Substance P receptor on parotid cell membranes.
A conjugate (125I-BH-SP) between substance P and 125I-labeled Bolton-Hunter reagent binds reversibly to a single class of high affinity (Kd = 4 nM) binding sites on dispersed rat parotid cells. The total number of binding sites is 49 +/- 17 fmol/mg of protein. The binding affinity of 13 fragments and analogs of substance P correlates with their relative potency in stimulating salivation. The smallest fragment of substance P which exhibits significant binding affinity and saliva-stimulating activity is the COOH-terminal hexa(6-11)peptide. Structurally unrelated neurotransmitters and hormones do not affect the parotid cell binding of 125 I-BH-SP. 125I-BH-SP pre-bound to the cells was recovered mainly in the particulate fractions of the cell homogenate. The 125I-BH-SP binding activity of the parotid cells was inactivated by pretreatment of the cells with papain but not with ribonuclease A or deoxyribonuclease I. Our results suggest that 125I-BH-SP binds to a substance P receptor on parotid membranes and that the receptor, at least in part, may be a protein.
D000818:Animals; D001667:Binding, Competitive; D002462:Cell Membrane / Q000378:metabolism; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D010306:Parotid Gland / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D011956:Receptors, Cell Surface / Q000378:metabolism*; D018040:Receptors, Neurokinin-1; D013329:Structure-Activity Relationship; D013373:Substance P / Q000031:analogs & derivatives / Q000378:metabolism*
D011956:Receptors, Cell Surface; D018040:Receptors, Neurokinin-1; D013373:Substance P