The nonpeptide neurotensin antagonist, SR 48692, used as a tool to reveal putative neurotensin receptor subtypes
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چکیده
منابع مشابه
Dose-dependent pain-facilitatory and -inhibitory actions of neurotensin are revealed by SR 48692, a nonpeptide neurotensin antagonist: influence on the antinociceptive effect of morphine.
Neurotensin has bipolar (facilitatory and inhibitory) effects on pain modulation that may physiologically exist in homeostasis. Facilitation predominates at low (picomolar) doses of neurotensin injected into the rostroventral medial medulla (RVM), whereas higher doses (nanomolar) produce antinociception. SR 48692, a neurotensin receptor antagonist, discriminates between receptors mediating thes...
متن کاملA neurotensin antagonist, SR 48692, inhibits colonic responses to immobilization stress in rats.
We previously reported that short-term immobilization stress of rats causes increased colonic mucin release, goblet cell depletion, prostaglandin E2 secretion, and colonic mast cell activation, as well as increased colonic motility. The purpose of this study was to investigate whether neurotensin (NT), a peptide expressed in both brain and digestive tract, participates in these responses. Rats ...
متن کاملRegulation of the neurotensin NT(1) receptor in the developing rat brain following chronic treatment with the antagonist SR 48692.
The aim of the present study was to investigate the role of neurotensin in the regulation of NT(1) receptors during postnatal development in the rat brain. Characterization of the ontogeny of neurotensin concentration and [(125)I]neurotensin binding to NT(1) receptors in the brain at different embryonic and postnatal stages showed that neurotensin was highly expressed at birth, reaching peak le...
متن کاملBiochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist.
SR 142948A, 2-[[5-(2,6-dimethoxyphenyl)-1-(4-(N-(3-dimethylaminopropyl)-N-methylc arbamoyl)-2-isopropylphenyl)-1H-pyrazole3-carbonyl]amino] adamantane-2-carboxylic acid, hydrochloride, a new and extremely potent neurotensin (NT) receptor antagonist, has been characterized in comparison with SR 48692. This selective compound possesses nanomolar affinities for NT receptors, recognizes the two bin...
متن کاملCharacterization of binding sites of a new neurotensin receptor antagonist, [3H]SR 142948A, in the rat brain.
The present study describes the characterization of the binding properties and autoradiographic distribution of a new nonpeptide antagonist of neurotensin receptors, [3H]SR 142948A (2-[[5-(2,6-dimethoxyphenyl)-1-(4-(N-(3-dimethylaminopropyl)-N-methyl carbamoyl)-2-isopropylphenyl)-1H-pyrazole-3-carbonyl]-amino]-ad amantane-2-carboxylic acid, hydrochloride), in the rat brain. The binding of [3H]S...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 1994
ISSN: 0007-1188
DOI: 10.1111/j.1476-5381.1994.tb13077.x