T200
(1,2,5,6-四氢吡啶-4-基)甲基次磷酸 水合物
≥97% (HPLC), solid
别名:
TPMPA 水合物
质量水平
方案
≥97% (HPLC)
表单
solid
颜色
white to off-white
溶解性
H2O: 16 mg/mL
DMSO: insoluble
SMILES字符串
[H]O[H].CP([O-])(=O)C1=CC[NH2+]CC1
InChI
1S/C6H12NO2P.H2O/c1-10(8,9)6-2-4-7-5-3-6;/h2,7H,3-5H2,1H3,(H,8,9);1H2
InChI key
GXVWAQPRAQORGS-UHFFFAOYSA-N
应用
(1,2,5,6-四氢吡啶-4-基)甲基次磷酸(TPMPA)水合物已用作视网膜神经节细胞的γ-氨基丁酸C(GABAc)抑制剂。
TPMA已作为GABAC受体拮抗剂，研究侏儒神经节细胞中的内层视网膜抑制作用。TPMPA还用于研究GABAC受体拮抗剂抑制神经节细胞定向选择性的作用。
生化/生理作用
TPMPA融合异四氢烟酸和3-APMPA特性，既保留GABAC受体亲和性，又不与GABAA或GABAB受体作用。电活动分析表明，TPMPA是非洲爪蟾卵母细胞表达克隆人mu 1 GABAC受体的竞争性拮抗剂（Kb约2μM）。TPMPA是弱>100倍的卵母细胞表达的大鼠脑GABAA受体抑制剂（Kb约320 μM），对大鼠海马体切片中的GABAB受体仅有较弱的激动剂活性（EC50约500 μM）。TPMPA 可用于研究视网膜外层和神经系统中其他受体表达区域中的GABAC受体功能。
特点和优势
该化合物是神经科学研究推荐产品。点击此处 ，查看更多神经科学精选产品。想要了解有关生物活性小分子在其他研究领域应用的更多信息，请访问 sigma.com/discover-bsm。
制备说明
(1,2,5,6-四氢吡啶-4-基)甲基次磷酸(TPMPA)水合物可溶于水(16 mg/ml)，但不溶于DMSO。
法律信息
根据加利福尼亚大学授予的独家许可在美国销售。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
G A Johnston
Trends in pharmacological sciences, 17(9), 319-323 (1996-09-01)
The inhibitory neurotransmitter, GABA, activates a variety of receptors in all areas of the CNS. Two major subtypes of GABA receptors are well known: (1) GABAA receptors are ligand-gated Cl- channels that consist of a heteromeric mixture of protein subunits
M Chebib et al.
British journal of pharmacology, 122(8), 1551-1560 (1998-01-10)
1. gamma-Aminobutyric acid (GABA) and trans-4-aminocrotonic acid (TACA) have been shown to activate GABAC receptors. In this study, a range of C2, C3, C4 and N-substituted GABA and TACA analogues were examined for activity at GABAC receptors. 2. The effects
Xinling Song et al.
International journal of molecular sciences, 21(8) (2020-04-23)
The present work investigated the anti-inflammatory, antioxidant, and lung protection effects of acetylated Pleurotus geesteranus polysaccharides (AcPPS) on acute lung injury (ALI) mice. The acetylation of AcPPS was successfully shown by the peaks of 1737 cm-1 and 1249 cm-1 by
The first selective antagonist for a GABAC receptor.
Murata, Y., et al.
Bioorganic & Medicinal Chemistry Letters, 6, 2073-2076 (1996)
Cindy Karouta et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 35(9), e21846-e21846 (2021-08-19)
Myopia (short-sightedness), usually caused by excessive elongation of the eye during development, has reached epidemic proportions worldwide. In animal systems including the chicken model, several treatments have been shown to inhibit ocular elongation and experimental myopia. Although diverse in their
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