UCSF678 HYDROCHLORIDE，25MG，SML3396-25MG，Sigma

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.