CGP 36216 hydrochloride

Selective GABAB antagonist CAS# 123691-29-2

CGP 36216 hydrochloride

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Quality Control of CGP 36216 hydrochloride

Number of papers citing our products

Chemical structure

CGP 36216 hydrochloride

3D structure

Chemical Properties of CGP 36216 hydrochloride

Cas No. 123691-29-2 SDF Download SDF
PubChem ID 9898878 Appearance Powder
Formula C5H14NO2P M.Wt 151.1
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water and to 100 mM in DMSO
Chemical Name 3-aminopropyl(ethyl)phosphinic acid
SMILES CCP(=O)(CCCN)O
Standard InChIKey RWCIPYZWXPUGRM-UHFFFAOYSA-N
Standard InChI InChI=1S/C5H14NO2P/c1-2-9(7,8)5-3-4-6/h2-6H2,1H3,(H,7,8)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of CGP 36216 hydrochloride

DescriptionSelective GABAB antagonist. Displays activity at presynaptic receptors; ineffective at GABAB postsynaptic receptors.

CGP 36216 hydrochloride Dilution Calculator

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CGP 36216 hydrochloride Molarity Calculator

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Preparing Stock Solutions of CGP 36216 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 6.6181 mL 33.0907 mL 66.1813 mL 132.3627 mL 165.4533 mL
5 mM 1.3236 mL 6.6181 mL 13.2363 mL 26.4725 mL 33.0907 mL
10 mM 0.6618 mL 3.3091 mL 6.6181 mL 13.2363 mL 16.5453 mL
50 mM 0.1324 mL 0.6618 mL 1.3236 mL 2.6473 mL 3.3091 mL
100 mM 0.0662 mL 0.3309 mL 0.6618 mL 1.3236 mL 1.6545 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on CGP 36216 hydrochloride

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:
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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References on CGP 36216 hydrochloride

CGP 36216 is a selective antagonist at GABA(B) presynaptic receptors in rat brain.[Pubmed:11274998]

Eur J Pharmacol. 2001 Mar;415(2-3):191-5.

In rat neocortical preparations maintained in Mg(2+)-free Krebs medium, baclofen depressed the frequency of spontaneous discharges in a concentration-dependent manner (EC(50) = 6 microM), sensitive to (3-aminopropyl)ethylphosphinic acid (CGP 36216) (100, 300 and 500 microM) (pA(2) = 3.9 +/- 0.1). By contrast, CGP 36216, up to 1 mM, was ineffective in antagonising baclofen-induced hyperpolarisations, mediated through gamma-aminobutyric acid(B) (GABA(B)) postsynaptic receptors. In electrically stimulated brain slices preloaded with [3H]GABA, CGP 36216 increased [3H]GABA release (IC(50) = 43 microM), which was reversed by baclofen (20 microM). While CGP 36216 is ineffective at GABA(B) postsynaptic receptors, it is appreciably more active at presynaptic receptors.

Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists.[Pubmed:7650685]

J Med Chem. 1995 Aug 18;38(17):3313-31.

In 1987, 25 years after the synthesis of the potent and selective GABAB agonist baclofen (1), Kerr et al. described the first GABAB antagonist phaclofen 2. However, phaclofen and structurally similar derivatives 3-5 did not cross the blood-brain barrier and hence were inactive in vivo as central nervous system agents. As a consequence, the therapeutic potential of GABAB antagonists remained unclear. In exploring GABA and baclofen derivatives by replacing the carboxylic acid residue with various phosphinic acid groups, we discovered more potent and water soluble GABAB antagonists. Electrophysiological experiments in vivo demonstrated that some of the new compounds were capable of penetrating the blood-brain barrier after oral administration. Neurotransmitter release experiments showed that they interacted with several presynaptic GABAB receptor subtypes, enhancing the release of GABA, glutamate, aspartate, and somatostatin. The new GABAB antagonists interacted also with postsynaptic GABAB receptors, as they blocked late inhibitory postsynaptic potentials. They facilitated the induction of long-term potentiation in vitro and in vivo, suggesting potential cognition enhancing effects. Fifteen compounds were investigated in various memory and learning paradigms in rodents. Although several compounds were found to be active, only 10 reversed the age-related deficits of old rats in a multiple-trial one-way active avoidance test after chronic treatment. The cognition facilitating effects of 10 were confirmed in learning experiments in Rhesus monkeys. The novel GABAB antagonists showed also protective effects in various animal models of absence epilepsy.

Description

GABAB antagonist; displays activity at presynaptic receptors

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