Baclofen activates two distinct receptors in the rat spinal cord and guinea pig ileum

J. Sawynok

doi:10.1016/0028-3908(86)90098-5

Baclofen activates two distinct receptors in the rat spinal cord and guinea pig ileum

J. Sawynok

Medicine

Résultat de recherche: Article › examen par les pairs

24 Citations (Scopus)

Résumé

Following intrathecal injection, pretreatment with both D-baclofen and 5-aminovaleric acid (5-AV) inhibited the antlnociceptive effect of L-baclofen, but homotaurlne (3-aminopropane sulphonic acid, APS) was Inactive as an antagonist (rank order D-baclofen > 5-AV > APS=0). In an established GABA_B system, the electrically stimulated guinea pig longitudinal muscle myenteric plexus preparation, APS and 5-AV but not D-baelofen reduced the inhibitory effect of L-baclofen (APS=5-AV > D-baclofen=0). Receptors with which baclofen interacts in the spinal cord to produce antinociception differ from GABA_B receptors with respect to the rank order of potency of antagonists as well as close structural analogs, and these criteria could be used for characterization of such receptors.

Langue d'origine	English
Pages (de-à)	795-798
Nombre de pages	4
Journal	Neuropharmacology
Volume	25
Numéro de publication	7
DOI	https://doi.org/10.1016/0028-3908(86)90098-5
Statut de publication	Published - juill. 1986

Note bibliographique

Funding Information:
I am particularly grateful to Drs. Gagneaux and Bencze at Ciba Geigy, Base1 for their continued supplies of Land D-baclofen and the provision of a repurified form of D-baclofen. I wish to thank C. Dickson and A. Reid for technical assistance in the intrathecal experiments. This work was supported by the MRC of Canada.

ASJC Scopus Subject Areas

Pharmacology
Cellular and Molecular Neuroscience

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10.1016/0028-3908(86)90098-5

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title = "Baclofen activates two distinct receptors in the rat spinal cord and guinea pig ileum",

abstract = "Following intrathecal injection, pretreatment with both D-baclofen and 5-aminovaleric acid (5-AV) inhibited the antlnociceptive effect of L-baclofen, but homotaurlne (3-aminopropane sulphonic acid, APS) was Inactive as an antagonist (rank order D-baclofen > 5-AV > APS=0). In an established GABAB system, the electrically stimulated guinea pig longitudinal muscle myenteric plexus preparation, APS and 5-AV but not D-baelofen reduced the inhibitory effect of L-baclofen (APS=5-AV > D-baclofen=0). Receptors with which baclofen interacts in the spinal cord to produce antinociception differ from GABAB receptors with respect to the rank order of potency of antagonists as well as close structural analogs, and these criteria could be used for characterization of such receptors.",

author = "J. Sawynok",

note = "Funding Information: I am particularly grateful to Drs. Gagneaux and Bencze at Ciba Geigy, Base1 for their continued supplies of Land D-baclofen and the provision of a repurified form of D-baclofen. I wish to thank C. Dickson and A. Reid for technical assistance in the intrathecal experiments. This work was supported by the MRC of Canada.",

year = "1986",

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doi = "10.1016/0028-3908(86)90098-5",

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PY - 1986/7

Y1 - 1986/7

N2 - Following intrathecal injection, pretreatment with both D-baclofen and 5-aminovaleric acid (5-AV) inhibited the antlnociceptive effect of L-baclofen, but homotaurlne (3-aminopropane sulphonic acid, APS) was Inactive as an antagonist (rank order D-baclofen > 5-AV > APS=0). In an established GABAB system, the electrically stimulated guinea pig longitudinal muscle myenteric plexus preparation, APS and 5-AV but not D-baelofen reduced the inhibitory effect of L-baclofen (APS=5-AV > D-baclofen=0). Receptors with which baclofen interacts in the spinal cord to produce antinociception differ from GABAB receptors with respect to the rank order of potency of antagonists as well as close structural analogs, and these criteria could be used for characterization of such receptors.

AB - Following intrathecal injection, pretreatment with both D-baclofen and 5-aminovaleric acid (5-AV) inhibited the antlnociceptive effect of L-baclofen, but homotaurlne (3-aminopropane sulphonic acid, APS) was Inactive as an antagonist (rank order D-baclofen > 5-AV > APS=0). In an established GABAB system, the electrically stimulated guinea pig longitudinal muscle myenteric plexus preparation, APS and 5-AV but not D-baelofen reduced the inhibitory effect of L-baclofen (APS=5-AV > D-baclofen=0). Receptors with which baclofen interacts in the spinal cord to produce antinociception differ from GABAB receptors with respect to the rank order of potency of antagonists as well as close structural analogs, and these criteria could be used for characterization of such receptors.

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Baclofen activates two distinct receptors in the rat spinal cord and guinea pig ileum

Résumé

Note bibliographique

ASJC Scopus Subject Areas

Accès au document

Autres fichiers et liens

Empreinte numérique

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