CGP 25454A


CAS No. : 104391-26-6

CGP 25454A,104391-26-6
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000250
Molecular Formula:C15H21Cl2N3O2
Molecular Weight:346.252
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Cat No:I000250
Cas No:104391-26-6
Product-Name:CGP 25454A
IUPAC Name:4-chloro-5-cyano-N-[2-(diethylamino)ethyl]-2-methoxybenzamide;hydrochloride
InChI:InChI=1S/C15H20ClN3O2.ClH/c1-4-19(5-2)7-6-18-15(20)12-8-11(10-17)13(16)9-14(12)21-3;/h8-9H,4-7H2,1-3H3,(H,18,20);1H
InChIKey:ZETCQNUMZFZSLJ-UHFFFAOYSA-N
SMILES:CCN(CC)CCNC(=O)C1=C(C=C(C(=C1)C#N)Cl)OC.Cl

CGP 25454A is a novel and selective presynaptic dopamine autoreceptor antagonist.
In vitro: CGP 25454A increase the field-stimulated [3H]- and [14C]-overflow from rat striatal slices preloaded with [3H]dopamine and [14C]choline, indicating that CGP 25454A is able to enhance the release of both dopamine (DA) and acetylcholine (ACh). However, CGP 25454A is 12.9 times more potent in increasing, by 1/6 of the apparent maximal increase, the release of [3H]DA than that of [14C]ACh.
In vivo: CGP 25454A increase [3H]spiperone binding to receptors of the D2 family in rat striatum by 90-110% (ED50: 13 mg/kg i.p.). As a similar increase in [3H]spiperone binding is found with a variety of agents which increase the synaptic concentration of endogenous DA, the effect of CGP 25454A most probably reflects an enhanced release of DA under in vivo conditions. At 30-100 mg/kg, CGP 25454A inhibit [3H]spiperone binding in the pituitary of the same animals as a result of a blockade of postsynaptic DA receptors.


[1]. Bischoff S et al. CGP 25454A, a novel and selective presynaptic dopamine autoreceptor antagonist. Naunyn Schmiedebergs Arch Pharmacol. 1994 Sep;350(3):230-8.

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