150175-54-5
Chemical Structure
CGP55845
- CAS No.: 150175-54-5
- Formula:C18H22Cl2NO3P
- Molecular Weight:402.25
IUPAC Name: benzyl((S)-3-(((S)-1-(3,4-dichlorophenyl)ethyl)amino)-2-hydroxypropyl)phosphinic acid
InChIKey: ZODSPDOOCZZEIM-BBRMVZONSA-N
SMILES: O=P(CC1=CC=CC=C1)(C[C@@H](O)CN[C@H](C2=CC=C(Cl)C(Cl)=C2)C)O
Biological Activity: CGP55845 is a selective GABAB receptor competitive antagonist (IC50 = 5 nM). CGP55845 prevents agonist binding (pKi = 8.35). CGP55845 blocks presynaptic GABAB receptors, relieves the inhibition of GABA release, and blocks GABAB-mediated inhibitory signaling. CGP55845 restores long-term potentiation and novel object recognition memory in knockout mice[1][2][3][4][5].
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CGP55845 | CGP55845 is a selective GABAB receptor competitive antagonist (IC50 = 5 nM). CGP55845 prevents agonist binding (pKi = 8.35). CGP55845 blocks presynaptic GABAB receptors, relieves the inhibition of GABA release, and blocks GABAB-mediated inhibitory signaling. CGP55845 restores long-term potentiation and novel object recognition memory in knockout mice. | |||||||||||||||||||||
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References
- [1]. Kirmse K, et al. Ambient GABA constrains the strength of GABAergic synapses at Cajal-Retzius cells in the developing visual cortex. The Journal of neuroscience : the official journal of the Society for Neuroscience. 2006 Apr 19;26(16):4216-27. [Content Brief]
- [2]. Gennaccaro L, et al. A GABAB receptor antagonist rescues functional and structural impairments in the perirhinal cortex of a mouse model of CDKL5 deficiency disorder. Neurobiol Dis. 2021 Jun;153:105304. [Content Brief]
- [3]. Brugger F, et al. The action of new potent GABAB receptor antagonists in the hemisected spinal cord preparation of the rat. Eur J Pharmacol. 1993 Apr 22;235(1):153-5. [Content Brief]
- [4]. Salio C, et al. GABA receptors-mediated tonic inhibition of glutamate release from Aβ fibers in rat laminae III/IV of the spinal cord dorsal horn. Molecular pain. 2017;13:1744806917710041. [Content Brief]
- [5]. Mott DD, et al. GABAB-Receptor-mediated currents in interneurons of the dentate-hilus border. J Neurophysiol. 1999 Sep;82(3):1438-50.
