For research use only. Not Intended for Therapeutic Use!
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Vapreotide, a synthetic analog of somatostatin, has NK1R antagonist activity.
In vitro: Vapreotide has NK1R antagonist activity. Vapreotide attenuates SP-triggered intracellular calcium increases and NF-κB activation in a dose-dependent manner. Vapreotide also inhibits SP-induced IL-8 and MCP-1 production in HEK293-NK1R and U373MG cell lines. Vapreotide inhibits HIV-1 infection of human MDM in vitro, an effect that is reversible by SP pretreatment.
In vivo: Vapreotide decreases portal pressure and blood flow of collateral circulation in rats with cirrhosis. Vapreotide administrated via the intravenous route is simple to use, with practically no contraindications and few, usually minor, side effects.
. Spitsin S et al. Analog of somatostatin vapreotide exhibits biological effects in vitro via interaction with neurokinin-1 receptor. Neuroimmunomodulation. 2013;20(5):247-55.