貨號	規格	價格	上海	北京	武漢	南京
S85311-5mg	98.4%	￥841.00 S85311-5mg ￥841.00 現貨	4 4	-	-	-
S85311-10mg	98.4%	￥1270.00 S85311-10mg ￥1270.00 現貨	4 4	-	-	-
S85311-25mg	98.4%	￥2210.00 S85311-25mg ￥2210.00 現貨	5 5	-	-	-
S85311-50mg	≥98%	￥3910.00 S85311-50mg ￥3910.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

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.

產品描述：

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

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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JNJ 16259685