. B., Ray-Prenger C., Murphy T. J. Alpha-2A and alpha-2B adrenergic receptor subtypes: antagonist binding in tissues and cell lines containing only one subtype. J Pharmacol Exp Ther. 1988 May;245(2):600–607. [PubMed] [Google Scholar]
  3. Connaughton S., Docherty J. R. Functional evidence for heterogeneity of peripheral prejunctional alpha 2-adrenoceptors. Br J Pharmacol. 1990 Oct;101(2):285–290. doi: 10.1111/j.1476-5381.1990.tb12702.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Connaughton S., Docherty J. R. No evidence for differences between pre- and postjunctional alpha 2-adrenoceptors in the periphery. Br J Pharmacol. 1990 Jan;99(1):97–102. doi: 10.1111/j.1476-5381.1990.tb14660.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Crist J., Surprenant A. Evidence that 8-hydroxy-2-(n-dipropylamino)tetralin (8-OH-DPAT) is a selective alpha 2-adrenoceptor antagonist on guinea-pig submucous neurones. Br J Pharmacol. 1987 Oct;92(2):341–347. doi: 10.1111/j.1476-5381.1987.tb11329.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Docherty J. R., Starke K. Postsynaptic alpha-adrenoceptor subtypes in rabbit blood vessels and rat anococcygeus muscle studied in vitro. J Cardiovasc Pharmacol. 1981 Jul-Aug;3(4):854–866. doi: 10.1097/00005344-198107000-00019. [DOI] [PubMed] [Google Scholar]
  7. Flordellis C. S., Handy D. E., Bresnahan M. R., Zannis V. I., Gavras H. Cloning and expression of a rat brain alpha 2B-adrenergic receptor. Proc Natl Acad Sci U S A. 1991 Feb 1;88(3):1019–1023. doi: 10.1073/pnas.88.3.1019. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Gobbi M., Frittoli E., Mennini T. The modulation of [3H]noradrenaline and [3H]serotonin release from rat brain synaptosomes is not mediated by the alpha 2B-adrenoceptor subtype. Naunyn Schmiedebergs Arch Pharmacol. 1990 Oct;342(4):382–386. doi: 10.1007/BF00169453. [DOI] [PubMed] [Google Scholar]
  9. Harsing L. G., Jr, Vizi E. S. Evidence that two stereochemically different alpha-2 adrenoceptors modulate norepinephrine release in rat cerebral cortex. J Pharmacol Exp Ther. 1991 Jan;256(1):44–49. [PubMed] [Google Scholar]
  10. Hicks P. E., Barras M., Herman G., Mauduit P., Armstrong J. M., Rossignol B. Alpha-adrenoceptor subtypes in dog saphenous vein that mediate contraction and inositol phosphate production. Br J Pharmacol. 1991 Jan;102(1):151–161. doi: 10.1111/j.1476-5381.1991.tb12146.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Kapocsi J., Somogyi G. T., Ludvig N., Serfozo P., Harsing L. G., Jr, Woods R. J., Vizi E. S. Neurochemical evidence for two types of presynaptic alpha 2-adrenoceptors. Neurochem Res. 1987 Feb;12(2):141–147. doi: 10.1007/BF00979530. [DOI] [PubMed] [Google Scholar]
  12. Limberger N., Späth L., Starke K. Subclassification of the presynaptic alpha 2-autoreceptors in rabbit brain cortex. Br J Pharmacol. 1991 May;103(1):1251–1255. doi: 10.1111/j.1476-5381.1991.tb12332.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  13. Lorenz W., Lomasney J. W., Collins S., Regan J. W., Caron M. G., Lefkowitz R. J. Expression of three alpha 2-adrenergic receptor subtypes in rat tissues: implications for alpha 2 receptor classification. Mol Pharmacol. 1990 Nov;38(5):599–603. [PubMed] [Google Scholar]
  14. Michel A. D., Loury D. N., Whiting R. L. Differences between the alpha 2-adrenoceptor in rat submaxillary gland and the alpha 2A-and alpha 2B-adrenoceptor subtypes. Br J Pharmacol. 1989 Nov;98(3):890–897. doi: 10.1111/j.1476-5381.1989.tb14618.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. Muramatsu I., Ohmura T., Kigoshi S., Hashimoto S., Oshita M. Pharmacological subclassification of alpha 1-adrenoceptors in vascular smooth muscle. Br J Pharmacol. 1990 Jan;99(1):197–201. doi: 10.1111/j.1476-5381.1990.tb14678.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  16. Neylon C. B., Summers R. J. [3H]-rauwolscine binding to alpha 2-adrenoceptors in the mammalian kidney: apparent receptor heterogeneity between species. Br J Pharmacol. 1985 Jun;85(2):349–359. doi: 10.1111/j.1476-5381.1985.tb08868.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  17. Niddam R., Angel I., Bidet S., Langer S. Z. Pharmacological characterization of alpha-2 adrenergic receptor subtype involved in the release of insulin from isolated rat pancreatic islets. J Pharmacol Exp Ther. 1990 Sep;254(3):883–887. [PubMed] [Google Scholar]
  18. Regan J. W., Kobilka T. S., Yang-Feng T. L., Caron M. G., Lefkowitz R. J., Kobilka B. K. Cloning and expression of a human kidney cDNA for an alpha 2-adrenergic receptor subtype. Proc Natl Acad Sci U S A. 1988 Sep;85(17):6301–6305. doi: 10.1073/pnas.85.17.6301. [DOI] [PMC free article] [PubMed] [Google Scholar]
  19. Simonneaux V., Ebadi M., Bylund D. B. Identification and characterization of alpha 2D-adrenergic receptors in bovine pineal gland. Mol Pharmacol. 1991 Aug;40(2):235–241. [PubMed] [Google Scholar]
  20. Uhlén S., Wikberg J. E. Delineation of three pharmacological subtypes of alpha 2-adrenoceptor in the rat kidney. Br J Pharmacol. 1991 Nov;104(3):657–664. doi: 10.1111/j.1476-5381.1991.tb12485.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  21. Vizi E. S., Harsing L. G., Jr, Gaal J., Kapocsi J., Bernath S., Somogyi G. T. CH-38083, a selective, potent antagonist of alpha-2 adrenoceptors. J Pharmacol Exp Ther. 1986 Aug;238(2):701–706. [PubMed] [Google Scholar]
  22. Young P., Berge J., Chapman H., Cawthorne M. A. Novel alpha 2-adrenoceptor antagonists show selectivity for alpha 2A- and alpha 2B-adrenoceptor subtypes. Eur J Pharmacol. 1989 Sep 22;168(3):381–386. doi: 10.1016/0014-2999(89)90801-7. [DOI] [PubMed] [Google Scholar]

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