Nov 1, 1989

Substance P-induced reduction in the initial accumulation of cytosolic myo-[3H]inositol in rat parotid acinar cells mediated by the NK1 tachykinin receptor

Journal of Neurochemistry
M M DietlJ Glowinski


Stimulation of rat parotid acinar cells by the tachykinin neurokinin (NK) 1 receptor agonist substance P (SP) resulted in a significant reduction in the initial accumulation of cytosolic myo-[3H]inositol. This effect was rapid, because a reduction of approximately 15% could be seen already at 30 s. with the maximal effect (approximately 45%) being observed at 15 min. The response to SP stimulation was temperature dependent, because at 4 degrees C no reduction was found. In addition, at 4 degrees C, cytosolic myo-[3H]inositol represented only 10% of the labeled inositol accumulated at 37 degrees C. The SP-induced reduction in cytosolic myo-[3H]inositol accumulation was concentration dependent; the EC50 obtained for SP was 5.8 +/- 2.5 nM. Spantide [D-Arg1, D-Trp7.9, Leu11]SP), a SP antagonist, used at a concentration of 10(-5) M, gave a competitive shift of the dose-response curve to SP. Various tachykinins and their analogs were evaluated for their ability to reduce cytosolic myo-[3H]inositol. [L-Pro9]SP and SP methyl ester, two highly selective agonists of NK1 receptors, reduced the initial accumulation of myo-[3H]inositol with EC50 values of 2.3 and 67.0 nM, respectively. Long SP C-terminal fragments were more potent than shor...Continue Reading

Mentioned in this Paper

Carboxy-Terminal Amino Acid
Antagonist Muscle Action
Tachykinin Receptor
Synaptic Receptors
Parotid Gland
Analogs & derivatives

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