Home Neuronal Signaling Serotonin Transporter inhibitor Venlafaxine HCl

Venlafaxine HCl

Catalog No.S1441

For research use only.

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.

Venlafaxine HCl Chemical Structure

CAS No. 99300-78-4

Selleck's Venlafaxine HCl has been cited by 2 Publications

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Biological Activity

Description 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.
Targets
5-HT [1]
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. [1] 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. [2]
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. [3] 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. [4]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 313.86
Formula

C17H27NO2·HCl
CAS No. 99300-78-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)CC(C1=CC=C(C=C1)OC)C2(CCCCC2)O.Cl

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04708834 Enrolling by invitation Drug: Troriluzole (BHV-4157) Obsessive Compulsive Disorder Biohaven Pharmaceuticals Inc. March 30 2021 Phase 3
NCT03532477 Recruiting Drug: Venlafaxine Obesity Morbid Norwegian University of Science and Technology|St. Olavs Hospital|Volvat Medisinsk Senter Stokkan|Namsos Hospital|Alesund Hospital November 2 2016 --
NCT02637193 Completed Drug: Venlafaxine|Drug: Moxifloxacin|Drug: Drug - placebo Healthy Subjects Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.|Pfizer December 2015 Phase 1
NCT02005107 Completed Drug: Venlafaxine IR and Venlafaxine XR Roux en Y Gastric Bypass|Sleeve Gastrectomy North Dakota State University|Neuropsychiatric Research Institute Fargo North Dakota December 2013 Phase 4
NCT01867255 Completed Drug: venlafaxine ER (extended-release) 75 mg Bariatric Surgery|Gastric Bypass|Roux-en-Y Gastric Bypass Mayo Clinic October 2013 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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