MPEP
MPEP
CAS: 96206-92-7
Molecular Formula: C14H11N
MPEP - Names and Identifiers
| Name | MPEP |
| Synonyms | MPEP CS-715 MPEP,HCl MPEP HYDROCHLORIDE 2-methyl-6-(2-phenylethynyl)pyridine 6-METHYL-2-(PHENYLETHYNYL)-PYRIDINE HCL 2-METHYL-6-(PHENYLETHYNYL)PYRIDINE HYDROCHLORIDE |
| CAS | 96206-92-7 |
MPEP - Physico-chemical Properties
| Molecular Formula | C14H11N |
| Molar Mass | 193.24 |
| Density | 1.10±0.1 g/cm3(Predicted) |
| Melting Point | 45-45.5 °C |
| Boling Point | 124.5-126.5 °C(Press: 0.5 Torr) |
| Solubility | Chloroform (Slightly), Methanol (Slightly) |
| Appearance | Off-white powder. |
| Color | White to Off-White |
| pKa | 2.97±0.12(Predicted) |
| Storage Condition | Desiccate at +4°C |
| Stability | Light Sensitive |
| In vitro study | Up to a concentration of 100 μm MPEP had no significant agonistic or antagonistic activity on the recombinant human mGlu1b receptor expressed in CHO-K1 cells as well as on the Purine receptor expressed endogenously in L(tk-) cells. In addition, MPEP accumulates at cAMP and [35S]-gtpγs with recombinant human metabotropic glutamate receptors type II and III (human mGlu2, -3, -4a, -6, -7b, -8a) and human NMDA (NMDAR1A/2A, -1A/2B), rat AMPA (GluR3), human kainic acid (GluR6) there was no significant agonistic or antagonistic activity during the binding of the receptor subtypes. MPEP inhibited DHPG-stimulated PI hydrolysis at IC50 of 8.0 nM, 20.5 nM, and 17.9 nM in sections of the hippocampus, striatum, and cerebral cortex but not the cerebellum of neonatal rats. MPEP in a recombinant expression system in the regulation of hmGluR4, This effect is completely dependent on activation with the orthosteric antagonist L -AP4. up to a concentration of 100 μm MPEP on recombinant human mGlu1b receptor expressed in CHO-K1 cells as well as L(tk. MPEP positively regulates hmGluR4 in a recombinant expression system, an effect that is completely dependent on the activation of the orthosteric antagonist L -AP4. |
| In vivo study | When microelectrophoretic administration was applied to rat brain, MPEP reduced DHPG-induced stimulation but had no effect on AMPA-induced stimulation. Intravenous MPEP rapidly inhibited DHPG-induced stimulation in a dose-dependent manner but had no effect on AMPA-induced stimulation. Oral MPEP also showed good anti-hyperalgesic activity in Freund's complete adjuvant and turpentine inflammatory pain models. MPEP (1-30 mg/kg) induced an anti-Anxiety effect in the rat conflict drinking and elevated plus maze test and the mouse quadruple dish test. MPEP (1-20 mg/kg) shortened the immobility time in the mouse tail suspension experiment but had no effect on the rats in the behavioral hopelessness test. MPEP had no effect on locomotor activity and motor coordination. MPEP significantly reduced the number and duration of central area entry of fmr1 but not wild-type. In the open field test, MPEP reduced the central region behavior of fmr1tm1Cgr so as to be indistinguishable from the wild type. In the four groups tested, 10 mg/kg and 30 mg/kg MPEP significantly reduced total autonomic activity in the three groups. when microelectrophoretic administration was applied to rat brain, MPEP reduced DHPG-induced stimulation but had no effect on AMPA-induced stimulation. Intravenous MPEP rapidly inhibited DHPG-induced stimulation in a dose-dependent manner but had no effect on AMPA-induced stimulation. Oral MPEP also showed good anti-hyperalgesic activity in Freund's complete adjuvant and turpentine inflammatory pain models. MPEP (1-30 mg/kg) induced an anti-Anxiety effect in the rat conflict drinking and elevated plus maze test and the mouse quadruple dish test. MPEP (1-20 mg/kg) shortened the immobility time in the mouse tail suspension experiment but had no effect on the rats in the behavioral hopelessness test. MPEP had no effect on locomotor activity and motor coordination. MPEP significantly reduced the number and duration of central area entry of fmr1 but not wild-type. In the open field test, MPEP reduced FMR1. |
MPEP - Reference Information
