CAS NO: | 219911-35-0 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
Cas No. | 219911-35-0 |
别名 | 2-甲基-6-(苯基乙炔基)吡啶盐酸盐 |
化学名 | 2-methyl-6-(2-phenylethynyl)pyridine;hydrochloride |
Canonical SMILES | CC1=CC=CC(=N1)C#CC2=CC=CC=C2.Cl |
分子式 | C14H12ClN |
分子量 | 229.7 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 5 mg/ml |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | IC50: 36 nM MPEP is a potent, selective and systemically active mGlu5 receptor antagonist. Metabotropic glutamate (mGlu) receptors are a of G-protein-coupled receptor family linked to multiple second messengers and modulation of ion channel functions in the nervous system. Group I receptors (mGlu1 and -5) couple to phospholipase C and up or down regulate neuronal excitability (Gereau and Conn, 1995) whereas group II (mGlu2 and -3) and group III (mGlu4, -6, -7, and -8) receptors inhibit adenylyl cyclase and reduce synaptic transmission. In vitro: In recombinant expressed cells human mGlu5a receptor, MPEP inhibited quisqualate-stimulated phosphoinositide hydrolysis completely with an IC50 value of 36 nM whereas with no agonist or antagonist activities at cells expressing the human mGlu1b receptor. MPEP did not show agonist or antagonist activity on human mGlu2, -3, -4a, -7b, and -8a receptors [1]. In vivo: In rat neonatal brain slices, MPEP inhibited DHPG-stimulated phosphoinositide hydrolysis with a potency and selectivity similar to that observed on human mGlu receptors. Moreover, in extracellular recordings in the hippocampus CA1 area of anesthetized rats, the microiontophoretic application of DHPG induced neuronal firing that was blocked when MPEP was administered [1]. Clinical trial: N/A Reference: |