Vapreotide acetate is a neurokinin-1 (NK1) receptor antagonist, characterized by an IC50 of 330 nM. It attenuates Substance P (SP)-triggered intracellular calcium increases and NF-κB activation, while inhibiting SP-induced IL-8 and MCP-1 production. It also inhibits HIV-1 infection and significantly reduces GH-, PRL, and/or alpha-subunit release from pituitary adenoma cells. The compound exhibits moderate-to-high affinities for SSTR2, -3, and -5.
- Neurokinin-1 (NK1) receptor antagonist.
- Attenuates SP-triggered calcium increases, NF-κB activation.
- Inhibits SP-induced IL-8 and MCP-1 production.
- Inhibits HIV-1 infection; reduces GH, PRL, and alpha-subunit release.
- Moderate-to-high affinities for SSTR2, -3, and -5.
- Can inhibit androgen-independent prostate cancer growth and decrease collateral circulation in cirrhotic rats.