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THE IMIDAZOLINE RECEPTORS AND THE CENTRAL REGULATION OF THE ARTERIAL BLOOD PRESSURE: A MINIREVIEW
Sistema nervoso central
Rilmenidina
Receptores preferidos da imidazolina
Hipotensão arterial
Núcleo reticular lateral
Medicamentos anti-hipertensivos
Rilmenidine
Imidazoline-preferring receptors
Nucleus reticularis lateralis
Arterial hypotension
Antihypertensive drugs
Central nervous system
Author
Affilliation
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Fisiologia e Farmacodinâmica. Rio de Janeiro, RJ. Brasil.
Université Louis Pasteur. Faculté de Médecine. CNRS URA 589. Laboratoire de Pharmacologie Cardiovasculaire et Rénale. Strasbourg, France.
Université Louis Pasteur. Faculté de Médecine. CNRS URA 589. Laboratoire de Pharmacologie Cardiovasculaire et Rénale. Strasbourg, France.
Université Louis Pasteur. Faculté de Médecine. CNRS URA 589. Laboratoire de Pharmacologie Cardiovasculaire et Rénale. Strasbourg, France.
Université Louis Pasteur. Faculté de Médecine. CNRS URA 589. Laboratoire de Pharmacologie Cardiovasculaire et Rénale. Strasbourg, France.
Université Louis Pasteur. Faculté de Médecine. CNRS URA 589. Laboratoire de Pharmacologie Cardiovasculaire et Rénale. Strasbourg, France.
Université Louis Pasteur. Faculté de Médecine. CNRS URA 589. Laboratoire de Pharmacologie Cardiovasculaire et Rénale. Strasbourg, France.
Université Louis Pasteur. Faculté de Médecine. CNRS URA 589. Laboratoire de Pharmacologie Cardiovasculaire et Rénale. Strasbourg, France.
Université Louis Pasteur. Faculté de Médecine. CNRS URA 589. Laboratoire de Pharmacologie Cardiovasculaire et Rénale. Strasbourg, France.
Université Louis Pasteur. Faculté de Médecine. CNRS URA 589. Laboratoire de Pharmacologie Cardiovasculaire et Rénale. Strasbourg, France.
Université Louis Pasteur. Faculté de Médecine. CNRS URA 589. Laboratoire de Pharmacologie Cardiovasculaire et Rénale. Strasbourg, France.
Université Louis Pasteur. Faculté de Médecine. CNRS URA 589. Laboratoire de Pharmacologie Cardiovasculaire et Rénale. Strasbourg, France.
Université Louis Pasteur. Faculté de Médecine. CNRS URA 589. Laboratoire de Pharmacologie Cardiovasculaire et Rénale. Strasbourg, France.
Université Louis Pasteur. Faculté de Médecine. CNRS URA 589. Laboratoire de Pharmacologie Cardiovasculaire et Rénale. Strasbourg, France.
Université Louis Pasteur. Faculté de Médecine. CNRS URA 589. Laboratoire de Pharmacologie Cardiovasculaire et Rénale. Strasbourg, France.
Abstract
Recently, we proposed the hypothesis according to wich the central hypotensive effect of clonidine and related substances could be related to an action upon specific receptors, requiring the imidazoline or imidazoline-like structures, rather than α2-adrenoceptors. Since then, direct evidences have been accumulated to confirm the existence of a population of imidazoline specific binding sites in the brainstem of animals and man, more precisely in the Nucleus Reticularis Lateralis (NRL) region of the ventrolateral medulla (VLM), site of the antihypertensive action of clonidine. The purification of the putative endogenous ligand of the imidazoline receptors - named endazoline - is currently being attempted from human brain extracts. This new concept might at last lead to the expected dissociation of the pharmacological mechanisms involved, on the one hand, in the therapeutic antihypertensive effect, and on the other, in their major side-effect, which is sedation. In fact, it has been recently confirmed that hypotension is mediated by the activation of imidazoline preferring receptors (IPR) within the NRL region, while sedation is attributed to the inhibition of α2-adrenergic mechanisms in the locus coeruleus, which is involved in the control of the sleep-waking cycle. The IPRmay constitute on interesting target for new drugs in the treatment of arterial hypertension. Finally, dysfunctions of this modulatory system which could be involved in the pathophysiologyof some forms of the hypertensive disease are under investigation.
Keywords in Portuguese
ClonidinaSistema nervoso central
Rilmenidina
Receptores preferidos da imidazolina
Hipotensão arterial
Núcleo reticular lateral
Medicamentos anti-hipertensivos
Keywords
ClonidineRilmenidine
Imidazoline-preferring receptors
Nucleus reticularis lateralis
Arterial hypotension
Antihypertensive drugs
Central nervous system
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