312637-48-2
312637-48-2 結(jié)構(gòu)式
基本信息
(R)-N-((R)-1-(4-((1H-1,2,4-三唑-1-基)甲基)-4-環(huán)己基哌啶-1-基)-3-(4-氯苯基 )-1-氧代丙-2-基)-1,2,3,4-四氫異喹啉-3-甲酰胺
N-[(1R)-1-[(4-Chlorophenyl)methyl]-2-[4-cyclohexyl-4-(1H-1,2,4-trazol-1-ylmethyl)-1-piperidinyl]-2-oxoethyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide
(3R)-N-[(1R)-1-[(4-Chlorophenyl)Methyl]-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylMethyl)-1-piperidinyl]-2-oxoethyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxaMide
3-IsoquinolinecarboxaMide, N-[(1R)-1-[(4-chlorophenyl)Methyl]-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylMethyl)-1-piperidinyl]-2-oxoethyl]-1,2,3,4-tetrahydro-, (3R)-
物理化學(xué)性質(zhì)
常見問(wèn)題列表
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.).