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DU125530
- Soluble in DMSO
- MF: C23H26ClN3O5S
- MW: 491.99
Description
DU125530 is a high-affinity, selective antagonist of the serotonin 5-HT1A receptor with a Ki value of 0.7 nM. It antagonizes both presynaptic somatodendritic autoreceptors and postsynaptic 5-HT1A receptors with similar low-nanomolar affinity and lacks meaningful intrinsic agonist activity.
DU125530 is used to investigate the contribution of 5-HT1A autoreceptor feedback and postsynaptic signaling to serotonergic neurotransmission. It is particularly useful in neurochemical, receptor-occupancy and behavioral studies involving antidepressant mechanisms, anxiety and cognition.
Key Features
- High-affinity 5-HT1A receptor antagonist
- Ki: 0.7 nM
- Blocks pre- and postsynaptic 5-HT1A receptors
- Minimal intrinsic agonist activity
Applications
- 5-HT1A receptor pharmacology
- Serotonin autoreceptor research
- Neurotransmitter-release studies
- Antidepressant mechanism research
- Anxiety and cognition models
More Information
| Parent CAS No. | 161611-99-0 |
|---|---|
| Chemical Name | 2-[4-[4-(7-Chloro-2,3-dihydro-1,4-benzodioxin-5-yl)-1-piperazinyl]butyl]-1,2-benzisothiazol-3(2H)-one-1,1-dioxide |
| SMILES | C12C(=O)N(CCCCN3CCN(C4C=C(Cl)C=C5OCCOC=45)CC3)S(=O)(=O)C=1C=CC=C2 |
| MFCD | N.A. |
| InChi | InChI=1S/C23H26ClN3O5S/c24-17-15-19(22-20(16-17)31-13-14-32-22)26-11-9-25(10-12-26)7-3-4-8-27-23(28)18-5-1-2-6-21(18)33(27,29)30/h1-2,5-6,15-16H,3-4,7-14H2 |
| InChiKey | LYXKFNHUJJDTIA-UHFFFAOYSA-N |
| CID | 9848499 |
| Short Description | 5-HT1A antagonist |
References
- J Mos et al. The putative 5-HT1A receptor antagonist DU125530 blocks the discriminative stimulus of the 5-HT1A receptor agonist flesinoxan in pigeons. Eur J Pharmacol. 1997 May 1;325(2-3):145-53.
- MC Scorza et al. Preclinical and clinical characterization of the selective 5-HT(1A) receptor antagonist DU-125530 for antidepressant treatment. Br J Pharmacol. 2012 Nov;167(5):1021-34.
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