您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > (+)-Igmesine hydrochloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
(+)-Igmesine 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。
(+)-Igmesine hydrochloride图片
CAS NO:130152-35-1
规格:98%
分子量:355.94
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
σ1 receptor ligand
CAS:130152-35-1
分子式:C23H29N.HCl
分子量:355.94
纯度:98%
存储:Store at -20°C

Background:

IC50: 19.1 nM


JO 1784 is a selective σ1 receptor ligand.


The CNS σ receptor ligands, as is known, modulates central neurotransmitter systems ( noradrenergic-, glutaminergic-, and dopaminergic-neurons was included).


In vitro: Compared with control, data obtained displayed significant reduction in the densities of β-adrenergic, but not σ1, 5-HT1A, and GABAB receptors in fluoxetine (18%), desipramine (DMI, 32%) and JO 1784 (20%)-treated groups. Tyrosine hydroxylase (TH) activity was significantly (30–32%) decreased in all treated groups. Further, fluoxetine and DMI excluding the JO 1784 -treated groups diaplayed 85 and 40% reductions in serotonin (5-HT) and noradrenaline (NE) neuronal uptake, respectively. Following acute treatment, JO 1784 is inactive for monoamine oxidase (MAO) A or B [1].


In vivo: In vivo studies, JO 1784 at behaviorally active doses exhibited weak effects on the NE uptake but has no activity in altering 5-HT and DA synthesis or antagonizing selective drug-stimulated depletion of monoamine neuronal uptake. NMDA-induced potentiates cGMP was inhibited by JO 1784, indicating that JO 1784 may interfere with the NMDA receptor/NOS/cGMP pathway. Although it appears that the pharmacological actions of JO 1784 partially is modulated by the monoaminergic system, there is still need to find other possible mechanisms of antidepressant action [1].


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


Reference:
[1].  Akunne HC, Zoski KT, Whetzel SZ, Cordon JJ, Brandon RM, Roman F, Pugsley TA. Neuropharmacological profile of a selective sigma ligand, igmesine: a potential antidepressant. Neuropharmacology. 2001 Jul;41(1):138-49.