The imidazoline receptors and the central regulation of the arterial blood pressure: a minireview
| Autor: | Monique Dontenwill, Josiane Feldman, Eduardo Tibiriçá, Hugues Greney, Pascal Bousquet, J. Stutzmann, G. Bricca, A. Belcourt |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 1993 |
| Předmět: |
Microbiology (medical)
medicine.medical_specialty lcsh:Arctic medicine. Tropical medicine lcsh:RC955-962 Receptors Drug Population Central nervous system lcsh:QR1-502 Imidazoline receptor Blood Pressure nucleus reticularis lateralis lcsh:Microbiology Internal medicine rilmenidine medicine Animals Humans Receptor education clonidine Medulla Medulla Oblongata education.field_of_study business.industry arterial hypotension central nervous system Rilmenidine Rats Clonidine Endocrinology medicine.anatomical_structure antihypertensive drugs Locus coeruleus Imidazoline Receptors business imidazoline-preferring receptors Brain Stem medicine.drug |
| Zdroj: | Memórias do Instituto Oswaldo Cruz., Vol 88, Iss 2, Pp 317-325 (1993) Memórias do Instituto Oswaldo Cruz, Volume: 88, Issue: 2, Pages: 317-325, Published: JUN 1993 |
| ISSN: | 1678-8060 0074-0276 |
| Popis: | Recently, we proposed the hypothesis according to which 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 alpha 2-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 alpha 2-adrenergic mechanisms in the locus coeruleus, which is involved in the control of the sleep-waking cycle. The IPR may constitute an interesting target for new drugs in the treatment of arterial hypertension. Finally, dysfunctions of this modulatory system which could be involved in the pathophysiology of some forms of the hypertensive disease are under investigation. |
| Databáze: | OpenAIRE |
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