Serodolin | ß-Arrestin-biased 5-HT7 antagonist

CAS:
1814929-81-1
Catalog Number:
10-4086
Activity:
ß-Arrestin-biased 5-HT7 antagonist
Chemical Names:
1-(5-(4-(4-Fluorophenyl)piperazin-1-yl)pentyl)-1H-benzo[d]imidazole-2(3H)-one
Molecular Weight:
382.47
Molecular Formula:
C22H27FN4O
Solubility:
Soluble in DMSO (at least 50 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
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:

  1. 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
  2. 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
CAS:
1814929-81-1
Catalog Number:
10-4086
Activity:
ß-Arrestin-biased 5-HT7 antagonist
Chemical Names:
1-(5-(4-(4-Fluorophenyl)piperazin-1-yl)pentyl)-1H-benzo[d]imidazole-2(3H)-one
Molecular Weight:
382.47
Molecular Formula:
C22H27FN4O
Solubility:
Soluble in DMSO (at least 50 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

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

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