Role of imidazoline receptors in cardiovascular regulation

The involvement of nonadrenergic imidazoline specific receptors in the central control of the vasomotor tone and in the mechanism of action of drugs bearing an imidazoline structure, or analogs, is now well documented. Imidazoline-specific binding sites were found in many tissues and species. Moreov...

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Veröffentlicht in:The American journal of cardiology 1994-12, Vol.74 (13), p.A3-A6
Hauptverfasser: Dontenwill, M., Tibiriça, E., Greney, H., Bennaï, F., Feldman, J., Stutzmann, J., Bricca, G., Belcourt, A., Bousquet, P.
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container_end_page A6
container_issue 13
container_start_page A3
container_title The American journal of cardiology
container_volume 74
creator Dontenwill, M.
Tibiriça, E.
Greney, H.
Bennaï, F.
Feldman, J.
Stutzmann, J.
Bricca, G.
Belcourt, A.
Bousquet, P.
description The involvement of nonadrenergic imidazoline specific receptors in the central control of the vasomotor tone and in the mechanism of action of drugs bearing an imidazoline structure, or analogs, is now well documented. Imidazoline-specific binding sites were found in many tissues and species. Moreover, until now, it is only in the brainstem that such binding sites are associated with a function: the hyportensive effect of imidazoline-like drugs. Rilmenidine, which is an oxazoline structurally related to the reference imidazolines, exerts a central hypotensive effect of central origin involving imidazoline receptors. The selectivity of rilmenidine for the imidazoline receptors compared to α 2-adrenergic receptors could explain the low incidence of sedative side effects observed with this antihypertensive drug. A specific anti-imidazoline radioimmunoassay allowed us to detect the presence of an immunoreactive imidazoline-like substance in human sera. High levels of this immunoreactive substance are associated with high blood pressure in 20–30% of the hypertensive patients. This observation indicates that high levels of this immunoreactive substance in the serum can be associated with some kinds of primary hypertension. The cause-and-effect relation between these 2 phenomena has not yet been determined. This substance is in process of purification; it could be a candidate to be an endogenous ligand of the imidazoline receptors.
doi_str_mv 10.1016/0002-9149(94)90035-3
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ispartof The American journal of cardiology, 1994-12, Vol.74 (13), p.A3-A6
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subjects Animals
Biological and medical sciences
Brain - drug effects
Brain - metabolism
Cardiovascular disease
Cardiovascular Physiological Phenomena
Drug therapy
Fundamental and applied biological sciences. Psychology
Heart
Humans
Hypertension - blood
Imidazoles - immunology
Imidazoles - metabolism
Imidazoline Receptors
Medical research
Receptors, Drug - immunology
Receptors, Drug - physiology
Vasomotor System - metabolism
Vasomotor System - physiopathology
Vertebrates: cardiovascular system
title Role of imidazoline receptors in cardiovascular regulation
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