MTEP: Difference between revisions

Content deleted Content added
No edit summary
Line 39:
'''3-((2-Methyl-4-thiazolyl)ethynyl)pyridine''' ('''MTEP''') is a research drug that was developed by [[Merck & Co.]] as a selective [[allosteric]] [[Antagonist (pharmacology)|antagonist]] of the [[metabotropic glutamate receptor]] subtype [[Metabotropic glutamate receptor 5|mGluR5]]. Identified through [[structure-activity relationship]] studies on an older mGluR5 antagonist [[2-Methyl-6-(phenylethynyl)pyridine|MPEP]],<ref>{{cite journal |vauthors=Cosford ND, Tehrani L, Roppe J, etal |title=3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity |journal=J. Med. Chem. |volume=46 |issue=2 |pages=204–6 |date=January 2003 |pmid=12519057 |doi=10.1021/jm025570j |url=}}</ref> MTEP has subsequently itself acted as a [[lead compound]] for newer and even more improved drugs.<ref>{{cite journal |vauthors=Iso Y, Grajkowska E, Wroblewski JT, etal |title=Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications |journal=J. Med. Chem. |volume=49 |issue=3 |pages=1080–100 |date=February 2006 |pmid=16451073 |doi=10.1021/jm050570f |url=}}</ref><ref>{{cite journal |vauthors=Kulkarni SS, Newman AH |title=Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists |journal=Bioorg. Med. Chem. Lett. |volume=17 |issue=11 |pages=2987–91 |date=June 2007 |pmid=17446071 |pmc=1973162 |doi=10.1016/j.bmcl.2007.03.066 |url=}}</ref>
 
MTEP is both more [[Potency (pharmacology)|potent]] and more [[Functional selectivity|selective]] than [[MPEP]] as a mGluR5 antagonist,<ref>{{Cite journal | last1 = Lea | first1 = P. M. | last2 = Faden | first2 = A. I. | doi = 10.1111/j.1527-3458.2006.00149.x | title = Metabotropic Glutamate Receptor Subtype 5 Antagonists MPEP and MTEP | journal = CNS Drug Reviews | volume = 12 | issue = 2 | pages = 149–166 | year = 2006 | pmid = 16958988| pmc = }}</ref> and produces similar [[neuroprotective]],<ref>{{Cite journal | last1 = Lea | first1 = P. M. | last2 = Movsesyan | first2 = V. A. | last3 = Faden | first3 = A. I. | doi = 10.1038/sj.bjp.0706219 | title = Neuroprotective activity of the mGluR5 antagonists MPEP and MTEP against acute excitotoxicity differs and does not reflect actions at mGluR5 receptors | journal = British Journal of Pharmacology | volume = 145 | issue = 4 | pages = 527–534 | year = 2009 | pmid = 15821750| pmc =1576169 }}</ref><ref>{{Cite journal
| last1 = Domin | first1 = H.
| last2 = Kajta | first2 = M.