CGP 55845
Synonym(s):(2S)-3-[[(1S)-1-(3,4-Dichlorophenyl)ethyl]amino-2-hydro xypropyl](phenylmethyl)phosphinic acid hydrochloride;CGP 55845A;CGP55845
- CAS NO.:149184-22-5
- Empirical Formula: C18H23Cl3NO3P
- Molecular Weight: 438.71
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is CGP 55845?
The Uses of CGP 55845
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].
storage
Room temperature
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.
Properties of CGP 55845
storage temp. | room temp |
solubility | DMSO: soluble5mg/mL, clear (warmed) |
form | powder |
color | white to beige |
Safety information for CGP 55845
Computed Descriptors for CGP 55845
New Products
4-Aminotetrahydropyran-4-carbonitrile Hydrochloride (R)-3-Aminobutanenitrile Hydrochloride 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-(Dimethylamino)tetrahydro-2H-pyran-4-carbonitrile 3-((Dimethylamino)methyl)-5-methylhexan-2-one oxalate 1,4-Dioxa-8-azaspiro[4.5]decane 5-Bromo-2-nitropyridine Nimesulide BP Aceclofenac IP/BP/EP Mefenamic Acid IP/BP/EP/USP Diclofenac Sodium IP/BP/EP/USP Ornidazole IP Diclofenac Potassium SODIUM AAS SOLUTION ZINC AAS SOLUTION BUFFER SOLUTION PH 10.0(BORATE) GOOCH CRUCIBLE SINTERED AQUANIL 5 BERYLLIUM AAS SOLUTION 2-Bromo-1-(bromomethyl)-3-chloro-5-nitrobenzene 2-Bromo-3-nitroaniline N-(3-Hydroxypropyl)-N-methylacetamide 3-Bromo-6-chloropyridazine 4-ethyl-3-nitrobenzoic acidRelated products of tetrahydrofuran
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