| 词条 | MTEP |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 424696647 | IUPAC_name = 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine | image = Mtep.png | alt = Skeletal formula | width = 200 | image2 = MTEP-3D-spacefill.png | alt2 = Space-filling model | tradename = | pregnancy_AU = | pregnancy_US = | legal_AU = | legal_CA = | legal_UK = | legal_US = | IUPHAR_ligand = 3336 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 329205-68-7 | PubChem = 9794218 | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 7969985 | C=11 | H=8 | N=2 | S=1 | molecular_weight = 200.260 g/mol | smiles = CC1=NC(=CS1)C#CC2=CN=CC=C2 | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C11H8N2S/c1-9-13-11(8-14-9)5-4-10-3-2-6-12-7-10/h2-3,6-8H,1H3 | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = NRBNGHCYDWUVLC-UHFFFAOYSA-N }}3-((2-Methyl-4-thiazolyl)ethynyl)pyridine (MTEP) is a research drug that was developed by Merck & Co. as a selective allosteric antagonist of the metabotropic glutamate receptor subtype mGluR5. Identified through structure-activity relationship studies on an older mGluR5 antagonist MPEP,[1] MTEP has subsequently itself acted as a lead compound for newer and even more improved drugs.[2][3] MTEP is both more potent and more selective than MPEP as a mGluR5 antagonist,[4] and produces similar neuroprotective,[5][6][7] antidepressant,[8][9][10][11] analgesic,[12][13] and anxiolytic effects but with either similar or higher efficacy depending on the test used.[14][15][16][17] MTEP also has similar efficacy to MPEP in reducing the symptoms of morphine withdrawal,[18][19][20] and has anti-addictive effects in a variety of animal models, both reducing ethanol self-administration,[21][22][23][24] and also decreasing the addictive effects of nicotine, cocaine and methamphetamine.[25][26][27][28][29] See also
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A. | last14 = Reggiani | first14 = A. | last15 = Bertorelli | first15 = R. | title = The antinociceptive and anxiolytic-like effects of the metabotropic glutamate receptor 5 (mGluR5) antagonists, MPEP and MTEP, and the mGluR1 antagonist, LY456236, in rodents: A comparison of efficacy and side-effect profiles | journal = Psychopharmacology | volume = 179 | issue = 1 | pages = 207–217 | year = 2005 | pmid = 15682298| pmc = }} 14. ^{{Cite journal | last1 = Klodzinska | first1 = A. | last2 = Tatarczyńska | first2 = E. | last3 = Chojnacka-Wójcik | first3 = E. | last4 = Nowak | first4 = G. | last5 = Cosford | first5 = N. D. P. | last6 = Pilc | first6 = A. | doi = 10.1016/j.neuropharm.2004.04.013 | title = Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABAA signaling | journal = Neuropharmacology | volume = 47 | issue = 3 | pages = 342–350 | year = 2004 | pmid = 15275823| pmc = }} 15. ^{{Cite journal | last1 = Busse | first1 = C. 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J. Pharmacol. |volume=558 |issue=1–3 |pages=113–8 |date=March 2007 |pmid=17222405 |doi=10.1016/j.ejphar.2006.11.067 |url=}} 21. ^{{cite journal |vauthors=Cowen MS, Djouma E, Lawrence AJ |title=The metabotropic glutamate 5 receptor antagonist 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-pyridine reduces ethanol self-administration in multiple strains of alcohol-preferring rats and regulates olfactory glutamatergic systems |journal=J. Pharmacol. Exp. Ther. |volume=315 |issue=2 |pages=590–600 |date=November 2005 |pmid=16014750 |doi=10.1124/jpet.105.090449 |url=}} 22. ^{{cite journal |vauthors=Cowen MS, Krstew E, Lawrence AJ |title=Assessing appetitive and consummatory phases of ethanol self-administration in C57BL/6J mice under operant conditions: regulation by mGlu5 receptor antagonism |journal=Psychopharmacology |volume=190 |issue=1 |pages=21–9 |date=January 2007 |pmid=17096086 |doi=10.1007/s00213-006-0583-0 |url=}} 23. ^{{cite journal |vauthors=Adams CL, Cowen MS, Short JL, Lawrence AJ |title=Combined antagonism of glutamate mGlu5 and adenosine A2A receptors interact to regulate alcohol-seeking in rats |journal=Int. J. Neuropsychopharmacol. |volume=11 |issue=2 |pages=229–41 |date=March 2008 |pmid=17517168 |doi=10.1017/S1461145707007845 |url=}} 24. ^{{cite journal |vauthors=Kotlinska J, Bochenski M |title=The influence of various glutamate receptors antagonists on anxiety-like effect of ethanol withdrawal in a plus-maze test in rats |journal=Eur. J. Pharmacol. |volume=598 |issue=1–3 |pages=57–63 |date=November 2008 |pmid=18838071 |doi=10.1016/j.ejphar.2008.09.026 |url=}} 25. ^{{cite journal |vauthors=Dravolina OA, Danysz W, Bespalov AY |title=Effects of group I metabotropic glutamate receptor antagonists on the behavioral sensitization to motor effects of cocaine in rats |journal=Psychopharmacology |volume=187 |issue=4 |pages=397–404 |date=September 2006 |pmid=16896963 |doi=10.1007/s00213-006-0440-1 |url=}} 26. ^{{cite journal |vauthors=Palmatier MI, Liu X, Donny EC, Caggiula AR, Sved AF |title=Metabotropic glutamate 5 receptor (mGluR5) antagonists decrease nicotine seeking, but do not affect the reinforcement enhancing effects of nicotine |journal=Neuropsychopharmacology |volume=33 |issue=9 |pages=2139–47 |date=August 2008 |pmid=18046312 |doi=10.1038/sj.npp.1301623 |url= |pmc=2812904}} 27. ^{{cite journal |vauthors=Gass JT, Osborne MP, Watson NL, Brown JL, Olive MF |title=mGluR5 antagonism attenuates methamphetamine reinforcement and prevents reinstatement of methamphetamine-seeking behavior in rats |journal=Neuropsychopharmacology |volume=34 |issue=4 |pages=820–33 |date=March 2009 |pmid=18800068 |pmc=2669746 |doi=10.1038/npp.2008.140 |url=}} 28. ^{{cite journal |vauthors=Osborne MP, Olive MF |title=A role for mGluR5 receptors in intravenous methamphetamine self-administration |journal=Ann. N. Y. Acad. Sci. |volume=1139 |issue= |pages=206–11 |date=October 2008 |pmid=18991866 |doi=10.1196/annals.1432.034 |url=}} 29. ^{{cite journal |vauthors=Martin-Fardon R, Baptista MA, Dayas CV, Weiss F |title=Dissociation of the effects of MTEP [3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]piperidine] on conditioned reinstatement and reinforcement: comparison between cocaine and a conventional reinforcer |journal=J. Pharmacol. Exp. Ther. |volume=329 |issue=3 |pages=1084–90 |date=June 2009 |pmid=19258516 |doi=10.1124/jpet.109.151357 |url= |pmc=2683783}} 4 : Thiazoles|Pyridines|Alkynes|MGlu5 receptor antagonists |
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