Guanidinoethyl sulfonate_竞争性甘氨酸受体拮抗剂_543-18-0_Apexbio

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生物活性
靶点 :
Membrane Transporter/Ion Channel
信号通路:
Glycine Receptors
产品描述:
Guanidinoethyl sulfonate is a competitive glycine receptor antagonist. The glycine receptor, the receptor for the amino acid neurotransmitter glycine, is an ionotropic receptor producing its effects via chloride current. Glycine receptor is one of the most widely distributed inhibitory receptors in the central nervous system and has important roles in various physiological processes. In vitro: Guanidinoethyl sulphonate was found to be an analogue of taurine and an inhibitor of
taurine transport. Guanidinoethyl sulphonate was also shown to be a weak agonist at GABA(A) receptors, and was able to antagonize GABA-evoked responses. Guanidinoethyl sulphonate did not gate GlyR. 3. but antagonized glycine responses in a concentration-dependent and surmountable manner. Glycine receptor-mediated taurine responses were competitively antagonized by guanidinoethyl sulphonate. Taurine dose-response curves, in contrast to the glycine dose-response curves were shifted by guanidinoethyl sulphonate to the right in a parallel manner [1]. In vivo: Guanidinoethyl sulphonate delivered in the drinking water of rats for 1 month could effectively reduce taurine levels in brain structures and outside the brain by between 50 and 80 %, depending on the tissue. This partial taurine depletion could not affect either basal synaptic transmission or the late phase of long-term potentiation in hippocampal slices. In-vivo microdialysis studies in the hippocampus demonstrated that guanidinoethyl sulphonate was able to reduce extracellular taurine levels and the magnitude of taurine released in response to the application of either N-methyl-D-aspartate or a hypoosmotic solution [2]. Clinical trial: So far, no clinical study has been conducted.
产品说明书
化学性质
产品名: Guanidinoethyl sulfonate 修订日期: 6/30/2016
产品名: Cas No.: 分子量: 分子式: 别名: 化学名: SMILES: 溶解性: 储存条件: 一般建议:
运输条件:
Guanidinoethyl sulfonate
543-18-0
167.2
//struct//
C3H9N3O3S
NSC 667063,Taurocyamine
2-[(aminoiminomethyl)amino]-ethanesulfonic acid
OS(CCNC(N)=N)(=O)=O
Soluble in DMSO
Store at -20°C
For obtaining a higher solubility , please warm the tube at 37°C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.
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