Zalospirone

SKU: orb1819134

Description

Zalospirone is a selective 5-HT1A receptor agonist utilized in neuroscience research. It is applied in both in vitro binding assays and in vivo behavioral models to investigate the pathophysiology and potential treatments for anxiety and depressive disorders.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 114298-18-9
• MW: 419.52
• Purity: >99.99% (May vary between batches)
• Formula: C₂₄H₂₉N₅O₂
• SMILES: O=C1[C@]2([C@]([C@@]3([C@@]4([C@]([C@]2(C=C3)[H])(C=C4)[H])[H])[H])(C(=O)N1CCCCN5CCN(CC5)C=6N=CC=CN6)[H])[H]
• Target: 5-HT Receptor
• Solubility: DMSO:2.1 mg/mL (5.01 mM)

Bioactivity

• In Vivo:
  We report here the results of an antidepressant trial with zalospirone, a novel cyclic imide with 5-HT1A partial agonist activity. Two hundred eighty-seven outpatients (mean age 44 years, 55% men, 45% nonfertile women) who met the criteria for unipolar major depression with a minimum 21-item Hamilton Rating Scale for Depression (HAM-D) score of 20 were randomly assigned to receive 6 weeks of double-blind treatment with either placebo or one of three fixed doses of zalospirone (6, 15, or 45 mg/day), administered three times daily. The high dose (45 mg) of zalospirone produced a significant antidepressant effect compared with the placebo from week 2 with mean improvement (change from baseline) in HAM-D total score of 12.8 versus 8.4 (p < 0.05) at week 6. Clinical improvement with the high dose of zalospirone was consistent across all outcome measures, however, only in the observed cases and not the last-observation-carried-forward analyses. Improvement with the 6-mg or 15-mg doses was greater than that with placebo, but not significantly so, suggesting a dose-response effect. Although the 45-mg dose of zalospirone seemed to have significant antidepressant efficacy, it was not well tolerated.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5HTReceptor, 5HT Receptor, 5-HT1A

Compound Identifiers

PubChem CID

163925