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About This Item
Empirical Formula (Hill Notation):
C15H18N2O2S · xHCl
Molecular Weight:
290.38 (free base basis)
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
H2O: 2 mg/mL, clear (Warmed)
storage temp.
-10 to -25°C
Biochem/physiol Actions
Selective, β-arrestin-biased high-affinity 5-HT5A partial agonist. A superior 5-HT5A probe than the non-selective and lower affinity 5-HT5A antagonist SB-699551.
UCSF678 (5A6-78) is a selective, high-affinity (Ki 41.6 nM) β-arrestin-biased 5-HT5A partial agonist (β-arrestin 2 recruitment Emax at 10 μM = 17% of 5-HT Emax) with only off-target affinity toward 1A/2B/7A among >300 GPCRs (>1 μM). UCSF678 is a superior 5-HT5A probe than the non-selective and lower affinity 5-HT5A antagonist SB-699551. The use of UCSF678 shows that 5-HT5AR engagement is nonessential for alleviating pain in a mouse model of peripheral nerve injury-induced mechanical hypersensitivity, which runs contrary to previous studies using less selective ligands.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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