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Cat. No. Name Size Price Add Cart
KI0725Venlafaxine hydrochloride25 mg$154
Venlafaxine hydrochloride50 mg$272

Chemical Characteristic

Product NameVenlafaxine hydrochloride
SynonymsWy 4503
CAS No.99300-78-4
Molecular Weight 313.86
FormulaC17H28ClNO2
Chemical Name(+/-)-1-(alpha-((Dimethylamino)methyl)-p-methoxybenzyl)cyclohexanol hydrochloride
SmilesC1(CCCCC1)(O)C(c1ccc(cc1)OC)CN(C)C Cl
Chemical Structure

Biological activities

Venlafaxine hydrochloride is the hydrochloride form of venlafaxine. Venlafaxine is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class. Venlafaxine is a dual serotonin (5-HT) and norepinephrine (NE) transporters reuptake inhibitor with Ki values of 0.2 µM and 82 nM, respectively, and with a Ki ratio of 30. Venlafaxine inhibits ex vivo binding to rat 5-HT transporters and NE transporters with ED50 values of 2 and 54 mg/kg, respectively. Besides, venlafaxine has ED50 values of 5.9 and 94 mg/kg for blocking p-chloramphetamine- and 6-hydroxydopamine-induced monoamine depletion, respectively.[1] Venlafaxine is less potent an inhibitor of imipramine 2-hydroxylation than the other selective serotonin reuptake inhibitors (SSRIs) (including fluoxetine, paroxetine, and fluvoxamine) with a Ki of 41.0 µM.[2] In vivo, daily treatment with venlafaxine (10 mg/kg i.p.) before the operant session attenuates the acquisition of responding for heroin, but not for food in rats.[3] In rats, the mean plasma ratio of (S)-venlafaxine to that of (R)-venlafaxine over 0.5 to 6.0 hours varied from 2.97 to 8.50 with a mean value of 5.51.[4]

Protocols

In vivo: Venlafaxine hydrochloride is dissolved in sterile water.[4]

References

[1] Bymaster FP, et al. Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. Neuropsychopharmacology. 2001, 25(6): 871-880.
[2] Ball SE, et al. Venlafaxine: in vitro inhibition of CYP2D6 dependent imipramine and desipramine metabolism; comparative studies with selected SSRIs, and effects on human hepatic CYP3A4, CYP2C9 and CYP1A2. Br J Clin Pharmacol. 1997, 43(6): 619-626.
[3] Magalas Z, et al. The serotonin/noradrenaline reuptake inhibitor venlafaxine attenuates acquisition, but not maintenance, of intravenous self-administration of heroin in rats. Eur J Pharmacol. 2005, 528(1-3): 103-109.
[4] Wang CP, et al. The disposition of venlafaxine enantiomers in dogs, rats, and humans receiving venlafaxine. Chirality. 1992, 4(2): 84-90.

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