醋酸阿肽地尔

GPR14

Aviptadil inhibits the basal proliferation of pulmonary arterial smooth muscle cells (PASMC) and the mobilization of intracellular free calcium concentration in these cells in a dose-dependent manner.Aviptadil (1 nM-10 μM) produces a concentration-dependent inhibition of CSE-induced cell death in L2 cells. At 10 μM, Aviptadil reduces CSE-stimulated MMP activity and caspase-3 activation in L2 cells.Aviptadil (10 nM-100 μM) attenuates lipopolisaccharide (LPS)-induced MMP-9 activity and its expression by alveolar macrophages (AM) in rats.

Aviptadil (1, 3 and 10 mg/kg; intravenous bolus injection) is injected into a tail vein. No-effect dose level is 1 mg/kg. Dose level with first intolerance reactions 3 mg/kg, Lowest lethal dose level is >10 mg/kg. i.v. LD ₅₀ of Aviptadil is >10 mg/kg in males, females and male and female combined after 24 hours and 14 days.Aviptadil (intravenous bolus injection) at 3 mg causes slightly reduced motility, slight ataxia and slight dyspnoea in all 5 male and 5 female animals 15 to 30 minutes after administration. At 10 mg, Aviptadil reveals slightly reduced motility, slight ataxia, and slight dyspnoea 15 to 60 minutes and slightly reduces muscle tone 15 to 30 minutes after administration, respectively, in all male and female animals.Nose-only inhalation exposure of CD1 mice to aerosolized.Aviptadil at a dose of 1546 µg/kg/day is well tolerated and produces no apparent changes in any of the parameters evaluated. No changes are observed after a single dose administration as high as 3920 µg/kg/day. The no-observable-adverse-effect level (NOAEL) is considered to be at least 3920 µg/kg/day fore an acute exposure and 1546 µg/kg/day for a 10 day repeated exposure.