| Identification | Back Directory | [Name]
CGP 36216 | [CAS]
123691-29-2 | [Synonyms]
CGP 36216
CGP 36216 hydrochloride
3-aminopropyl(ethyl)phosphinic acid
(3-Aminopropyl)ethylphosphinic acid hydrochloride | [Molecular Formula]
C5H14NO2P | [MDL Number]
MFCD20926328 | [MOL File]
123691-29-2.mol | [Molecular Weight]
151.14 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. |
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| Company Name: |
BOC Sciences
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| Tel: |
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| Website: |
https://www.bocsci.com |
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