CGP 25454A
Names
[ CAS No. ]:
104391-26-6
[ Name ]:
CGP 25454A
[Synonym ]:
Benzamide, 4-chloro-5-cyano-N-[2-(diethylamino)ethyl]-2-methoxy-, hydrochloride (1:1)
4-Chloro-5-cyano-N-[2-(diethylamino)ethyl]-2-methoxybenzamide hydrochloride (1:1)
Biological Activity
[Description]:
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.
[Related Catalog]:
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Molecular Formula ]:
C15H21Cl2N3O2
[ Molecular Weight ]:
346.252
[ Exact Mass ]:
345.101074
[ Storage condition ]:
2-8℃