| biological activity | MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM and almost no activity on mGlu1b/2/3/4a/7b/8a/6 receptors. MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM and has little activity on mGlu1b/2/3/4a/7b/8a/6 receptor. |
| in vitro studies | until a concentration of 100 μM MPEP has no obvious agonistic or antagonistic activity on recombinant human mGlu1b receptors expressed in CHO-K1 cells and endogenous purine receptors expressed in L(tk-) cells. In addition, MPEP accumulated in cAMP and [35S]-GTP γS with recombinant human type II and type III metabotropic glutamate receptors (human mGlu2, -3, -4a, -6, -7b, -8a) and human NMDA (NMDAR1A/2A, -1A/2B), rat AMPA (GluR3), there is no obvious agonistic or antagonistic activity during the binding of human kalanine (GluR6) receptor subtypes. In sections of neonatal rat hippocampus, striatum, and cerebral cortex but not cerebellum, MPEP inhibited DHPG-stimulated PI hydrolysis with IC50 of 8.0 nM, 20.5 nM and 17.9 nM, respectively. MPEP regulates the hmGluR4 in a recombinant expression system, and this effect is completely dependent on the activation of the orthosteric antagonist L-AP4. until the concentration of 100 μM MPEP on recombinant human mGlu1b receptor and L(tk) expressed in CHO-K1 cells. MPEP regulates the hmGluR4 in a recombinant expression system, and this effect is completely dependent on the activation of the orthosteric antagonist L-AP4. |
| In vivo studies | When microelectrophoresis is applied to the rat brain, MPEP will reduce DHPG-induced stimulation But it has no effect on AMPA-induced stimulation. Intravenous injection of MPEP quickly inhibited DHPG-induced stimuli, which had a dose-dependent property but had no effect on AMPA-induced stimuli. Oral MPEP also showed good antihyperalgesic activity in Freund's complete adjuvant and turpentine inflammatory pain models. MPEP (1-30 mg/kg) induced anti-anxiety-like effects in rat conflict drinking water and elevated cross maze test and mouse four-square dish test. MPEP (1-20 mg/kg) shortened the immobility time in the mouse tail suspension experiment but had no effect on rats in the behavioral despair test. MPEP has no effect on autonomous activities and motor coordination. MPEP significantly reduced the number and duration of central area entry in fmr1 instead of wild type. In the open field test, MPEP reduced the central area behavior of the fmr1tm1Cgr, so that it could not be distinguished from the wild type. In the four groups tested, 10 mg/kg and 30 mg/kg MPEP significantly reduced the total autonomous activity of the three groups. when microelectrophoresis is applied to rat brain, MPEP will reduce DHPG induced stimulation but have no effect on AMPA induced stimulation. Intravenous injection of MPEP quickly inhibited DHPG-induced stimuli, which had a dose-dependent property but had no effect on AMPA-induced stimuli. Oral MPEP also showed good antihyperalgesic activity in Freund's complete adjuvant and turpentine inflammatory pain models. MPEP (1-30 mg/kg) induced anti-anxiety-like effects in rat conflict drinking water and elevated cross maze test and mouse four-square dish test. MPEP (1-20 mg/kg) shortened the immobility time in the mouse tail suspension experiment but had no effect on rats in the behavioral despair test. MPEP has no effect on autonomous activities and motor coordination. MPEP significantly reduced the number and duration of central area entry in fmr1 instead of wild type. In the open field test, MPEP reduced fmr1. |
| characteristics | MPEP has no effect on other type I/II/III metabotropic glutamate receptors. |
| target | TargetValue mGluR5 36 nM |
| Target | Value |
| mGluR5 | 36 nM |
Last Update：2024-04-09 21:01:54
Supplier List
Product Name: MPEP Visit Supplier Webpage Request for quotation
CAS: 96206-92-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 96206-92-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: MPEP Visit Supplier Webpage Request for quotation
CAS: 96206-92-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 96206-92-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History