Literature DB >> 2566507

Rilmenidine selectivity for imidazoline receptors in human brain.

G Bricca1, M Dontenwill, A Molines, J Feldman, E Tibirica, A Belcourt, P Bousquet.   

Abstract

The selectivity of three centrally acting antihypertensive agents for the medullary imidazoline-preferring receptors (IPR) versus cortical alpha-adrenoceptors was investigated in human brain. [3H]Clonidine binding was studied in various membrane preparations. Competition experiments were performed. Cortical membrane preparations were used as they mainly contained classical alpha-adrenoceptors whereas medullary membrane preparations from the nucleus reticularis lateralis contained only IPR insensitive to catecholamines. Rilmenidine, a new antihypertensive agent, appeared 2.5 and 3.5 times more selective than clonidine and guanfacine, respectively, for medullary IPR sites than for cortical alpha-adrenoceptors, thus providing a possible explanation for the low sedative effects of this new molecule.

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Year:  1989        PMID： 2566507     DOI： 10.1016/0014-2999(89)90210-0

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN： 0014-2999            Impact factor:   4.432


  13 in total

Review 1.  Drugs acting on imidazoline receptors: a review of their pharmacology, their use in blood pressure control and their potential interest in cardioprotection.

Authors:  P Bousquet; J Feldman
Journal:  Drugs       Date:  1999-11       Impact factor: 9.546

2.  Evidence for the involvement of imidazoline receptors in the central hypotensive effect of rilmenidine in the rabbit.

Authors:  J Feldman; E Tibiriça; G Bricca; M Dontenwill; A Belcourt; P Bousquet
Journal:  Br J Pharmacol       Date:  1990-07       Impact factor: 8.739

3.  Extracellular brain cortical levels of noradrenaline in ischemia: effects of desipramine and postischemic administration of idazoxan.

Authors:  I Gustafson; E J Westerberg; T Wieloch
Journal:  Exp Brain Res       Date:  1991       Impact factor: 1.972

4.  Dose-effect relationship of rilmenidine after chronic administration.

Authors:  R Luccioni; M Lambert; P Ambrosi; M Scemama
Journal:  Eur J Clin Pharmacol       Date:  1993       Impact factor: 2.953

5.  Central alpha-2 adrenoceptors are responsible for a clonidine-induced cue in a rat drug discrimination paradigm.

Authors:  S Jordan; H C Jackson; D J Nutt; S L Handley
Journal:  Psychopharmacology (Berl)       Date:  1993       Impact factor: 4.530

6.  Relevance of the use of [3H]-clonidine to identify imidazoline receptors in the rabbit brainstem.

Authors:  G Bricca; J Zhang; H Greney; M Dontenwill; J Stutzmann; A Belcourt; P Bousquet
Journal:  Br J Pharmacol       Date:  1993-12       Impact factor: 8.739

7.  Mediation of the hypotensive action of systemic clonidine in the rat by alpha 2-adrenoceptors.

Authors:  J P Hieble; D C Kolpak
Journal:  Br J Pharmacol       Date:  1993-12       Impact factor: 8.739

8.  Corticotropin-releasing factor in the basolateral amygdala enhances memory consolidation via an interaction with the beta-adrenoceptor-cAMP pathway: dependence on glucocorticoid receptor activation.

Authors:  Benno Roozendaal; Gustav Schelling; James L McGaugh
Journal:  J Neurosci       Date:  2008-06-25       Impact factor: 6.167

9.  Presynaptic I1-imidazoline receptors reduce GABAergic synaptic transmission in striatal medium spiny neurons.

Authors:  Mitsuo Tanabe; Yurika Kino; Motoko Honda; Hideki Ono
Journal:  J Neurosci       Date:  2006-02-08       Impact factor: 6.167

10.  Binding of [3H]clonidine to I1-imidazoline sites in bovine adrenal medullary membranes.

Authors:  G J Molderings; D Moura; K Fink; H Bönisch; M Göthert
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1993-07       Impact factor: 3.000
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