S85311 |
JNJ 16259685 |
源葉(MedMol) | 98% |
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- 產(chǎn)品描述:
JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
- 靶點: mGluR1:19 nM (IC50);GluR
- 體內(nèi)研究:
JNJ16259685 (0.125, 0.25, 0.5, 1, 2, 4 and 8 mg/kg, i.p) significantly reduces the time spent in digging behaviours (0.25-8 mg/kg), threat (all doses) and attack, in comparison with vehicle group. JNJ16259685 (30 mg/kg) produces very minimal effects on locomotor activity. JNJ16259685 dramatically reduces rearing behavior, exploration of a novel environment and lever pressing for a food reward (rat: 0.3 mg/kg; mouse: 1 mg/kg). Subcutaneously administered JNJ16259685 (30 mg/kg) has no effect on reflexive startle responses to loud auditory stimuli or foot shock in mice[2]. JNJ16259685 exhibits high potencies in occupying central mGlu1 receptors in the rat cerebellum and thalamus (ED50=0.040 and 0.014 mg/kg, respectively)
- 參考文獻:
1. Navarro JF,et al. JNJ16259685, a selective mGlu1 antagonist, suppresses isolation-induced aggression in male mice. Eur J Pharmacol. 2008 May 31;586(1-3):217-20. 2. Hodgson RA, et al. Characterization of the selective mGluR1 antagonist, JNJ16259685, in rodent models of movement and coordination. Pharmacol Biochem Behav. 2011 Apr;98(2):181-7. 3. Lavreysen H,et al. JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist. Neuropharmacology. 2004 Dec;47(7):961-72. 4. I Fukunaga , et al. Potent and Specific Action of the mGlu1 Antagonists YM-298198 and JNJ16259685 on Synaptic Transmission in Rat Cerebellar Slices. Br J Pharmacol. 2007 Jul;151(6):870-6.
- 溶解性: Soluble in DMSO
- 保存條件: 2-8℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 3.073 ml 15.366 ml 30.731 ml 5 mM 0.615 ml 3.073 ml 6.146 ml 10 mM 0.307 ml 1.537 ml 3.073 ml 50 mM 0.061 ml 0.307 ml 0.615 ml
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輸入產(chǎn)品批號:
本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)