SML3690
Serodolin
≥98% (HPLC)
别名:
1-(5-(4-(4-Fluorophenyl)piperazin-1-yl)pentyl)-1H-benzo[d]imidazol-2(3H)-one, 1-[5-[4-(4-Fluorophenyl)-1-piperazinyl]pentyl]-1,3-dihydro-2H-benzimidazol-2-one
SMILES string
O=C1NC2=C(N1CCCCCN3CCN(CC3)C4=CC=C(C=C4)F)C=CC=C2
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
β-arrestin-biased 5-HT7-selective agonist with antagonist/inverse agonist activity against Gs signaling and in vivo antinociceptive efficacy in mouse pain models.
Serodolin is a β-arrestin-biased, 5-HT7-selective 5-hydroxytryptamine receptor agonist (5HT7/2A/1A/6 Ki = 6.2/19/454/1224 nM) that induces ERK activation through a β-arrestin-dependent signaling mechanism that requires c-SRC activation (309% of basal pErk in 5HT7-transfected HEK293 post 2-15 min 10 μM treatment) while acting as an antagonist/inverse agonist against Gs signaling (IC50 = 14 & 5 nM, respectively, against basal and 10 nM 5-CT-induced cAMP production in 5HT7-transfected HEK293). Serodolin exhibits antinociceptive efficacy in response to inflammatory, thermal, and mechanical stimulation in mice in vivo (0.1-10 mg/kg s.c.).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Rational Design, Pharmacomodulation, and Synthesis of Dual 5-Hydroxytryptamine 7 (5-HT7)/5-Hydroxytryptamine 2A (5-HT2A) Receptor Antagonists and Evaluation by [(18)F]-PET Imaging in a Primate Brain
Journal of medicinal chemistry, 58(20), 8066-8096 (2015)
Chayma El Khamlichi et al.
Proceedings of the National Academy of Sciences of the United States of America, 119(21), e2118847119-e2118847119 (2022-05-21)
G protein–coupled receptors (GPCRs) are involved in regulation of manifold physiological processes through coupling to heterotrimeric G proteins upon ligand stimulation. Classical therapeutically active drugs simultaneously initiate several downstream signaling pathways, whereas biased ligands, which stabilize subsets of receptor conformations
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