| Identification | Back Directory | [Name]
CGP 55845 | [CAS]
149184-22-5 | [Synonyms]
CGP 55845
CGP 55845 hydrochlor
CGP 55845 hydrochloride
benzyl-[(2S)-3-[[(1S)-1-(3,4-dichlorophenyl)ethyl]amino]-2-hydroxypropyl]phosphinic acid
(2S)-3-[[(1S)-1-(3,4-DICHLOROPHENYL)ETHYL]AMINO-2-HYDROXYPROPYL](PHENYLMETHYL)PHOSPHINIC ACID
(2S)-3-[[(1S)-1-(3,4-Dichlorophenyl)ethyl]amino-2-hydroxypropyl](phenylmethyl)phosphinicacidhydrochloride | [Molecular Formula]
C18H22Cl2NO3P | [MOL File]
149184-22-5.mol | [Molecular Weight]
402.25 |
| Hazard Information | Back Directory | [Uses]
CGP is a potent, selectie GABAB receptor antagonist. | [Biological Activity]
Potent, selective GABA B receptor antagonist (IC 50 = 5 nM) that prevents agonist binding (pK i = 8.35) and inhibits GABA and glutamate release (pEC 50 values are 8.08 and 7.85 respectively). Inhibits GABA B responses to baclofen (IC 50 = 130 nM in an isoproterenol assay) and potentiates the hypoglycemic response to glucose in vitro . | [Biochem/physiol Actions]
CGP 55845 is a potent selective GABA-B receptor antagonist with an IC50 of 5 nM. | [in vitro]
antagonist cgp 55845a of the gabab receptor in the presence of cnqx and d(2)-2-amino-5-phosphonovaleric acid prevented the inhibitory postsynaptic potential-b and paired-pulse depression. [3]. | [IC 50]
5 nm | [storage]
Store at RT | [References]
[1] waldmeier pc, wicki p, feldtrauer jj, mickel sj, bittiger h, baumann pa. gaba and glutamate release affected by gabab receptor antagonists with similar potency: no evidence for pharmacologically different presynaptic receptors. br j pharmacol. 1994 dec;113(4):1515-21.
[2] cunningham md, enna sj. evidence for pharmacologically distinct gabab receptors associated with camp production in rat brain. brain res. 1996 may 13;720(1-2):220-4.
[3] deisz ra. the gaba(b) receptor antagonist cgp 55845a reduces presynaptic gaba(b) actions in neocortical neurons of the rat in vitro. neuroscience. 1999;93(4):1241-9.
[4] zhang m, buttigieg j, nurse ca. neurotransmitter mechanisms mediating low-glucose signalling in cocultures and fresh tissue slices of rat carotid body. j physiol. 2007 feb 1;578(pt 3):735-50. epub 2006 nov 23.
[5] salah a, perkins kl. effects of subtype-selective group i mglur antagonists on synchronous activity induced by 4-aminopyridine/cgp 55845 in adult guinea pig hippocampal slices. neuropharmacology. 2008 jul;55(1):47-54. doi: 10.1016/j.neuropharm.2008.04.010. epub 2008 apr 23. |
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