CGP 25454A

Modify Date: 2024-01-13 11:56:01

CGP 25454A Structure
CGP 25454A structure
Common Name CGP 25454A
CAS Number 104391-26-6 Molecular Weight 346.252
Density N/A Boiling Point N/A
Molecular Formula C15H21Cl2N3O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of CGP 25454A


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.

 Names

Name CGP 25454A
Synonym More Synonyms

 CGP 25454A 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

[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.

 Chemical & Physical Properties

Molecular Formula C15H21Cl2N3O2
Molecular Weight 346.252
Exact Mass 345.101074
Storage condition 2-8℃

 Synonyms

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)
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