Characterization of binding sites of a new neurotensin receptor antagonist, [3H]SR 142948A, in the rat brain

European Journal of Pharmacology
C BetancurD Pélaprat

Abstract

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]SR 142948A in brain membrane homogenates was specific, time-dependent, reversible and saturable. [3H]SR 142948A bound to an apparently homogeneous population of sites, with a Kd of 3.5 nM and a Bmax value of 508 fmol/mg of protein, which was 80% higher than that observed in saturation experiments with [3H]neurotensin. [3H]SR 142948A binding was inhibited by SR 142948A, the related nonpeptide receptor antagonist, SR 48692 (2-[[1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)-1H-pyrazole -3-carbonyl]amino]-adamantane-2-carboxylic acid) and neurotensin. Saturation and competition studies in the presence or absence of the histamine H1 receptor antagonist, levocabastine, revealed that [3H]SR 142948A bound with similar affinities to both the levocabastine-insensitive neurotensin NT1 receptors (20% of the total binding population) and the recent...Continue Reading

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Citations

Oct 18, 2000·Regulatory Peptides·B M Tyler-McMahonE Richelson
Feb 26, 2013·Chemical Reviews·Lukas WankaPeter R Schreiner
Jan 5, 2016·The Journal of Organic Chemistry·Piotr SzcześniakSebastian Stecko
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Aug 27, 2005·The Psychiatric Clinics of North America·Paul FredricksonElliott Richelson

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