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| CGP 55845 Basic information |
| Product Name: | CGP 55845 | | Synonyms: | CGP 55845;(2S)-3-[[(1S)-1-(3,4-Dichlorophenyl)ethyl]amino-2-hydroxypropyl](phenylmethyl)phosphinicacidhydrochloride;CGP 55845 hydrochloride;(2S)-3-[[(1S)-1-(3,4-DICHLOROPHENYL)ETHYL]AMINO-2-HYDROXYPROPYL](PHENYLMETHYL)PHOSPHINIC ACID;benzyl-[(2S)-3-[[(1S)-1-(3,4-dichlorophenyl)ethyl]amino]-2-hydroxypropyl]phosphinic acid;CGP 55845 hydrochlor | | CAS: | 149184-22-5 | | MF: | C18H23Cl3NO3P | | MW: | 438.71 | | EINECS: | | Product Categories: | GABA/Glycine receptor | | Mol File: | 149184-22-5.mol |
| CGP 55845 Chemical Properties |
| storage temp. | room temp | | solubility | DMSO: soluble5mg/mL, clear (warmed) | | form | powder | | color | white to beige |
| WGK Germany | 3 | | RTECS | SZ4680000 |
| CGP 55845 Usage And Synthesis |
| 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 | | 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. |
| CGP 55845 Preparation Products And Raw materials |
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