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DOWNLOAD NOWSpantide I is a peptide antagonist of the neurokinin-1 (NK1) receptor (Ki = 177.83 nM).1 It is selective for the NK1 receptor over NK2 and NK3 receptors (Kis = 5,000 and >10,000 nM, respectively). Spantide I induces histamine release from isolated rat mast cells (EC50 = 2.5 µM).2 It inhibits neurokinin B-induced contractions in isolated and perfused guinea pig taenia coli when used at a concentration of 10 µM. Intrathecal administration of spantide I (2 µg/animal) increases the latency to withdrawal in the tail-flick- or hot plate test but also induces hindlimb paralysis in rats.3 Spantide I (36 µg/animal per day for five days) decreases corneal P. aeruginosa levels and polymorphonuclear cell infiltration, reduces corneal Il-1β levels, and increases corneal Il-10 levels in a mouse model of corneal P. aeruginosa infection.4
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1. Pharmacology of CP-
2. Spantide II, a novel tachykinin antagonist having high potency and low histamine-
3. Antinociceptive and neurotoxic actions of substance P analogues in the rat’s spinal cord after intrathecal administration. Neurosci. Lett. 57(2), 159-164 (1985).
4. Spantide I decreases type I cytokines, enhances IL-