化合物 2-FUROYL-LIGRLO-AMIDE TFA
化合物 2-FUROYL-LIGRLO-AMIDE TFA 用途与合成方法
Proteinase-activated receptor 2 (PAR2)
2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH
2
) is equally effective to and 10 to 25 times more potent than SLIGRLNH
2
for increasing intracellular calcium in cultured human and rat PAR2-expressing cells, respectively.
In bioassays of tissue PAR2 activity, measured as arterial vasodilation and hyperpolarization, 2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH
2
) is 10 to 300 times more potent than SLIGRL-NH
2
. Unlike trans-cinnamoyl-LIGRLO-NH
2
, 2-Furoyl-LIGRLO-amide do not cause a prominent non-PAR2-mediated contraction of murine femoral arteries.
Furoyl-LIGRLO-amide TFA (injected intradermally at the nape of the neck; 10 μg; pre-injected) exhibits fewer scratches in response to 2-Furoyl-LIGRLO-amide but not to histamine in Trpv3 -/- mice. But it decreases significantly the number of scratches in WT mice.
| Animal Model: | Adult male (2/3-month-old) Trpv3 -/- and WT mice |
| Dosage: | 10 μg |
| Administration: | Injected intradermally at the nape of the neck |
| Result: | Was involved in PAR2- induced acute itch. |
