Biological Description
Potent 5-HT2A receptor antagonist (Ki = 7.1 nM for inhibition of [3H] ketanserin binding in rat cortex). Additionally blocks α1-adrenoceptors (Ki values are 5.5 and 84 nM at α1 and α2 respectively). Acts as a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) (Ki values are 220 and 555 nM at rat SERT and NET respectively). Anti-depressant.
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Useful References
Cusack et al (1994) Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 114:559-65. abstract
Owens et al (1997) Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites. J Pharmacol Exp Ther. 283:1305-22. abstract
Taylor et al (1995) Pharmacology and neurochemistry of nefazodone, a novel antidepressant drug. J Clin Psychiatry. 6:3-11. abstract
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Chemical Information
2-[3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-2,4-dihydro-4-(2-phenoxyethyl)-3H-1,2,4-triazol-3-one hydrochloride
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- Desiccate at RT
- MW 506.47
- Soluble in DMSO to 25 mM, in ethanol to 10 mM and in 1eq. HCl to 10 mM
- C25H32ClN5O2.HCl
- 82752-99-6
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