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PRE-084 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PRE-084 hydrochloride图片
CAS NO:75136-54-8
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
PRE-084 hydrochloride 是一种高度选择性的 σ1 受体 (S1R) 激动剂,IC50 为 44 nM。
Cas No.75136-54-8
别名1-苯基环己烷羧酸2-(4-吗啉基)乙基酯盐酸盐
化学名2-morpholinoethyl 1-phenylcyclohexanecarboxylate hydrochloride
Canonical SMILESO=C(C1(C2=CC=CC=C2)CCCCC1)OCCN3CCOCC3.Cl
分子式C19H27NO3.HCl
分子量353.89
溶解度≥ 17.3mg/mL in DMSO with gentle warming
储存条件Store at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ki: 2.2 and 13091 nM for σ1 and σ2 receptors respectively.

PRE-084 hydrochloride is a selective σ1 agonist with high affinity, rather than over PCP receptors (IC50 > 100000 nM) and several other receptor systems. It was reported that sigma (s) receptor ligands to alleviate learning and memory impairments on several pharmacological and pathological rodent models of amnesia, involving the s1 subtype of s receptor.

In vitro: PRE-084 had an IC50 of 44 nM in the receptor assay and an IC50 of more than 100,000 nM for PCP receptors and an IC50 higher than 1 0,000 nM in many other receptor systems. In general, hydroxy-substituted phenyl groups in these compounds like PRE-084 tended to have attenuated potency at a receptors, whereas methylphenyl and chlorophenyl substitutions enhanced potencies. Reduction of cycloalkyl ring size lowered potencies for a receptors and quatemized amine groups invariably decreased the compound’s potencies. [1]. The Sig-1R agonist PRE084 not only increases cell survival, but also counteracts the deleterious effects caused by NMHP in neuronal PC6.3 cells. Particularly, PRE084 stimulates the NF-kB pathway that is compromised by the expression of mutant huntingtin proteins, increasing the levels of cellular antioxidants. These data show that the Sig-1R agonist beneficially effects on models of HD and that compounds binding the Sig-1R may be potent targets for future drug development in HD [2].

In vivo: After exposure to CO or 14 days after intoxication with trimethyltin, the spontaneous alternation deficits was reversed significantly by the selective sigma1 ligand PRE-084 (1 mg kg-1) [3]. Administration of Pre-084 (5 mg/kg, i.p.) inhibited citric-acid-induced cough in guinea-pigs. In addition, when administered by aerosol, sigma agonist Pre-084 (1 mg/ml) inhibited cough [4].

Clinical trial: So far, no clinical study has been conducted.

References:
[1]. Su TP, Wu XZ, Cone EJ, Shukla K, Gund TM, Dodge AL, Parish DW. Sigma compounds derived from phencyclidine: identification of PRE-084, a new, selective sigma ligand. J Pharmacol Exp Ther. 1991 Nov;259(2):543-50.
[2]. Hyrskyluoto A, Pulli I, Trnqvist K, Ho TH, Korhonen L, Lindholm D. Sigma-1 receptor agonist PRE084 is protective against mutant huntingtin-induced cell degeneration: involvement of calpastatin and the NF-κB pathway. Cell Death Dis. 2013 May 23; 4:e646.
[3]. Maurice T, Phan VL, Noda Y, Yamada K, Privat A, Nabeshima T. The attenuation of learning impairments induced after exposure to CO or trimethyltin in mice by sigma (sigma) receptor ligands involves both sigma1 and sigma2 sites. Br J Pharmacol. 1999 May; 127(2):335-42.
[4]. Brown C, Fezoui M, Selig WM, Schwartz CE, Ellis JL. Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br J Pharmacol. 2004 Jan; 141(2):233-40. Epub 2003 Dec 22.