Serodolin | ß-Arrestin-biased 5-HT7 antagonist
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $80.00 | ||
| 25 mg | $295.00 |
Serodolin (1814929-81-1) is a potent dual antagonist of the serotonin receptors 5-HT7 (Ki = 6.2 nM; IC50 = 5.7 nM cAMP response) and 5-HT2A (Ki = 19 nM; IC50 = 110 nM IP1 response) with significant selectivity over 5-HT1A and 5-HT6.1 Serodolin has recently been found to act as a ß-arrestin-biased inverse agonist on Gs signaling while inducing ERK activation requiring c-SRS activation, a unique pharmacological profile among 5-HT7 ligands.2 It decreased hyperalgesia and pain sensation in response to inflammatory, thermal, and mechanical stimulation in a mouse model demonstrating the therapeutic potential of a ß-arrestin-biased ligand for pain relief. Blood-brain barrier permeable.
References/Citations:
- Deau et al. (2015), Rational Design, Pharmacomodulation, and Synthesis of Dual 5-Hydroxytryptamine 7 (5-HT7)/5-Hydroxytryptamine 2A (5-HT2A) Receptor Antagonists and Evaluation by [18F]-PET Imaging in a Primate Brain; J. Med. Chem. 58 8066
- El Kamlichi et al. (2022), Serodolin, a ß-arrestin-biased ligand of 5-HT7 receptor, attenuates pain-related behaviors; Proc. Natl. Acad. Sci. USA 119 e2118847119
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
Serodolin (1814929-81-1) is a potent dual antagonist of the serotonin receptors 5-HT7 (Ki = 6.2 nM; IC50 = 5.7 nM cAMP response) and 5-HT2A (Ki = 19 nM; IC50 = 110 nM IP1 response) with significant selectivity over 5-HT1A and 5-HT6.1 Serodolin has recently been found to act as a ß-arrestin-biased inverse agonist on Gs signaling while inducing ERK activation requiring c-SRS activation, a unique pharmacological profile among 5-HT7 ligands.2 It decreased hyperalgesia and pain sensation in response to inflammatory, thermal, and mechanical stimulation in a mouse model demonstrating the therapeutic potential of a ß-arrestin-biased ligand for pain relief. Blood-brain barrier permeable.
References/Citations:
- Deau et al. (2015), Rational Design, Pharmacomodulation, and Synthesis of Dual 5-Hydroxytryptamine 7 (5-HT7)/5-Hydroxytryptamine 2A (5-HT2A) Receptor Antagonists and Evaluation by [18F]-PET Imaging in a Primate Brain; J. Med. Chem. 58 8066
- El Kamlichi et al. (2022), Serodolin, a ß-arrestin-biased ligand of 5-HT7 receptor, attenuates pain-related behaviors; Proc. Natl. Acad. Sci. USA 119 e2118847119
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