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BOC Sciences |
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inquiry@bocsci.com |
| Company Name: |
BOC Sciences |
| Tel: |
16314854226 |
| Email: |
info@bocsci.com |
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| | CGP 36216 Basic information |
| Product Name: | CGP 36216 | | Synonyms: | CGP 36216;CGP 36216 hydrochloride;(3-Aminopropyl)ethylphosphinic acid hydrochloride;3-aminopropyl(ethyl)phosphinic acid;Phosphinic acid, P-(3-aminopropyl)-P-ethyl- | | CAS: | 123691-29-2 | | MF: | C5H14NO2P | | MW: | 151.14 | | EINECS: | | | Product Categories: | | | Mol File: | 123691-29-2.mol |  |
| | CGP 36216 Chemical Properties |
| Boiling point | 370.5±25.0 °C(Predicted) | | density | 1.108±0.06 g/cm3(Predicted) | | storage temp. | Desiccate at RT | | solubility | <18.76mg/ml in DMSO; <18.76mg/ml in H2O | | form | solid | | pka | 2.79±0.50(Predicted) | | color | White |
| | CGP 36216 Usage And Synthesis |
| Uses | CGP 36216 Hydrochloride is a selective GABA antagonist, active at the presynaptic but not postsynaptic. | | Biological Activity | 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. | | in vivo | | Animal Model: | Rats[3]. | | Dosage: | 20 μg/Rat. | | Administration: | Intra-VTA injection (ventral tegmental area). | | Result: | Abolishes CPP induced by intra-VTA injection of morphine. |
| | references | 1. ong j, bexis s, marino v, et al. cgp 36216 is a selective antagonist at gaba(b) presynaptic receptors in rat brain. european journal of pharmacology. 2001;415(2-3):191-195. |
| | CGP 36216 Preparation Products And Raw materials |
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