184162-21-8
Chemical Structure
SR 142948A
- CAS No.: 184162-21-8
- Formula:C39H52ClN5O6
- Molecular Weight:722.31
IUPAC Name: 2-(5-(2,6-dimethoxyphenyl)-1-(4-((3-(dimethylamino)propyl)(methyl)carbamoyl)-2-isopropylphenyl)-1H-pyrazole-3-carboxamido)adamantane-2-carboxylic acid hydrochloride
InChIKey: CUYNEHGBVHUQQW-UHFFFAOYSA-N
SMILES: O=C(C1(NC(C2=NN(C3=CC=C(C(N(CCCN(C)C)C)=O)C=C3C(C)C)C(C4=C(OC)C=CC=C4OC)=C2)=O)C5CC6CC(C5)CC1C6)O.Cl
Biological Activity: SR 142948A is a blood-brain barrier-permeable, orally active, selective, non-peptide Neurotensin Receptor antagonist. SR 142948A exhibits an IC50 of 4.0 nM at the NTS1 site. SR 142948A competitively antagonizes neurotensin-dependent neurotransmitter release and modulates neurotensin-related dopaminergic and serotonergic signaling, making it useful for research on neurobehavioral mechanisms associated with schizophrenia[1][2][3][4][5][6][7][8][9].
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SR 142948A | 99.0% | SR 142948A is a blood-brain barrier-permeable, orally active, selective, non-peptide Neurotensin Receptor antagonist. SR 142948A exhibits an IC50 of 4.0 nM at the NTS1 site. SR 142948A competitively antagonizes neurotensin-dependent neurotransmitter release and modulates neurotensin-related dopaminergic and serotonergic signaling, making it useful for research on neurobehavioral mechanisms associated with schizophrenia. | ||||||||||||||||||||
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References
- [1]. Betancur C, et al. Characterization of binding sites of a new neurotensin receptor antagonist, [3H]SR 142948A, in the rat brain. Eur J Pharmacol. 1998;343:67-77. [Content Brief]
- [2]. Héaulme M, et al. Stimulation by neurotensin of (3H)5-hydroxytryptamine (5HT) release from rat frontal cortex slices. Neuropeptides. 1998;32(5):465-471.
- [3]. Kinkead B, et al. Endogenous neurotensin is involved in estrous cycle related alterations in prepulse inhibition of the acoustic startle reflex in female rats. Psychoneuroendocrinology. 2008 Feb;33(2):178-87.
- [4]. Casti P, et al. Blockade of neurotensin receptors affects differently hypo-locomotion and catalepsy induced by haloperidol in mice. Neuropharmacology. 2004 Jul;47(1):128-35.
- [5]. Binder EB, et al. Effects of neurotensin receptor antagonism on latent inhibition in Sprague-Dawley rats. Psychopharmacology. 2002;161:288-295.
- [6]. Marie-Claire C, et al. Effects of the selective neurotensin antagonist SR 142948A on 3,4-methylenedioxymethamphetamine-induced behaviours in mice. Neuropharmacology. 2008 Jun;54(7):1107-11.
- [7]. Brun P, et al. Endogenous neurotensin down-regulates dopamine efflux in the nucleus accumbens as revealed by SR-142948A, a selective neurotensin receptor antagonist. Journal of neurochemistry. 2001 Jun;77(6):1542-52.
- [8]. Binder EB, et al. Neurotensin receptor antagonist SR 142948A alters Fos expression and extrapyramidal side effect profile of typical and atypical antipsychotic drugs. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2004 Dec;29(12):2200-7.
- [9]. Leonetti M, et al. The neurotensin receptor antagonist SR 142948A blocks the efflux of dopamine evoked in nucleus accumbens by neurotensin ejection into the ventral tegmental area. Naunyn-Schmiedeberg's archives of pharmacology. 2002 Jun;365(6):427-33. [Content Brief]
