| 货号 | 13667-5mg |
| 描述 | The amino acid γ-aminobutyric acid (GABA) is an inhibitory neurotransmitter that acts through two families of heteromeric ligand-gated ion channels, GABAA and GABAC and a G protein-coupled receptor, GABAB. Muscimol is a full GABAA agonist and partial GABAC agonist. It binds GABAA on both high- and low-affinity sites (Kd = 10 and 270 nM, respectively), stimulating chloride efflux with an EC50 value of 200 nM.1 Benzodiazepines enhance the effects of muscimol viaGABAA without altering its binding.1,2 Muscimol activates GABAC receptors with an EC50 value of 1.3 μM.3 It also acts as an inhibitor of GABAA uptake and a substrate for the GABA-metabolizing enzyme GABA transaminase.4 Muscimol impairs memory formation and retrieval in mice and attenuates airway constriction in guinea pigs in vivo.5,6 |
| 别名 | Agarin;Pantherine; |
| 是否危险品 | 是 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Dunn, S.M.J. and Thuynsma, R.P. Reconstitution of purified GABAA receptors: Ligand binding and chloride transporting properties. Biochemistry 33, 755-763 (1994). 2.Parramón, M.,González, M.P. and Oset-Gasque, M.J. Pharmacological modulation of adrenal medullary GABAA receptor: Consistent with its subunit composition. British Journal of Pharmacology 116, 1875-1881 (1995). 3.Zhang, D.,Pan, Z.H.,Awobuluyi, M., et al. Structure and function of GABAc receptors: A comparison of native versus recombinant receptors. Trends in Pharamacological Sciences 22(3), 121-132 (2001). 4.Krogsgaard-Larsen, P.,Frolund, B. and Frydenvang, K. GABA uptake inhibitors. Design, molecular pharmacology and therapeutic aspects. Current Pharmaceutical Design 6, 1193-1209 (2000). 5.Jafari-Sabet, M. and Jannat-Dastjerdi, I. Muscimol state-dependent memory: Involvement of dorsal hippocampal μ-opioid receptors. Behavioural Brain Research 202, 5-10 (2009). 6.Gleason, N.R.,Gallos, G.,Zhang, Y., et al. The GABAA agonist muscimol attenuates induced airway constriction in guinea pigs in vivo. Journal of Applied Physiology 106, 1257-1263 (2009). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 114.1 |
| 分子式 | C4H6N2O2 |
| CAS号 | 2763-96-4 |
| 稳定性 | ≥ 2 years |
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