Diclofensine (hydrochloride)

Modify Date: 2024-01-03 02:27:52

Diclofensine (hydrochloride) Structure
Diclofensine (hydrochloride) structure
Common Name Diclofensine (hydrochloride)
CAS Number 34041-84-4 Molecular Weight 358.690
Density N/A Boiling Point N/A
Molecular Formula C17H18Cl3NO Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Diclofensine (hydrochloride)


Diclofensine(Ro-8-4650) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.IC50 value:Target: Dopamine reuptake inhibitorThe action of diclofensine on peripheral neuronal adrenergic function was studied through tests of the blood pressure response to NE, tyramine, and phenylephrine (PE). The blood pressure response to NE was enhanced and that to tyramine was decreased by diclofensine, as a result of its inhibitive action on peripheral neuronal amine uptake [2]. Diclofensine, in concentrations of 0.01, 0.1 and 1 microM caused a marked decrease of 3H-DA uptake. In addition, it was unable to stimulate basal endogenous DA release which, on the contrary, was elicited by d-amphetamine in the same concentration (50 microM). On the other hand, diclofensine (50 microM) caused a 3 fold enhancement of K+-evoked DA release [3].

 Names

Name Diclofensine Hydrochloride
Synonym More Synonyms

 Diclofensine (hydrochloride) Biological Activity

Description Diclofensine(Ro-8-4650) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.IC50 value:Target: Dopamine reuptake inhibitorThe action of diclofensine on peripheral neuronal adrenergic function was studied through tests of the blood pressure response to NE, tyramine, and phenylephrine (PE). The blood pressure response to NE was enhanced and that to tyramine was decreased by diclofensine, as a result of its inhibitive action on peripheral neuronal amine uptake [2]. Diclofensine, in concentrations of 0.01, 0.1 and 1 microM caused a marked decrease of 3H-DA uptake. In addition, it was unable to stimulate basal endogenous DA release which, on the contrary, was elicited by d-amphetamine in the same concentration (50 microM). On the other hand, diclofensine (50 microM) caused a 3 fold enhancement of K+-evoked DA release [3].
Related Catalog
References

[1]. Hyttel J, et al. Neurochemical profile of Lu 19-005, a potent inhibitor of uptake of dopamine, noradrenaline, and serotonin. J Neurochem. 1985 May;44(5):1615-22.

[2]. Gasic S, et al. Effect of diclofensine, a novel antidepressant, on peripheral adrenergic function. Clin Pharmacol Ther. 1986 May;39(5):582-5.

[3]. Di Renzo G, et al. Pure uptake blockers of dopamine can reduce prolactin secretion: studies with diclofensine. Life Sci. 1988;42(21):2161-9.

 Chemical & Physical Properties

Molecular Formula C17H18Cl3NO
Molecular Weight 358.690
Exact Mass 357.045410
PSA 12.47000
LogP 5.31920
Storage condition 2-8℃

 Synonyms

Isoquinoline, 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-7-methoxy-2-methyl-, hydrochloride
4-(3,4-Dichlorophenyl)-7-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline hydrochloride (1:1)
Isoquinoline, 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-7-methoxy-2-methyl-, hydrochloride (1:1)
4-(3,4-Dichlorophenyl)-7-methoxy-2-methyl-1,2,3,4-tetrahydroisoqu inoline hydrochloride (1:1)
UNII:8U71XY6JQK
Diclofensine (hydrochloride)