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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

Pietraszek M
Preclinical R&D, Merz Pharmaceuticals GmbH, Eckenheimer Landstrasse 100, 60318 Frankfurt am Main, Germany.
Sukhanov I
No affiliation info available
Maciejak P
No affiliation info available
Szyndler J
No affiliation info available
Gravius A
No affiliation info available
Wisłowska A
No affiliation info available
Płaźnik A
No affiliation info available
Bespalov AY
No affiliation info available
Danysz W
No affiliation info available

MeSH

Analysis of VarianceAnimalsAnti-Anxiety AgentsAnxietyBehavior, AnimalChlordiazepoxideConditioning, OperantDiazepamDose-Response Relationship, DrugMaleMaze LearningMidazolamPunishmentPyridinesQuinolinesRatsRats, Sprague-DawleyReceptor, Metabotropic Glutamate 5Receptors, Metabotropic GlutamateReflex, StartleThiazoles

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_ DB - PRIME DP - Unbound Medicine ER -