Quality Level
assay
≥97% (HPLC)
form
solid
color
white to off-white
solubility
H2O: 16 mg/mL, DMSO: insoluble
SMILES string
[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
Application
(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。
Biochem/physiol Actions
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。
Features and Benefits
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。
Preparation Note
(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。
Legal Information
根据加利福尼亚大学授予的独家许可在美国销售。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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
The first selective antagonist for a GABAC receptor.
Murata, Y., et al.
Bioorganic & Medicinal Chemistry Letters, 6, 2073-2076 (1996)
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| T200-50MG | 04061832093918 |
| T200-10MG | 04061832093901 |