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Research ArticleCELLULAR AND MOLECULAR

Rabbit α2-Adrenoceptors: Both Platelets and Adipocytes Have α2A-Pharmacology

Diane P. Naselsky, Daryl Ashton, Robert R. Ruffolo Jr. and J. Paul Hieble
Journal of Pharmacology and Experimental Therapeutics July 2001, 298 (1) 219-225;
Diane P. Naselsky
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Daryl Ashton
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Robert R. Ruffolo Jr.
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J. Paul Hieble
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Abstract

The recombinant α2-adrenoceptors, designated as α2a and α2d, have highly similar amino acid sequences, but distinct pharmacological properties. It has been suggested that these two receptor subtypes are species orthologs, since the α2-adrenoceptors of a given species have pharmacological characteristics corresponding to either the α2a- (human, pig) or α2d- (rat, mouse, guinea pig, cow) adrenoceptor. Radioligand binding assays in rabbit adipocyte suggest α2D-adrenoceptor pharmacology. However, functional studies examining prejunctional α2-adrenoceptors in several tissues pharmacologically define the receptor of the rabbit as an α2A-adrenoceptor rather than an α2D-adrenoceptor. We characterized the α2-adrenoceptor of rabbit adipocyte and platelet, comparing the ability of norepinephrine and 13 adrenoceptor antagonists to inhibit the binding of [3H]RX821002 with the affinity of these drugs for the human α2a-adrenoceptor or the rat α2d-adrenoceptor. Pharmacological characteristics of the adipocyte and platelet receptor were very similar, with an excellent correlation between pKi values (r2 = 0.95, slope of regression = 1.01). Drug affinities for both platelet and adipocyte receptors correlated better with the α2a-adrenoceptor (r2 = 0.68–0.77) than with the α2d-adrenoceptor (r2 = 0.37–0.38). Despite the relatively low affinity of the rabbit adipocyte α2-adrenoceptor for yohimbine and rauwolscine, this receptor, as well as the platelet receptor, have α2A-adrenoceptor pharmacology. Subtle differences in the α2-adrenoceptor binding characteristics of these native rabbit tissues compared with the recombinant human α2a-adrenoceptor may result either from minor differences in the sequence of human and rabbit α2a-adrenoceptors or from differences in the environment to which native and recombinant receptors are exposed.

Footnotes

  • ↵1 Current address: Wyeth-Ayerst Research, P.O. Box 42528, Philadelphia, PA 19101.

  • Abbreviations:
    RX 821002
    2-(2-methoxy-1,4-benzodioxan-2-yl)-2-imidazoline
    WB 4101
    2-(2,6-dimethoxyphenoxyethyl)aminomethyl-1,4-benzodioxane
    BAM 1303
    1-(2-bromo-6-methylergolin-8b-ylmethyl)-2-phenylimidazole
    ARC 239
    2-(4-(2-methoxyphenyl)-piperazine-1-yl)ethyl-4,4-dimethyl-1,3-(2H,4H)-isoquinolindione
    SK&F 104078
    6-chloro-9-[(3-methyl-2-butenyl)oxy]-3-methyl-1,2,3,4-tetrahydro-1H-3-benzazepine
    • Received December 27, 2000.
    • Accepted March 18, 2001.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 298 (1)
Journal of Pharmacology and Experimental Therapeutics
Vol. 298, Issue 1
1 Jul 2001
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Research ArticleCELLULAR AND MOLECULAR

Rabbit α2-Adrenoceptors: Both Platelets and Adipocytes Have α2A-Pharmacology

Diane P. Naselsky, Daryl Ashton, Robert R. Ruffolo and J. Paul Hieble
Journal of Pharmacology and Experimental Therapeutics July 1, 2001, 298 (1) 219-225;

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Research ArticleCELLULAR AND MOLECULAR

Rabbit α2-Adrenoceptors: Both Platelets and Adipocytes Have α2A-Pharmacology

Diane P. Naselsky, Daryl Ashton, Robert R. Ruffolo and J. Paul Hieble
Journal of Pharmacology and Experimental Therapeutics July 1, 2001, 298 (1) 219-225;
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