THIQ

THIQ maintains low potency at human MC1R, MC3R and MC5R with IC ₅₀ s of 2067, 761, 326 nM and EC ₅₀ s of 2850, 2487, 737 nM, resepectively. THIQ maintains low potency at rat MC3R and MC5R with IC ₅₀ s 1883 and 1575 nM, and EC ₅₀ s of 1325 and >3000 nM, respectively.
THIQ (10 μM; 24 hours) decreases the signal intensity of WT MC4R by approximately 50% whereas increases that of three mutants (N62S, C84R, and C271Y) in HEK293 cells.

THIQ (0.3-10 mg/kg; i.v.) dose-dependently increases erections (ED ₅₀ =0.87 mg/kg) in sexually mature male Sprague Dawley rats. The maximal increase in the number of erections (60%) is detected at 5 mg/kg but was not significantly different from that produced by 1 mg/kg. THIQ (20 mg/kg; p.o.) also produces statistically significant increases in erectile responses with a mean increase of 31±4%.
THIQ treatment shows the t _1/2 is 0.6 hours in Sprague-Dawley rats (1 mg/kg, i.v. and 10 mg/kg, p.o.).