Aviptadilacetate是一种内源性的血管活性肠多肽(VIP)，可从小肠的粘膜中分离，具有强的血管舒张作用。Aviptadilacetate诱导肺血管扩张，抑制血管SMCs增殖、血小板聚集。Aviptadilacetate可用于肺纤维化、肺动脉高压(PAH)、SARS-CoV-2引起呼吸衰竭等的研究。
Aviptadil acetate is an endogenous vasoactive intestinal polypeptide (VIP) isolated from mucous membrane of small intestin, has potent vasodilatory effects. Aviptadil acetate induces pulmonary vasodilation and inhibits vascular SMCs proliferation, platelet aggregation. Aviptadil acetate can be used for the research of pulmonary fibrosis, pulmonary arterial hypertension (PAH) and SARS-CoV-2 caused respiratory failure, et al[1].
Aviptadil acetate 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[3].Aviptadil acetate (1 nM-10 μM) produces a concentration-dependent inhibition of CSE-induced cell death in L2 cells. At 10 μM, Aviptadil acetate reduces CSE-stimulated MMP activity and caspase-3 activation in L2 cells[1].Aviptadil acetate (10 nM-100 μM) attenuates lipopolisaccharide (LPS)-induced MMP-9 activity and its expression by alveolar macrophages (AM) in rats[3].
Aviptadil acetate (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. LD50 of Aviptadil is >10 mg/kg in males, females and male and female combined after 24 hours and 14 days[3].Aviptadil acetate (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[3].Nose-only inhalation exposure of CD1 mice to aerosolized.Aviptadil acetate 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[3].
[1]. Intravenous Aviptadil for Critical COVID-19 With Respiratory Failure (COVID-AIV) [2]. Jian Hu, et al. Novel Targets of Drug Treatment for Pulmonary Hypertension. Am J Cardiovasc Drugs [3]. INVESTIGATOR'S BROCHURE Sponsor: NeuroRx, Inc
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