Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists

被引：56

作者：

Kulkarni, Santosh S. ^{[1
]}

Newman, Amy Hauck ^{[1
]}

机构：

[1] NIH, Med Chem Sect, NIDA, DHHS, Baltimore, MD 21224 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 11期

关键词：

D O I：

10.1016/j.bmcl.2007.03.066

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Investigation of a series of heterobicyclic compounds with essential pharmacophoric features of the metabotropic glutamate receptor 5 (mGluR5) antagonists MPEP and MTEP provided novel structural templates with sub-micromolar affinities at the mGluR5. Published by Elsevier Ltd.

引用

页码：2987 / 2991

页数：5

共 31 条

[1] mGluR5 antagonist MPEP reduces ethanol-seeking and relapse behavior [J].

Bäckström, P ;

Bachteler, D ;

Koch, S ;

Hyytiä, P ;

Spanagel, R .

NEUROPSYCHOPHARMACOLOGY, 2004, 29 (05) :921-928

[2] Catalysts for Suzuki-Miyaura coupling processes: Scope and studies of the effect of ligand structure [J].

Barder, TE ;

Walker, SD ;

Martinelli, JR ;

Buchwald, SL .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2005, 127 (13) :4685-4696

[3] Therapeutic implications of the mGluR theory of fragile X mental retardation [J].

Bear, MF .

GENES BRAIN AND BEHAVIOR, 2005, 4 (06) :393-398

[4]

BRODKIN J, 2002, PHARM BIOCH BEHAV, V23, P207

[5] Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists [J].

Büttelmann, B ;

Peters, JU ;

Ceccarelli, S ;

Kolczewski, S ;

Vieira, E ;

Prinssen, EP ;

Spooren, W ;

Schuler, F ;

Huwyler, J ;

Porter, RHP ;

Jaeschke, G .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (07) :1892-1897

[6] Reinforcing and locomotor stimulant effects of cocaine are absent in mGluR5 null mutant mice [J].

Chiamulera, C ;

Epping-Jordan, MP ;

Zocchi, A ;

Marcon, C ;

Cottiny, C ;

Tacconi, S ;

Corsi, M ;

Orzi, F ;

Conquet, F .

NATURE NEUROSCIENCE, 2001, 4 (09) :873-874

[7] Pharmacology and functions of metabotropic glutamate receptors [J].

Conn, PJ ;

Pin, JP .

ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, 1997, 37 :205-237

[8] 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: A potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity [J].

Cosford, NDP ;

Tehrani, L ;

Roppe, J ;

Schweiger, E ;

Smith, ND ;

Anderson, J ;

Bristow, L ;

Brodkin, J ;

Jiang, XH ;

McDonald, I ;

Rao, S ;

Washburn, M ;

Varney, MA .

JOURNAL OF MEDICINAL CHEMISTRY, 2003, 46 (02) :204-206

[9] Up-regulation of metabotropic glutamate receptor subtypes 3 and 5 in spinal cord in a clinical model of persistent inflammation and hyperalgesia [J].

Dolan, S ;

Kelly, JG ;

Monteiro, AM ;

Nolan, AM .

PAIN, 2003, 106 (03) :501-512

[10] Discovery and characterization of non-competitive antagonists of group I metabotropic glutamate receptors [J].

Gasparini, F ;

Floersheim, P ;

Flor, PJ ;

Heinrich, M ;

Inderbitzin, W ;

Ott, D ;

Pagano, A ;

Stierlin, C ;

Stoehr, N ;

Vranesic, I ;

Kuhn, R .

FARMACO, 2001, 56 (1-2) :95-99

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