Comparison of binding assay and biological activity on a NK-1 system with new selective agonists.

Neuropeptides
C TousignantD Regoli

Abstract

Binding sites for the [125I]Bolton-Hunter labeled substance P (BH.SP) were studied in homogenates of rat brain. Binding at 4 degrees C was much lower than at 25 degree C or 37 degrees C, but degradation of the peptide was very important at 37 degrees C. A mixture of peptidases inhibitors (bacitracin 4 x 10(-5) M), chymostatin (2 x 10(-6) M), leupeptin (4 x 10(-6) M), phosphoramidon (4 x 10(-6) M) was needed to stabilize the binding conditions, which were established as follows: BH.SP 40 pM, membrane preparation 1.25 mg/ml, incubation 20 min, temperature 25 degrees C and pH 7.4, in the presence of peptidase inhibitors. Binding occurred rapidly and was maximum at 20 min: it increased linearly with the amount of membranes added. It was saturable and readily reversible. Kd and receptor concentration were respectively 0.4 +/- 0.2 nM and 17 +/- 1 fmol/mg protein. Kd value measured in kinetic studies (0.2 nM) was similar to the one measured by saturation experiments (0.6 nM). Several analogues, homologues or fragments of SP were shown to inhibit BH.SP binding: their relative affinities were compatible with an interaction on a binding site of the type NK-1. This was confirmed with new selective agonists. [Sar9,Met(O2)11]SP, the NK-1 se...Continue Reading

References

Nov 4, 1986·European Journal of Pharmacology·C M LeeL L Iversen
Jan 12, 1987·Life Sciences·D RegoliP D'Orléans-Juste
Aug 21, 1980·Nature·M R HanleyR Wade
Sep 1, 1982·Journal of Medicinal Chemistry·B E Sandberg, L L Iversen
Apr 1, 1983·Journal of Neurochemistry·A VigerJ Glowinski
Jul 1, 1984·Regulatory Peptides·S P Watson, L L Iversen
Apr 1, 1964·British Journal of Pharmacology and Chemotherapy·H P RANG

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