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Vol. 53, Issue 2, 319-356, June 2001

Vascular Adrenoceptors: An Update

Serafim Guimarães1 and Daniel Moura

Institute of Pharmacology and Therapeutics, Faculty of Medicine, Alameda Hernani Monteiro, Porto, Portugal

I. Introduction
II. Subclassification of Adrenoceptors
    A. alpha 1-Adrenoceptors
    B. alpha 2-Adrenoceptors
    C. beta -Adrenoceptors
III. Postjunctional Adrenoceptors in Vascular Smooth Muscle
    A. alpha 1-Adrenoceptors
        1. In Vitro.
        2. In Vivo.
        3. alpha 1-Adrenoceptor Antagonists in the Symptomatic Treatment of Prostatic Hypertrophy.
    B. alpha 2-Adrenoceptors
        1. In Vitro.
        2. In Vivo.
        3. Blood Pressure Regulation in alpha 2-Adrenoceptor-Deficient Mice.
    C. beta -Adrenoceptors
        1. In Vitro
            a. beta 1- and beta 2-Adrenoceptors.
            b. beta 3-Adrenoceptors.
            c. Putative beta 4-Adrenoceptors.
        2. In Vivo.
IV. Prejunctional Adrenoceptors
    A. alpha 2-Adrenoceptors
    B. beta -Adrenoceptors
V. Endothelial Adrenoceptors
    A. alpha 2-Adrenoceptors
    B. beta -Adrenoceptors
VI. Distribution of Vascular Adrenoceptors
    A. Localization in Relation to Sympathetic Nerve Terminals
    B. Distribution Upstream and Downstream
    C. Distribution in Particular Vascular Beds
VII. Influence of Maturation and Aging
    A. On alpha -Adrenoceptors
    B. On beta -Adrenoceptors
VIII. Influence of Temperature on Vascular Adrenoceptor-Mediated Responses
IX. Vascular Adrenoceptors in Some Diseases
X. Conclusions
Acknowledgments
References

The total and regional peripheral resistance and capacitance of the vascular system is regulated by the sympathetic nervous system, which influences the vasculature mainly through changes in the release of catecholamines from both the sympathetic nerve terminals and the adrenal medulla. The knowledge of the targets for noradrenaline and adrenaline, the main endogenous catecholamines mediating that influence, has recently been greatly expanded. From two types of adrenoceptors (alpha  and beta ), we have now nine subtypes (alpha 1A, alpha 1B, alpha 1D, alpha 2A/D, alpha 2B, alpha 2A/D, beta 1, beta 2, and beta 3) and two other candidates (alpha 1L and beta 4), which may be conformational states of alpha 1A and beta 1-adrenoceptors, respectively. The vascular endothelium is now known to be more than a pure anatomical entity, which smoothly contacts the blood and forms a passive barrier against plasma lipids. Instead, the endothelium is an important organ possessing at least five different adrenoceptor subtypes (alpha 2A/D, alpha 2C, beta 1, beta 2, and beta 3), which either directly or through the release of nitric oxide actively participate in the regulation of the vascular tone. The availability of transgenic models has resulted in a stepwise progression toward the identification of the role of each adrenoceptor subtype in the regulation of blood pressure and fine-tuning of blood supply to the different organs: alpha 2A/D-adrenoceptors are involved in the central control of blood pressure; alpha 1-(primarily) and alpha 2B-adrenoceptors (secondarily) contribute to the peripheral regulation of vascular tone; and alpha 2A/D- and alpha 2C-adrenoceptors modulate transmitter release. The increased knowledge on the involvement of vascular adrenoceptors in many diseases like Raynaud's, scleroderma, several neurological degenerative diseases (familial amyloidotic polyneuropathy, Parkinson disease, multiple-system atrophy), some kinds of hypertension, etc., will contribute to new and better therapeutic approaches.


1 Address for correspondence: Dr. Serafim Guimarães, Institute of Pharmacology and Therapeutics, Faculty of Medicine, Alameda Hernani Monteiro, 4200-319, Porto, Portugal. E-mail: sguimara{at}med.up.pt


0031-6997/01/5302-0319$03.00/0
PHARMACOLOGICAL REVIEWS
Copyright © 2001 by The American Society for Pharmacology and Experimental Therapeutics



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