Diclofensine

Modify Date: 2024-01-08 10:06:13

Diclofensine Structure
Diclofensine structure
Common Name Diclofensine
CAS Number 67165-56-4 Molecular Weight 322.229
Density 1.2±0.1 g/cm3 Boiling Point 422.6±45.0 °C at 760 mmHg
Molecular Formula C17H17Cl2NO Melting Point N/A
MSDS N/A Flash Point 209.4±28.7 °C

 Use of Diclofensine


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 4-(3,4-Dichlorophenyl)-7-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline
Synonym More Synonyms

 Diclofensine 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

Density 1.2±0.1 g/cm3
Boiling Point 422.6±45.0 °C at 760 mmHg
Molecular Formula C17H17Cl2NO
Molecular Weight 322.229
Flash Point 209.4±28.7 °C
Exact Mass 321.068726
PSA 12.47000
LogP 4.42
Vapour Pressure 0.0±1.0 mmHg at 25°C
Index of Refraction 1.591
Storage condition 2-8℃

 Safety Information

HS Code 2933499090

 Precursor & DownStream

Precursor  1

DownStream  0

 Customs

HS Code 2933499090
Summary 2933499090. other compounds containing in the structure a quinoline or isoquinoline ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

(±)-4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydro-7-methoxy-2-methylisoquinoline
(±)-4-(3,4-dichlorophenyl)-7-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline
4-(3,4-dichlorophenyl)-7-methoxy-2-methyl-3,4-dihydro-1H-isoquinoline
Isoquinoline, 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-7-methoxy-2-methyl-
Ro 8-4650
Diclofensine
4-(3,4-Dichlorophenyl)-7-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline
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