A GABAB receptor antagonist
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CGP 55845 (hydrochloride)

Item No. 21912

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
P-[(2S)-3-[[(1S)-1-(3,4-dichlorophenyl)ethyl]amino]-2-hydroxypropyl]-P-(phenylmethyl)-phosphinic acid, monohydrochloride
CAS Number
149184-22-5
Synonyms
  • CGP 55845A
Molecular Formula
C18H22Cl2NO3P • HCl
Formula Weight
438.7
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
OP(CC1=CC=CC=C1)(C[C@@H](O)CN[C@@H](C)C2=CC(Cl)=C(Cl)C=C2)=O.Cl
InChi Code
InChI=1S/C18H22Cl2NO3P.ClH/c1-13(15-7-8-17(19)18(20)9-15)21-10-16(22)12-25(23,24)11-14-5-3-2-4-6-14;/h2-9,13,16,21-22H,10-12H2,1H3,(H,23,24);1H/t13-,16-;/m0./s1
InChi Key
PXQAIXBYWZBYKJ-LINSIKMZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $119

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    10 mg

    $225

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    25 mg

    $532

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    Product Description

    CGP 55845 is a GABAB receptor antagonist (Ki = 4.5 nM).1 It increases electrical stimulation-induced GABA release in the absence and presence of the GABAB receptor agonist (–)-baclofen, as well as glutamate release in the presence of (–)-baclofen, in rat cerebral cortex slices (EC50s = 8.3, 25, and 14 nM, respectively). CGP 55845 (1 µM) inhibits (–)-baclofen-induced postsynaptic hyperpolarization of evoked inhibitory postsynaptic potentials (IPSPs) and field excitatory postsynaptic potentials (fEPSPs) in rat CA1 hippocampal slices.2 It increases swimming time, but does not decrease immobility time, in the forced swim test in rats when administered at a dose of 3 or 10 mg/kg.3 CGP 55845 (0.01 and 0.1 mg/kg) reverses age-induced impairments in olfactory discrimination learning in rats.4 It increases seizure intensity in a mouse model of epilepsy induced by pentylenetetrazole (PTZ; Item No. 18682) kindling.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Waldmeier, P.C., Wicki, P., Feldtrauer, J.J., et al. GABA and glutamate release affected by GABAB receptor antagonists with similar potency: No evidence for pharmacologically different presynaptic receptors. Br. J. Pharmacol. 113(4), 1515-1521 (1994).

    2. Davies, C.H., Pozza, M.F., and Collingridge, G.L. CGP 55845A: A potent antagonist of GABAB receptors in the CA1 region of rat hippocampus. Neuropharmacology 32(10), 1071-1073 (1993).

    3. Slattery, D.A., Desrayaud, S., and Cryan, J.F. GABAB receptor antagonist-mediated antidepressant-like behavior is serotonin-dependent. J. Pharmacol. Exp. Ther. 312(1), 290-296 (2005).

    4. LaSarge, C.L., Bañuelos, C., Mayse, J.D., et al. Blockade of GABA(B) receptors completely reverses age-related learning impairment. Neuroscience 164(3), 941-947 (2009).

    5. De Sarro, G., Palma, E., Costa, N., et al. Effects of compounds acting on GABA(B) receptors in the pentylenetetrazole kindling model of epilepsy in mice. Neuropharmacology 39(11), 2147-2161 (2000).