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nefazodone + pindolol
- Development stage
- Preclinical
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Nefazodone + pindolol is a combination of two drugs, each with distinct mechanisms of action. Nefazodone is an antidepressant that acts as a serotonin modulator, specifically as an antagonist at type 2 serotonin (5-HT2) receptors and a weak inhibitor of serotonin and norepinephrine reuptake[1][6]. Pindolol is a nonselective beta blocker used primarily for hypertension and angina, but it also has adjunctive use in depression due to its ability to block presynaptic 5-HT1A autoreceptors, which may enhance serotonergic neurotransmission when combined with antidepressants like nefazodone[3][4]. The combination has been studied in treatment-resistant major depressive disorder (TR-MDD), where it was found to be effective in some patients who had not responded to multiple previous antidepressant trials[2].
- Other names
- Dalhousie serotonin cocktail (when combined with tryptophan)
02
Targets
ADRA1A (α1A)HTR2A (Serotonin receptor 5-HT2A)SERT (Sodium-dependent serotonin transporter)HTR2C (5-hydroxytryptamine 2C receptor)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))ADRB1 (β1)NET (Norepinephrine Transporter)
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