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. 1993 May;109(1):80–87. doi: 10.1111/j.1476-5381.1993.tb13534.x

Investigation of the subtypes of alpha 1-adrenoceptor mediating contractions of rat aorta, vas deferens and spleen.

R Aboud 1, M Shafii 1, J R Docherty 1
PMCID: PMC2175602  PMID: 8098642

Abstract

1. The subtypes of alpha 1-adrenoceptor mediating contractions to exogenous noradrenaline (NA) or phenylephrine in rat vas deferens, spleen and aorta, and mediating contractions to endogenous NA in rat vas deferens have been examined. 2. In rat vas deferens, the competitive antagonists prazosin, WB 4101, benoxathian and 5-methyl-urapidil inhibited contractions to NA with pA2 values of 9.26, 9.54, 9.02 and 8.43, respectively. The irreversible antagonist chloroethylclonidine (CEC) (100 microM) failed to affect contractions to NA. 3. In rat vas deferens in the presence of nifedipine (10 microM), contractions to NA were significantly attenuated and under these conditions, CEC (100 microM) significantly reduced the maximum response to NA. 4. In rat spleen, the competitive antagonists prazosin, WB 4101 and benoxathian inhibited contractions to phenylephrine with pA2 values of 9.56, 8.85 and 7.60, respectively, and 5-methyl-urapidil had a KB of 6.62. CEC (100 microM) significantly reduced the maximum contraction to phenylephrine. 5. In rat aorta, the competitive antagonists, prazosin, WB 4101, benoxathian and 5-methyl-urapidil inhibited contractions to NA with pA2 values of 9.45, 9.21, 8.55 and 8.12, respectively. CEC (100 microM) produced an approximately parallel shift in the potency of NA, without significantly reducing the maximum response. 6. In epididymal portions of rat vas deferens in the presence of nifedipine (10 microM), the isometric contraction to a single electrical pulse was significantly reduced by CEC (100 microM), and by the competitive antagonists prazosin, WB 4101, benoxathian and 5-methyl-urapidil at concentrations of 1 nM.(ABSTRACT TRUNCATED AT 250 WORDS)

