(RS)-MCPG - CAS 146669-29-6
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
(RS)-MCPG is a non-selective group I/group II metabotropic glutamate receptor antagonist.
≥99% by HPLC
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1.Glutamatergic receptors of the rostral ventrolateral medulla are involved in the ventilatory response to hypoxia.
de Paula PM;Branco LG Respir Physiol Neurobiol. 2005 Apr 15;146(2-3):125-34.
Rostral ventrolateral medulla (RVLM) is a region in the brainstem that is involved in the physiologic responses to hypoxia (i.e. hyperventilation and regulated hypothermia) and contains l-glutamate receptors. Therefore, we examined the effects of blocked of glutamatergic receptors in the RVLM on hypoxic hyperventilation and regulated hypothermia. Ventilation (V(E)) and body temperature (T(b)) were measured before and after bilaterally microinjection of kynurenic acid (KYN, 5 nmol/100 nl, an ionotropic glutamatergic receptors antagonist) and alpha-methyl-4-carboxyphenylglycine (MCPG, 10 nmol/100 nl, a metabotropic glutamatergic receptors antagonist) into the RVLM, followed by a 60-min period of hypoxia exposure. Control rats received microinjection of saline (vehicle). KYN or MCPG into the RVLM did not change V(E) and T(b) under normoxia, but reduced the hypoxic hyperventilation due to a lower tidal volume, although regulated hypothermia persisted. These data suggest that glutamatergic receptors in the RVLM are involved in the ventilatory response to hypoxia, exercising an excitatory modulation of the RVLM neurons, but play no role in hypoxia-induced hypothermia.
2.[Involvement of the amygdala on place aversion induced by naloxone in single-dose morphine-treated rats].
Ishida S;Shimosaka R;Kawasaki Y;Jin C;Kitamura Y;Araki H;Sendo T;Gomita Y Yakugaku Zasshi. 2008 Mar;128(3):395-403.
Signs characteristic of opiate withdrawal symptoms can be precipitated by an opiate antagonist after short-term infusion or even a single dose of an opiate both in humans and in animals. This phenomenon has been referred to as acute dependence. In contrast to extensive studies on chronic dependence, less is known about the neural mechanisms mediating acute dependence. It will benefit the development of appropriate therapies to facilitate opiate abstinence and reduced craving to better understand the mechanisms underlying acute opiate dependence and to determine whether there are dissociation and similarity between the early and fully developed stages of dependence. In the present study, we examined the influence of c-Fos expression in the amygdala in acquisition of conditioned place aversion (CPA) induced by naloxone-precipitated withdrawal from a single morphine exposure 24 h earlier. The effect of microinjection into the central amygdaloid nucleus (CeA) of various kinds of glutamatergic neurotransmission inhibitors was also investigated. Findings showed that CeA displayed significant increase in c-Fos expression in the acquisition of CPA. Furthermore, CPA was attenuated significantly and dose-dependently by microinjection into CeA of all glutamatergic neurotransmission inhibitors (NMDA receptor antagonist (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclo-hepten-5,10-imine maleate (MK-801), AMPA receptor antagonist 1-(4-aminophenyl)4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride (GYKI52466), metabotropic glutamate receptor antagonist (+/-)-alpha-methyl-4-carboxyphenylglycine (MCPG), and glutamate release inhibitor riluzole).
3.Immunocytochemical and pharmacological characterization of metabotropic glutamate receptors of the vestibular end organs in the frog.
Andrianov GN;Puyal J;Raymond J;Ventéo S;Demêmes D;Ryzhova IV Hear Res. 2005 Jun;204(1-2):200-9.
Using immunocytochemistry and multiunit recording of afferent activity of the whole vestibular nerve, we investigated the role of metabotropic glutamate receptors (mGluR) in the afferent neurotransmission in the frog semicircular canals (SCC). Group I (mGluR1alpha) and group II (mGluR2/3) mGluR immunoreactivities were distributed to the vestibular ganglion neurons, and this can be attributed to a postsynaptic locus of metabotropic regulation of rapid excitatory transmission. The effects of group I/II mGluR agonist (1S,3R)-1-aminocyclopentane-trans-1,3-dicarboxylic acid (ACPD) and antagonist (R,S)-alpha-methyl-4-carboxyphenylglycine (MCPG) on resting and chemically induced afferent activity were studied. ACPD (10-100 microM) enhanced the resting discharge frequency. MCPG (5-100 microM) led to a concentration-dependent decrease of both resting activity and ACPD-induced responses. If the discharge frequency had previously been restored by L-glutamate (L-Glu) in high-Mg2+ solution, ACPD elicited a transient increase in the firing rate in the afferent nerve suggesting that ACPD acts on postsynaptic receptors. The L-Glu agonists, alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA) and N-methyl-D-aspartate (NMDA), were tested during application of ACPD.
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CAS 146669-29-6 (RS)-MCPG

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