Characterization of the substance P receptor on the rat submaxillary gland
Substance P (SP) is an undecapeptide widely distributed in both the central and peripheral nervous systems. Its actions include vasodilation, intestinal contraction, salivation and probably nocioception, effects which are thought to be mediated by receptors. To characterize SP receptors, the binding of (/sup 3/H)SP and (/sup 3/H)physalaemin to rat submaxillary gland membranes and the effects of monovalent cations under conditions in which the peptides are protected from degradation and nonspecific adsorption to the filter were studied. In low ionic strength media (0.3 M sucrose) (/sup 3/H)SP binds to two sites, a high affinity one with an affinity (K/sub D/) = 0.14 nM and a receptor density (B/sub max/) = 370 fmole/mg, and a low affinity-high capacity site with a K/sub D/ = 1400 nM and B/sub max/ = 24,000 fmole/mg. Under these conditions physalaemin, which is about twice as potent as SP as a sialogogue, had one hundredth the potency of SP in competing with (/sup 3/H)SP, with an IC/sub 50/ = 150 nM. The increase in the ionic strength of the binding medium had a profound effect on the binding of (/sup 3/H)SP. The addition of monovalent cations reduced the non specific binding by 90%, abolished the low affinity-high capacity site and decreased the K/sub D/ of (/sup 3/H)SP.
- Research Organization:
- New York Univ., NY (USA)
- OSTI ID:
- 5151408
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
AFFINITY
ANIMALS
CATIONS
CELL CONSTITUENTS
CELL MEMBRANES
CHARGED PARTICLES
CHEMICAL BONDS
CHEMICAL COMPOSITION
CULTURE MEDIA
IONS
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
MAMMALS
MEMBRANES
ORGANIC COMPOUNDS
PEPTIDES
PROTEINS
RATS
RECEPTORS
RODENTS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VALENCE
VERTEBRATES