For research use only.
CAS No. 99300-78-4
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.
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|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.|
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. |
|In vitro||DMSO||55.5 mg/mL (176.83 mM)|
|Water||55.5 mg/mL (176.83 mM)|
|Ethanol||55.5 mg/mL (176.83 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|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||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|
|NCT02086929||Completed||Drug: Trazodone|Drug: Venlafaxine||Major Depressive Disorder||Aziende Chimiche Riunite Angelini Francesco S.p.A||December 2012||Phase 3|
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