| CAS NO: | 123691-29-2 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Cas No. | 123691-29-2 |
| 化学名 | (3-aminopropyl)(ethyl)phosphinic acid hydrochloride |
| Canonical SMILES | CCP(CCCN)(O)=O.Cl |
| 分子式 | C5H14NO2P.HCl |
| 分子量 | 187.6 |
| 溶解度 | <18.76mg/ml in DMSO;<18.76mg/ml in Water |
| 储存条件 | Desiccate at RT |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | CGP 36216 hydrochloride is a potent and selective antagonist of GABAB receptors with IC50 value of 43 μM. GABAB receptors (GABABR) are metabotropic transmembrane receptors for gamma-aminobutyric acid (GABA) and are linked through G-proteins to potassium channels. Expression of GABAB receptors are found in the central as well as in the autonomic division of the peripheral nervous system. GABAB receptors play a key role in regulating membrane excitability and synaptic transmission in the brain. In rat neocortical preparations maintained in Mg2+-free Krebs medium, CGP 36216 acts as antagonism of baclofen-induced suppression of spontaneous discharges in a concentration-dependent manner. However, CGP 36216, up to 1 mM, was ineffective in antagonising baclofen-induced hyperpolarisations, mediated through gamma-aminobutyric acid (B) GABAB postsynaptic receptors 1. In electrically stimulated brain slices preloaded with [3H] GABA, CGP 36216 increased the release of [3H] GABA, that was reversed by baclofen. While CGP 36216 is ineffective at GABAB postsynaptic receptors, it is appreciably more active at presynaptic receptors1. Reference: |
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