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Anxiolytic-like effects of mGlu1 and mGlu5 receptor antagonists in rats.
Eur J Pharmacol. 2005 May 02; 514(1):25-34.EJ

Abstract

The purpose of the present study was to compare anxiolytic activity of the metabotropic glutamate receptor 1 (mGlu) antagonist, EMQMCM ((3-ethyl-2-methyl-quinolin-6-yl)-(4-methoxy-cyclohexyl)-methanone methanesulfonate) and the mGlu5 receptor antagonist MTEP ([(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine) and MPEP (2-methyl-6-(phenylethynyl)pyridine) in animal models of anxiety. In the elevated plus maze, diazepam (1 mg/kg), but not the mGlu1 or mGlu5 receptor antagonists induced anxiolytic-like effects. Meanwhile, MTEP (2.5 and 5 mg/kg), EMQMCM (5 mg/kg), and diazepam (2 mg/kg) all significantly inhibited fear potentiated startle. In the contextual fear conditioning test, MTEP (1.25 and 2.5 but not 5 mg/kg) and EMQMCM (0.6 to 5 mg/kg) attenuated freezing responding. In the Geller-Seifter conflict test, MPEP (1 and 3 mg/kg), MTEP (3 mg/kg), chlordiazepoxide (10 and 20 mg/kg) and midazolam (1 mg/kg) all facilitated punished responding, while ECMQCM failed to produce any significant effects up to 3 mg/kg dose. To summarise, the present data further support a significant anxiolytic potential of group I mGlu receptor antagonists, while suggesting the effects of mGlu1 receptor antagonists may depend on the experimental procedure and may be qualitatively different from those of mGlu5 receptor antagonists.

Authors+Show Affiliations

Preclinical R&D, Merz Pharmaceuticals GmbH, Eckenheimer Landstrasse 100, 60318 Frankfurt am Main, Germany.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

15878321

Citation

Pietraszek, Małgorzata, et al. "Anxiolytic-like Effects of mGlu1 and mGlu5 Receptor Antagonists in Rats." European Journal of Pharmacology, vol. 514, no. 1, 2005, pp. 25-34.
Pietraszek M, Sukhanov I, Maciejak P, et al. Anxiolytic-like effects of mGlu1 and mGlu5 receptor antagonists in rats. Eur J Pharmacol. 2005;514(1):25-34.
Pietraszek, M., Sukhanov, I., Maciejak, P., Szyndler, J., Gravius, A., Wisłowska, A., Płaźnik, A., Bespalov, A. Y., & Danysz, W. (2005). Anxiolytic-like effects of mGlu1 and mGlu5 receptor antagonists in rats. European Journal of Pharmacology, 514(1), 25-34.
Pietraszek M, et al. Anxiolytic-like Effects of mGlu1 and mGlu5 Receptor Antagonists in Rats. Eur J Pharmacol. 2005 May 2;514(1):25-34. PubMed PMID: 15878321.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Anxiolytic-like effects of mGlu1 and mGlu5 receptor antagonists in rats. AU - Pietraszek,Małgorzata, AU - Sukhanov,Ilia, AU - Maciejak,Piotr, AU - Szyndler,Janusz, AU - Gravius,Andreas, AU - Wisłowska,Aleksandra, AU - Płaźnik,Adam, AU - Bespalov,Anton Y, AU - Danysz,Wojciech, Y1 - 2005/04/19/ PY - 2004/12/02/received PY - 2005/03/15/revised PY - 2005/03/18/accepted PY - 2005/5/10/pubmed PY - 2005/8/27/medline PY - 2005/5/10/entrez SP - 25 EP - 34 JF - European journal of pharmacology JO - Eur J Pharmacol VL - 514 IS - 1 N2 - The purpose of the present study was to compare anxiolytic activity of the metabotropic glutamate receptor 1 (mGlu) antagonist, EMQMCM ((3-ethyl-2-methyl-quinolin-6-yl)-(4-methoxy-cyclohexyl)-methanone methanesulfonate) and the mGlu5 receptor antagonist MTEP ([(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine) and MPEP (2-methyl-6-(phenylethynyl)pyridine) in animal models of anxiety. In the elevated plus maze, diazepam (1 mg/kg), but not the mGlu1 or mGlu5 receptor antagonists induced anxiolytic-like effects. Meanwhile, MTEP (2.5 and 5 mg/kg), EMQMCM (5 mg/kg), and diazepam (2 mg/kg) all significantly inhibited fear potentiated startle. In the contextual fear conditioning test, MTEP (1.25 and 2.5 but not 5 mg/kg) and EMQMCM (0.6 to 5 mg/kg) attenuated freezing responding. In the Geller-Seifter conflict test, MPEP (1 and 3 mg/kg), MTEP (3 mg/kg), chlordiazepoxide (10 and 20 mg/kg) and midazolam (1 mg/kg) all facilitated punished responding, while ECMQCM failed to produce any significant effects up to 3 mg/kg dose. To summarise, the present data further support a significant anxiolytic potential of group I mGlu receptor antagonists, while suggesting the effects of mGlu1 receptor antagonists may depend on the experimental procedure and may be qualitatively different from those of mGlu5 receptor antagonists. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/15878321/Anxiolytic_like_effects_of_mGlu1_and_mGlu5_receptor_antagonists_in_rats_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0014-2999(05)00315-8 DB - PRIME DP - Unbound Medicine ER -