Analog of Somatostatin Vapreotide Exhibits Biological Effects in vitro via Interaction with Neurokinin-1 Receptor

  title={Analog of Somatostatin Vapreotide Exhibits Biological Effects in vitro via Interaction with Neurokinin-1 Receptor},
  author={Sergei V. Spitsin and Florin Tuluc and John Meshki and Jian Ping Lai and Richard Tustin Iii and Steven D. Douglas},
  pages={247 - 255}
Objectives: Vapreotide, a synthetic analog of somatostatin, has analgesic activity most likely mediated through the blockade of neurokinin-1 receptor (NK1R), the substance P (SP)-preferring receptor. The ability of vapreotide to interfere with other biological effects of SP has yet to be investigated. Methods: We studied the ability of vapreotide to antagonize NK1R in three different cell types: immortalized U373MG human astrocytoma cells, human monocyte-derived macrophages (MDM) and a human… Expand
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Front & Back Matter
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In vitro and in vivo evidence for a tachykinin NK1 receptor antagonist effect of vapreotide, an analgesic cyclic analog of somatostatin.
It is concluded that vapreotide possesses an antagonist activity on guinea-pig tachykinin NK1 receptors; the involvement in its analgesic action is discussed. Expand
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