CGP 36216 hydrochloride

Catalog No. Size PriceQuantity
M22860-C Contact for quotation $100Unavailable


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.

Product information

CAS Number: 123691-29-2

Molecular Weight: 187.60

Formula: C5H15ClNO2P

Chemical Name: (3-aminopropyl)(ethyl)phosphinic acid hydrochloride

Smiles: Cl.CCP(O)(=O)CCCN


InChi: InChI=1S/C5H14NO2P.ClH/c1-2-9(7,8)5-3-4-6;/h2-6H2,1H3,(H,7,8);1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.

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