O-Desmethylvenlafaxine

Modify Date: 2024-01-02 22:00:03

O-Desmethylvenlafaxine structure	Common Name	O-Desmethylvenlafaxine
	CAS Number	93413-62-8	Molecular Weight	263.375
	Density	1.1±0.1 g/cm3	Boiling Point	403.8±25.0 °C at 760 mmHg
	Molecular Formula	C₁₆H₂₅NO₂	Melting Point	208-213ºC
	MSDS	N/A	Flash Point	193.2±21.8 °C
	Symbol	GHS02, GHS06, GHS08	Signal Word	Danger

Use of O-Desmethylvenlafaxine

Desvenlafaxine is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively. Target: SSRIsDesvenlafaxine is a serotonin-norepinephrine reuptake inhibitor and is the active metabolite of the antidepressant venlafaxine. Similar to venlafaxine, desvenlafaxine inhibits the neuronal uptake of serotonin and norepinephrine. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. Desvenlafaxine inhibits [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively. Desvenlafaxine rapidly penetrates the male rat brain and hypothalamus. Desvenlafaxine significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis [1]. Desvenlafaxine has the potential to inhibit CYP2D6, which could result in increased concentrations of drugs metabolized through this pathway. Induction of CYP3A4 is also possible with desvenlafaxine, which could impact the metabolism of drugs metabolized via this enzyme. Desvenlafaxine exhibits a linear and dose-proportional pharmacokinetic single-dose profile in a dose range from 100 to 600 mg/day. The absolute bioavailability of the oral formulation is 80.5% [2].

Name	O-desmethylvenlafaxine
Synonym	More Synonyms

Description	Desvenlafaxine is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively. Target: SSRIsDesvenlafaxine is a serotonin-norepinephrine reuptake inhibitor and is the active metabolite of the antidepressant venlafaxine. Similar to venlafaxine, desvenlafaxine inhibits the neuronal uptake of serotonin and norepinephrine. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. Desvenlafaxine inhibits [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively. Desvenlafaxine rapidly penetrates the male rat brain and hypothalamus. Desvenlafaxine significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis [1]. Desvenlafaxine has the potential to inhibit CYP2D6, which could result in increased concentrations of drugs metabolized through this pathway. Induction of CYP3A4 is also possible with desvenlafaxine, which could impact the metabolism of drugs metabolized via this enzyme. Desvenlafaxine exhibits a linear and dose-proportional pharmacokinetic single-dose profile in a dose range from 100 to 600 mg/day. The absolute bioavailability of the oral formulation is 80.5% [2].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> Serotonin Transporter Research Areas >> Neurological Disease
References	[1]. Deecher, D.C., et al., Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther, 2006. 318(2): p. 657-65. [2]. Sopko, M.A., Jr., M.J. Ehret, and M. Grgas, Desvenlafaxine: another "me too" drug? Ann Pharmacother, 2008. 42(10): p. 1439-46.

Description

Related Catalog

Signaling Pathways >> Neuronal Signaling >> Serotonin Transporter

Research Areas >> Neurological Disease

References

[1]. Deecher, D.C., et al., Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther, 2006. 318(2): p. 657-65.

[2]. Sopko, M.A., Jr., M.J. Ehret, and M. Grgas, Desvenlafaxine: another "me too" drug? Ann Pharmacother, 2008. 42(10): p. 1439-46.

Density	1.1±0.1 g/cm3
Boiling Point	403.8±25.0 °C at 760 mmHg
Melting Point	208-213ºC
Molecular Formula	C₁₆H₂₅NO₂
Molecular Weight	263.375
Flash Point	193.2±21.8 °C
Exact Mass	263.188538
PSA	43.70000
LogP	2.26
Vapour Pressure	0.0±1.0 mmHg at 25°C
Index of Refraction	1.573
Storage condition	-20°C Freezer

O-Desmethylvenlafaxine MSDS(Chinese)

Symbol	GHS02, GHS06, GHS08
Signal Word	Danger
Hazard Statements	H225-H301 + H311 + H331-H370
Precautionary Statements	P210-P260-P280-P301 + P310-P311
Hazard Codes	F,T,Xi
Risk Phrases	11-23/24/25-39/23/24/25-36
Safety Phrases	7-16-36/37-45-26
RIDADR	UN1230 - class 3 - PG 2 - Methanol, solution
RTECS	GV8872620
HS Code	2922509090

Precursor 9
CAS#:93413-61-7 1-[1-(4-Benzylo... CAS#:93413-69-5 Venlafaxine CAS#:1000377-24-1 O-(4-methoxyben... CAS#:99300-78-4 Venlafaxine hyd...
CAS#:918344-20-4 2-(1-hydroxycyc... CAS#:124-40-3 Dimethylamine CAS#:64-18-6 Formic Acid CAS#:93413-56-0 5-(4-Methoxyphe...
CAS#:149289-29-2 N,N,O-Tridesmet...
DownStream 3
CAS#:386750-22-7 Desvenlafaxine ... CAS#:300827-87-6 Desvenlafaxine ... CAS#:448904-47-0 WY 45233 succinate

HS Code	2922509090
Summary	2922509090. other amino-alcohol-phenols, amino-acid-phenols and other amino-compounds with oxygen function. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

Evaluation of the matrix effect of different sample matrices for 33 pharmaceuticals by post-column infusion.

J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 1000 , 84-94, (2015)

Matrix effects that occur during quantitative measurement by liquid chromatography mass spectrometry specifically when using electrospray ionization are a widely recognized phenomenon. Sample matrix c...

Hollow-fiber liquid-phase microextraction and chiral LC-MS/MS analysis of venlafaxine and its metabolites in plasma.

Bioanalysis 5(6) , 721-30, (2013)

An enantioselective analytical method was developed and validated for determination of venlafaxine and its metabolites O-desmethylvenlafaxine and N-desmethylvenlafaxine in plasma samples. The method e...

A poor metabolizer of both CYP2C19 and CYP2D6 identified by mechanistic pharmacokinetic simulation in a fatal drug poisoning case involving venlafaxine.

Forensic Sci. Int. 226(1-3) , e26-31, (2013)

We present a fatal drug poisoning case involving venlafaxine (VEN). The deceased took his medication regularly (including 150 mg VEN twice daily), and nothing in the case or autopsy findings pointed t...

Phenol, 4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]-

desvenlafaxine

O-Desmethylvenlafaxine

L6TJ AYR DQ&1N1&1 AQ

4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenol

4-(2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl)phenol

Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: O-Desmethylvenlafaxine
Price: ￥318.0/5g ￥108.0/1g
Purity: 98.0%
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DC Chemicals Limited
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Dayang Chem (Hangzhou) Co., Ltd.
China
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Purity: 98.0%
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Zhejiang Hangyu API Co., Ltd
China
Product Name: O-Desmethylvenlafaxine
Price: ￥Inquiry/1kg
Purity: 99.5%
Stocking Period: Inquiry
Contact: Vinnie

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O-Desmethylvenlafaxine

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