Venlafaxine HCl - 10mM in DMSO , Norepinephrine transporter inhibitor, CAS No.99300-78-4, Norepinephrine transporter inhibitor

CAS: 99300-78-4 Cat. No.: V408207 Molecular Weight: 313.86 EC Number: 619-421-1 PubChem CID: 62923

GRADE & PURITY 10mM in DMSO

Synonyms

1-(2-(dimethylamino)-1-(4-methoxyphenyl)ethyl)cyclohexanol hydrochloride

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Venlafaxine HCl Venlafaxine HCl is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia.
In vitro

Venlafaxine has a low potential to inhibit the metabolism of substrates for CYP2D6 such as imipramine and desipramine compared with several of the most widely used SSRIs, as well as the metabolism of substrates for several of the other major human hepatic P450s. Venlafaxine inhibits binding to the human norepinephrine (NE) and serotonin (5-HT) transporters with K(i) values of 2480 nM and 82 nM, respectively, and with a K(i) ratio of 30. Venlafaxine has ED(50) values of 5.9 mg/kg and 94 mg/kg for blocking p-chloramphetamine- and 6-hydroxydopamine-induced monoamine depletion, respectively.

In vivo

Venlafaxine induces a dose-dependent antinociceptive effect following i.p. administration with an ED50 of 46.7 mg/kg in mice. Venlafaxine-induced antinociception is significantly inhibited by naloxone, nor-BNI and naltrindole but not by beta-FNA or naloxonazine, implying involvement of kappa1- and delta-opioid mechanisms in mice. Venlafaxine reverses hyperalgesia in rats with a fully developed neuropathic lesion. Venlafaxine also appears to have a mild non-specific analgesic effect that increased paw withdrawal latency (PWL) in the sham limb.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

1-(2-(dimethylamino)-1-(4-methoxyphenyl)ethyl)cyclohexanol hydrochloride

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Venlafaxine HCl is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Mechanism of action

Norepinephrine transporter inhibitor

Names and Identifiers

• Isomeric SMILES: CN(C)CC(C1=CC=C(C=C1)OC)C2(CCCCC2)O.Cl
• WGK Germany: 3
• RTECS: GV8872760
• Alternate CAS: 93413-69-5
• PubChem CID: 62923
• Molecular Weight: 313.86
• Reaxy-Rn: 4240401

Associated Targets(Human)

SLC6A4 Tclin Sodium-dependent serotonin transporter (8 Activities)

Discover Target: SLC6A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Melt Point(°C): 217°C

References

1. Niu Ting, Wei Zhiying, Fu Jiao, Chen Shu, Wang Ru, Wang Yuya, Zheng Ruihe.  (2023)  Venlafaxine, an anti-depressant drug, induces apoptosis in MV3 human melanoma cells through JNK1/2-Nur77 signaling pathway.  Frontiers in Pharmacology,      [PMID:36686679] [10.3389/fphar.2022.1080412]

2. Haibo You, Ben Chen, Liqun Fang, Tingting Lin, Ping Xu, Chu Chu, Shengqiang Tong.  (2022)  Analytical enantioseparation of N-alkyl drugs by reversed-phase liquid chromatography with carboxymethyl-β-cyclodextrin as mobile phase additive.  CHIRALITY,  35  (1): (58-66).  [PMID:36345792] [10.1002/chir.23516]

3. Jun Luo, Yuxuan Dai, Xiaoming Xu, Yazi Liu, Shaogui Yang, Huan He, Cheng Sun, Qiming Xian.  (2021)  Green and efficient synthesis of Co-MOF-based/g-C3N4 composite catalysts to activate peroxymonosulfate for degradation of the antidepressant venlafaxine.  JOURNAL OF COLLOID AND INTERFACE SCIENCE,      [PMID:34922080] [10.1016/j.jcis.2021.11.162]

4. Lisha Jin, Sisi Zhou, Shujie Zhu, Shaowei Lei, Weijuan Du, Huidi Jiang, Su Zeng, Hui Zhou.  (2019)  Dehydrocorydaline induced antidepressant-like effect in a chronic unpredictable mild stress mouse model via inhibiting uptake-2 monoamine transporters.  EUROPEAN JOURNAL OF PHARMACOLOGY,      [PMID:31604070] [10.1016/j.ejphar.2019.172725]

5. Xuesong Liu, Liuliu Cheng, Yehong Han, Mingyu Wang, Hongyuan Yan.  (2024)  Development of a novel second-generation polyester dendritic functionalized graphene oxide for efficient pipette tip micro solid-phase extraction and detection of venlafaxine and desvenlafaxine in urine.  JOURNAL OF CHROMATOGRAPHY A,      [PMID:39647375] [10.1016/j.chroma.2024.465582]

6. Bo Zhao, Guojing Yang, Zhouyun Xie, Ni Zhang, Jingfen Xia, Xuran Liu, Dongbo Wang, Peier Wang, Li Tang.  (2024)  Efficient degradation of venlafaxine using intimately coupled high-active crystal facets exposed TiO2 and biodegradation system: Kinetic studies, biofilm stress behavior and transformation mechanism.  JOURNAL OF ENVIRONMENTAL MANAGEMENT,      [PMID:38759549] [10.1016/j.jenvman.2024.121159]

7. Bin Wang, Yongyue Chen, Wenxuan Li, Yuwei Liu, Xudong Xia, Xia Xu, Yongli Yang, Di Chen.  (2024)  Magnetic phytic acid-modified kapok fiber biochar as a novel sorbent for magnetic solid-phase extraction of antidepressants in biofluids.  ANALYTICA CHIMICA ACTA,      [PMID:38401926] [10.1016/j.aca.2024.342295]

8. Yumei Gan, Linlin Hua, Yuanyuan Zheng, Bin Wang, Di Chen.  (2024)  Natural kapok fiber as a green and efficient adsorbent for in-syringe solid-phase extraction in the determination of antidepressants in biofluids.  MICROCHEMICAL JOURNAL,      [PMID:] [10.1016/j.microc.2024.110638]

9. Zhanwu Li, Bowen Deng, Jiajia Chen, Ru Feng, Shuling Wang, Shu Li, Di Chen, Linlin Hua.  (2025)  One-pot synthesis of magnetic adsorbent with integrated pH regulation for convenient and rapid determination of antidepressant in biofluids.  MICROCHEMICAL JOURNAL,      [PMID:] [10.1016/j.microc.2025.112834]