DICLOFENSINE HYDROCHLORIDE

Investigational

Details

Stereochemistry	RACEMIC
Molecular Formula	C17H17Cl2NO.ClH
Molecular Weight	358.69
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

Cl.COC1=CC=C2C(CN(C)CC2=C1)C3=CC=C(Cl)C(Cl)=C3

InChI

InChIKey=PEHOXCSPLOXNOK-UHFFFAOYSA-N

InChI=1S/C17H17Cl2NO.ClH/c1-20-9-12-7-13(21-2)4-5-14(12)15(10-20)11-3-6-16(18)17(19)8-11;/h3-8,15H,9-10H2,1-2H3;1H

HIDE SMILES / InChI

Molecular Formula	C17H17Cl2NO
Molecular Weight	322.229
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description

Diclofensine is an antidepressant with equipotent inhibitive effects on the neuronal uptake of norepinephrine (NE), serotonin, and dopamine. It is devoid of monoamine-releasing or monoaminoxidase-inhibiting properties. Diclofensine was found to be an effective antidepressant in human trials, with relatively few side effects, but was ultimately dropped from clinical development.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Dopamine transporter 183	Inhibitor 8,504	16.8 nM [IC50]
Norepinephrine transporter 197	Inhibitor 8,504	15.7 nM [IC50]
Serotonin transporter 183	Inhibitor 8,504	51.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Depression 240	Primary		Phase I 438	Unknown

Doses

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Dose	Population	Adverse events
75 mg 1 times / day multiple, oral Studied dose	unhealthy, ADULT	Disc. AE: Agitation, Sweating...

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AEs

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AE	Significance	Dose	Population
Agitation	1 pt Disc. AE	75 mg 1 times / day multiple, oral Studied dose	unhealthy, ADULT
Sweating	1 pt Disc. AE	75 mg 1 times / day multiple, oral Studied dose	unhealthy, ADULT

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Overview

Overview

CYP3A4	CYP2C9	CYP2D6	hERG

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer

Sourcing

Sourcing

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Vendor/Aggregator	ID	URL
001 Chemical	DY100452	https://www.001chemical.com/chem/67165-56-4
AA Blocks	AA006KJ6	https://www.aablocks.com/goods/Goods/detail?id=AA006KJ6
Aaron Chemicals	AR006LAY	http://www.aaronchem.com/67165-56-4
Achemtek	0104-035491	http://www.achemtek.com/67165-56-4
Active Biopharma	ABP000808	http://www.activebiopharma.com/67165-56-4

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PubMed

Title	Date	PubMed
No data available in table

Patents

Sample Use Guides

In Vivo Use Guide

Treatment of depression: a 50 mg daily dose of diclofensine would be sufficient for the majority of the patients. The dosage can be safely increased up to 150 mg daily but this offers few therapeutic advantages.

Route of Administration: Oral

In Vitro Use Guide

Diclofensine, in concentrations of 0.01, 0.1 and 1 uM caused a marked decrease of 3H-DA uptake in rat arcuate-periventricular nucleus-median eminence synaptosomes. Diclofensine (50 uM) caused a 3 fold enhancement of K+-evoked endogenous DA release from tuberoinfundibular dopaminergic (TIDA) neurons.