| 词条 | Meclinertant |
| 释义 |
| verifiedrevid = 451220237 | IUPAC_name = 2-([1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazole-3-carbonyl]amino)admantane-2-carboxylic acid | image = SR-48692_structure.png | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 146362-70-1 | ATC_prefix = | ATC_suffix = | ChEMBL = 506981 | PubChem = 119192 | IUPHAR_ligand = 1582 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 5JBP4SI96H | C=32 | H=31 | Cl=1 | N=4 | O=5 | molecular_weight = 587.064 | smiles = c7cc3c(cc7Cl)nccc3-n4nc(cc4-c1c(OC)cccc1OC)C(=O)NC2(C(O)=O)C5CC(C6)CC2CC6C5 }}Meclinertant (SR-48692) is a drug which acts as a selective, non-peptide antagonist at the neurotensin receptor NTS1, and was the first non-peptide antagonist developed for this receptor.[1][2] It is used in scientific research to explore the interaction between neurotensin and other neurotransmitters in the brain,[3][4][5][6][7][8] and produces anxiolytic, anti-addictive and memory-impairing effects in animal studies.[9][10][11][12] References1. ^{{cite journal |vauthors=Gully D, Canton M, Boigegrain R, Jeanjean F, Molimard JC, Poncelet M, Gueudet C, Heaulme M, Leyris R, Brouard A |title=Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor |journal=Proceedings of the National Academy of Sciences of the United States of America |volume=90 |issue=1 |pages=65–9 |date=January 1993 |pmid=8380498 |pmc=45600 |doi= 10.1073/pnas.90.1.65|url=}} 2. ^{{cite journal |vauthors=Gully D, Jeanjean F, Poncelet M, Steinberg R, Soubrié P, Le Fur G, Maffrand JP |title=Neuropharmacological profile of non-peptide neurotensin antagonists |journal=Fundamental & Clinical Pharmacology |volume=9 |issue=6 |pages=513–21 |year=1995 |pmid=8808171 |doi= 10.1111/j.1472-8206.1995.tb00528.x|url=}} 3. ^{{cite journal |vauthors=Rostene W, Azzi M, Boudin H, Lepee I, Souaze F, Mendez-Ubach M, Betancur C, Gully D |title=Use of nonpeptide antagonists to explore the physiological roles of neurotensin. Focus on brain neurotensin/dopamine interactions |journal=Annals of the New York Academy of Sciences |volume=814 |issue= |pages=125–41 |date=April 1997 |pmid=9160965 |doi= 10.1111/j.1749-6632.1997.tb46151.x|url=}} 4. ^{{cite journal |vauthors=Jolas T, Aghajanian GK |title=Neurotensin and the serotonergic system |journal=Progress in Neurobiology |volume=52 |issue=6 |pages=455–68 |date=August 1997 |pmid=9316156 |doi= 10.1016/S0301-0082(97)00025-7|url=}} 5. ^{{cite journal |vauthors=Dobner PR, Deutch AY, Fadel J |title=Neurotensin: dual roles in psychostimulant and antipsychotic drug responses |journal=Life Sciences |volume=73 |issue=6 |pages=801–11 |date=June 2003 |pmid=12801600 |doi= 10.1016/S0024-3205(03)00411-9|url=}} 6. ^{{cite journal |vauthors=Chen L, Yung KK, Yung WH |title=Neurotensin selectively facilitates glutamatergic transmission in globus pallidus |journal=Neuroscience |volume=141 |issue=4 |pages=1871–8 |date=September 2006 |pmid=16814931 |doi=10.1016/j.neuroscience.2006.05.049 |url=}} 7. ^{{cite journal |vauthors=Petkova-Kirova P, Rakovska A, Della Corte L, Zaekova G, Radomirov R, Mayer A |title=Neurotensin modulation of acetylcholine, GABA, and aspartate release from rat prefrontal cortex studied in vivo with microdialysis |journal=Brain Research Bulletin |volume=77 |issue=2–3 |pages=129–35 |date=September 2008 |pmid=18721670 |doi=10.1016/j.brainresbull.2008.04.003 |url=}} 8. ^{{cite journal |vauthors=Petkova-Kirova P, Rakovska A, Zaekova G, Ballini C, Corte LD, Radomirov R, Vágvölgyi A |title=Stimulation by neurotensin of dopamine and 5-hydroxytryptamine (5-HT) release from rat prefrontal cortex: possible role of NTR1 receptors in neuropsychiatric disorders |journal=Neurochemistry International |volume=53 |issue=6–8 |pages=355–61 |date=December 2008 |pmid=18835308 |doi=10.1016/j.neuint.2008.08.010 |url=}} 9. ^{{cite journal |vauthors=Griebel G, Moindrot N, Aliaga C, Simiand J, Soubrié P |title=Characterization of the profile of neurokinin-2 and neurotensin receptor antagonists in the mouse defense test battery |journal=Neuroscience and Biobehavioral Reviews |volume=25 |issue=7–8 |pages=619–26 |date=December 2001 |pmid=11801287 |doi= 10.1016/S0149-7634(01)00045-8|url=}} 10. ^{{cite journal |vauthors=Tirado-Santiago G, Lázaro-Muñoz G, Rodríguez-González V, Maldonado-Vlaar CS |title=Microinfusions of neurotensin antagonist SR 48692 within the nucleus accumbens core impair spatial learning in rats |journal=Behavioral Neuroscience |volume=120 |issue=5 |pages=1093–102 |date=October 2006 |pmid=17014260 |doi=10.1037/0735-7044.120.5.1093 |url=}} 11. ^{{cite journal |vauthors=Felszeghy K, Espinosa JM, Scarna H, Bérod A, Rostène W, Pélaprat D |title=Neurotensin receptor antagonist administered during cocaine withdrawal decreases locomotor sensitization and conditioned place preference |journal=Neuropsychopharmacology |volume=32 |issue=12 |pages=2601–10 |date=December 2007 |pmid=17356568 |doi=10.1038/sj.npp.1301382 |url= |pmc=2992550}} 12. ^{{cite journal |vauthors=Lévesque K, Lamarche C, Rompré PP |title=Evidence for a role of endogenous neurotensin in the development of sensitization to the locomotor stimulant effect of morphine |journal=European Journal of Pharmacology |volume=594 |issue=1–3 |pages=132–8 |date=October 2008 |pmid=18706409 |doi=10.1016/j.ejphar.2008.07.048 |url=}} External links
5 : Adamantanes|Pyrazoles|Quinolines|Chloroarenes|Phenol ethers |
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