product name Venlafaxine
Description: Venlafaxine is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), it is used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia. Venlafaxine is a dual serotonin/noradrenalin re-uptake inhibitor that displays ~ 30-fold higher affinity for SERT than NET (Ki values are 82 and 2480 nM respectively).
References: Br J Clin Pharmacol. 1997 Jun;43(6):619-26; Pain. 1996 Nov;68(1):151-5.
313.86
Formula
C17H27NO2·HCl
CAS No.
99300-78-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 55 mg/mL (176.8 mM)
Water: 55 mg/mL (176.8 mM)
Ethanol: 55 mg/mL (176.8 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Br J Clin Pharmacol. 1997 Jun;43(6):619-26; Pain. 1996 Nov;68(1):151-5. |