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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. Brown D. A., Docherty J. R., French A. M., MacDonald A., McGrath J. C., Scott N. C. Separation of adrenergic and non-adrenergic contractions to field stimulation in the rat vas deferens. Br J Pharmacol. 1983 Jun;79(2):379–393. doi: 10.1111/j.1476-5381.1983.tb11010.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Cotecchia S., Schwinn D. A., Randall R. R., Lefkowitz R. J., Caron M. G., Kobilka B. K. Molecular cloning and expression of the cDNA for the hamster alpha 1-adrenergic receptor. Proc Natl Acad Sci U S A. 1988 Oct;85(19):7159–7163. doi: 10.1073/pnas.85.19.7159. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Docherty J. R. The pharmacology of alpha 1- and alpha 2-adrenoceptors: evidence for and against a further subdivision. Pharmacol Ther. 1989;44(2):241–284. doi: 10.1016/0163-7258(89)90067-3. [DOI] [PubMed] [Google Scholar]
  5. Gross G., Hanft G., Rugevics C. 5-Methyl-urapidil discriminates between subtypes of the alpha 1-adrenoceptor. Eur J Pharmacol. 1988 Jul 7;151(2):333–335. doi: 10.1016/0014-2999(88)90819-9. [DOI] [PubMed] [Google Scholar]
  6. Han C., Abel P. W., Minneman K. P. Alpha 1-adrenoceptor subtypes linked to different mechanisms for increasing intracellular Ca2+ in smooth muscle. Nature. 1987 Sep 24;329(6137):333–335. doi: 10.1038/329333a0. [DOI] [PubMed] [Google Scholar]
  7. Han C., Li J., Minneman K. P. Subtypes of alpha 1-adrenoceptors in rat blood vessels. Eur J Pharmacol. 1990 Nov 6;190(1-2):97–104. doi: 10.1016/0014-2999(90)94116-f. [DOI] [PubMed] [Google Scholar]
  8. Hanft G., Gross G. Subclassification of alpha 1-adrenoceptor recognition sites by urapidil derivatives and other selective antagonists. Br J Pharmacol. 1989 Jul;97(3):691–700. doi: 10.1111/j.1476-5381.1989.tb12005.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Kenakin T. P., Novak P. J. Classification of phenoxybenzamine/prazosin-resistant contractions of rat spleen to norepinephrine by Schild analysis: similarities and differences to postsynaptic alpha-2 adrenoceptors. J Pharmacol Exp Ther. 1988 Jan;244(1):206–212. [PubMed] [Google Scholar]
  10. Lomasney J. W., Cotecchia S., Lorenz W., Leung W. Y., Schwinn D. A., Yang-Feng T. L., Brownstein M., Lefkowitz R. J., Caron M. G. Molecular cloning and expression of the cDNA for the alpha 1A-adrenergic receptor. The gene for which is located on human chromosome 5. J Biol Chem. 1991 Apr 5;266(10):6365–6369. [PubMed] [Google Scholar]
  11. Mallard N. J., Marshall R. W., Sithers A. J., Spriggs T. L. Separation of putative alpha 1A- and alpha 1B-adrenoceptor mediated components in the tension response of the rat vas deferens to electrical field stimulation. Br J Pharmacol. 1992 Mar;105(3):727–731. doi: 10.1111/j.1476-5381.1992.tb09046.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Martinotti E., Breschi M. C., Nieri P., Omini C. Differences in activity between noradrenaline and other alpha-agonists in rat vas deferens. J Auton Pharmacol. 1991 Jun;11(3):147–153. doi: 10.1111/j.1474-8673.1991.tb00314.x. [DOI] [PubMed] [Google Scholar]
  13. Morrow A. L., Creese I. Characterization of alpha 1-adrenergic receptor subtypes in rat brain: a reevaluation of [3H]WB4104 and [3H]prazosin binding. Mol Pharmacol. 1986 Apr;29(4):321–330. [PubMed] [Google Scholar]
  14. Muramatsu I., Kigoshi S., Ohmura T. Subtypes of alpha 1-adrenoceptors involved in noradrenaline-induced contractions of rat thoracic aorta and dog carotid artery. Jpn J Pharmacol. 1991 Dec;57(4):535–544. doi: 10.1254/jjp.57.535. [DOI] [PubMed] [Google Scholar]
  15. Oriowo M. A., Ruffolo R. R., Jr Heterogeneity of postjunctional alpha 1-adrenoceptors in mammalian aortae: subclassification based on chlorethylclonidine, WB 4101 and nifedipine. J Vasc Res. 1992 Jan-Feb;29(1):33–40. doi: 10.1159/000158929. [DOI] [PubMed] [Google Scholar]
  16. Perez D. M., Piascik M. T., Graham R. M. Solution-phase library screening for the identification of rare clones: isolation of an alpha 1D-adrenergic receptor cDNA. Mol Pharmacol. 1991 Dec;40(6):876–883. [PubMed] [Google Scholar]
  17. Piascik M. T., Sparks M. S., Pruitt T. A., Soltis E. E. Evidence for a complex interaction between the subtypes of the alpha 1-adrenoceptor. Eur J Pharmacol. 1991 Jul 9;199(3):279–289. doi: 10.1016/0014-2999(91)90491-8. [DOI] [PubMed] [Google Scholar]
  18. Schwinn D. A., Lomasney J. W., Lorenz W., Szklut P. J., Fremeau R. T., Jr, Yang-Feng T. L., Caron M. G., Lefkowitz R. J., Cotecchia S. Molecular cloning and expression of the cDNA for a novel alpha 1-adrenergic receptor subtype. J Biol Chem. 1990 May 15;265(14):8183–8189. [PubMed] [Google Scholar]
  19. Tian W. N., Gupta S., Deth R. C. Species differences in chlorethylclonidine antagonism at vascular alpha-1 adrenergic receptors. J Pharmacol Exp Ther. 1990 May;253(2):877–883. [PubMed] [Google Scholar]
  20. Voigt M. M., Kispert J., Chin H. M. Sequence of a rat brain cDNA encoding an alpha-1B adrenergic receptor. Nucleic Acids Res. 1990 Feb 25;18(4):1053–1053. doi: 10.1093/nar/18.4.1053. [DOI] [PMC free article] [PubMed] [Google Scholar]

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