Otro sistema de transmisión opioide en el cerebro de los mamíferos. Las endomorfinas y el receptor opioide mu. Parte II
Fuente:
Redalyc
Enregistré dans:
| Auteur principal: | |
|---|---|
| Format: | Artículo científico |
| Langue: | en |
| Publié: |
Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz
2000
|
| Sujets: | |
| Accès en ligne: | |
| Tags: |
Ajouter un tag
Pas de tags, Soyez le premier à ajouter un tag!
|
| _version_ | 1876478582913499136 |
|---|---|
| author | Philippe Leff |
| author_facet | Philippe Leff |
| contents | Otro sistema de transmisión opioide en el cerebro de los mamíferos. Las endomorfinas y el receptor opioide mu. Parte II Philippe Leff Rodolfo Acevedo Armando Valdés Iván Martínez Aline Morales Juan Carlos Calva Benito Antón Medicina endomorphins Opiate receptors agonists ligands endogenous opiates Several opioid peptides have been identified, cloned andsubsequently characterized by pharmacological and molecularapproaches. These peptides mediate a vast number ofbiological functions in discrete brain regions, where theyactivate the different opioid receptors subtypes referred to asmu, delta and kappa. These receptors belong to a class of Giproteincoupled membrane receptors being structurally definedby seven peptide transmembrane domains. Opiate drugsmainly mediate their analgesic, euphoric and rewarding effectsby activating the mu-opioid receptor subtype. Besides thedetailed description of the anatomical expression of each opioidreceptor subtype throughout the CNS of mammals, opioidreceptors reveal a distinct but overlapping distribution as wellas a single pharma-cological profile. Moreover, opioid receptorsactivate a similar subcellular effector system, which involvesa functional modulation of the adenylyl cyclase, protein kinases,phosphoinositide turnover as well as ion conductances suchas calcium and potassium. Pharmacological studies relatedto the structure-activity relationships of the cloned opioidreceptors expressed in heterologous cellular systems haverevealed that natural occurring opioid peptides selectively bindwith differential affinities to the different opioid receptorsubtypes. Thus, enkephalins display a preferential binding tothe deltaopioid receptor while dynorphins are considered theselective endogenous ligands for the kappa-opioid receptor.Furthermore, no endogenous peptide agonist ligandsdisplaying high affinity binding for the m opioid receptor subtypehave been identified. Recently, two novel endogenous opioidpeptides referred to as endomorphins were isolated and clonedfrom the CNS of mammals. The pharmacological and functional properties of these two peptides have just begun. In line withthese investigations, initial studies have shown thatendomorphins display the highest affinity binding for the muopioid receptor reported to date as well as a very potent andprolonged analgesic activity in rodents. 2000 artículo científico 0185-3325 https://www.redalyc.org/articulo.oa?id=58222306 en http://www.redalyc.org/revista.oa?id=582 Salud Mental application/pdf Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz Salud Mental (México) Num.2 Vol.23 |
| format | Artículo científico |
| id | redalyc_58222306 |
| institution | Redalyc |
| language | en |
| publishDate | 2000 |
| publisher | Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz |
| spellingShingle | Otro sistema de transmisión opioide en el cerebro de los mamíferos. Las endomorfinas y el receptor opioide mu. Parte II Philippe Leff Medicina endomorphins Opiate receptors agonists ligands endogenous opiates Otro sistema de transmisión opioide en el cerebro de los mamíferos. Las endomorfinas y el receptor opioide mu. Parte II Philippe Leff Rodolfo Acevedo Armando Valdés Iván Martínez Aline Morales Juan Carlos Calva Benito Antón Medicina endomorphins Opiate receptors agonists ligands endogenous opiates Several opioid peptides have been identified, cloned andsubsequently characterized by pharmacological and molecularapproaches. These peptides mediate a vast number ofbiological functions in discrete brain regions, where theyactivate the different opioid receptors subtypes referred to asmu, delta and kappa. These receptors belong to a class of Giproteincoupled membrane receptors being structurally definedby seven peptide transmembrane domains. Opiate drugsmainly mediate their analgesic, euphoric and rewarding effectsby activating the mu-opioid receptor subtype. Besides thedetailed description of the anatomical expression of each opioidreceptor subtype throughout the CNS of mammals, opioidreceptors reveal a distinct but overlapping distribution as wellas a single pharma-cological profile. Moreover, opioid receptorsactivate a similar subcellular effector system, which involvesa functional modulation of the adenylyl cyclase, protein kinases,phosphoinositide turnover as well as ion conductances suchas calcium and potassium. Pharmacological studies relatedto the structure-activity relationships of the cloned opioidreceptors expressed in heterologous cellular systems haverevealed that natural occurring opioid peptides selectively bindwith differential affinities to the different opioid receptorsubtypes. Thus, enkephalins display a preferential binding tothe deltaopioid receptor while dynorphins are considered theselective endogenous ligands for the kappa-opioid receptor.Furthermore, no endogenous peptide agonist ligandsdisplaying high affinity binding for the m opioid receptor subtypehave been identified. Recently, two novel endogenous opioidpeptides referred to as endomorphins were isolated and clonedfrom the CNS of mammals. The pharmacological and functional properties of these two peptides have just begun. In line withthese investigations, initial studies have shown thatendomorphins display the highest affinity binding for the muopioid receptor reported to date as well as a very potent andprolonged analgesic activity in rodents. 2000 artículo científico 0185-3325 https://www.redalyc.org/articulo.oa?id=58222306 en http://www.redalyc.org/revista.oa?id=582 Salud Mental application/pdf Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz Salud Mental (México) Num.2 Vol.23 |
| title | Otro sistema de transmisión opioide en el cerebro de los mamíferos. Las endomorfinas y el receptor opioide mu. Parte II |
| topic | Medicina endomorphins Opiate receptors agonists ligands endogenous opiates |
| url | https://www.redalyc.org/articulo.oa?id=58222306 |