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Two bradykinin binding sites with picomolar affinities.
J Pharmacol Exp Ther. 1986 May; 237(2):504-12.JP

Abstract

Bradykinin (BK) and related peptides exert a wide range of effects on several organ systems. We have attempted to sort out these effects by studying the binding interaction of [3H]BK at the membrane level with in vitro receptor binding techniques. High specific activity [3H]BK and an enzyme inhibitor "cocktail" has enabled us to label two BK binding sites with different affinity and peptide specificity in several guinea-pig tissues. In the guinea-pig ileum the high-affinity site has an equilibrium dissociation constant (Kd) for [3H]BK of 13 pM and a maximal number of binding sites of 8.3 pmol/g of tissue wet weight. The low-affinity guinea-pig ileum site displays a Kd of 910 pM, a maximum number of binding sites of 14 pmol/g of tissue wet weight and shows a greater selectivity for BK analogs over Lysyl-BK analogs. Two similar sites can also be discriminated in kidney and heart. The potencies of a series of BK analogs at the high-affinity guinea-pig ileum site correlate well with their potencies in contracting ileal smooth muscle. The binding of [3H]BK in the guinea-pig ileum is inhibited by physiological concentrations of monovalent and divalent cations.

Authors

No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

2871174

Citation

Manning, D C., et al. "Two Bradykinin Binding Sites With Picomolar Affinities." The Journal of Pharmacology and Experimental Therapeutics, vol. 237, no. 2, 1986, pp. 504-12.
Manning DC, Vavrek R, Stewart JM, et al. Two bradykinin binding sites with picomolar affinities. J Pharmacol Exp Ther. 1986;237(2):504-12.
Manning, D. C., Vavrek, R., Stewart, J. M., & Snyder, S. H. (1986). Two bradykinin binding sites with picomolar affinities. The Journal of Pharmacology and Experimental Therapeutics, 237(2), 504-12.
Manning DC, et al. Two Bradykinin Binding Sites With Picomolar Affinities. J Pharmacol Exp Ther. 1986;237(2):504-12. PubMed PMID: 2871174.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Two bradykinin binding sites with picomolar affinities. AU - Manning,D C, AU - Vavrek,R, AU - Stewart,J M, AU - Snyder,S H, PY - 1986/5/1/pubmed PY - 1986/5/1/medline PY - 1986/5/1/entrez SP - 504 EP - 12 JF - The Journal of pharmacology and experimental therapeutics JO - J Pharmacol Exp Ther VL - 237 IS - 2 N2 - Bradykinin (BK) and related peptides exert a wide range of effects on several organ systems. We have attempted to sort out these effects by studying the binding interaction of [3H]BK at the membrane level with in vitro receptor binding techniques. High specific activity [3H]BK and an enzyme inhibitor "cocktail" has enabled us to label two BK binding sites with different affinity and peptide specificity in several guinea-pig tissues. In the guinea-pig ileum the high-affinity site has an equilibrium dissociation constant (Kd) for [3H]BK of 13 pM and a maximal number of binding sites of 8.3 pmol/g of tissue wet weight. The low-affinity guinea-pig ileum site displays a Kd of 910 pM, a maximum number of binding sites of 14 pmol/g of tissue wet weight and shows a greater selectivity for BK analogs over Lysyl-BK analogs. Two similar sites can also be discriminated in kidney and heart. The potencies of a series of BK analogs at the high-affinity guinea-pig ileum site correlate well with their potencies in contracting ileal smooth muscle. The binding of [3H]BK in the guinea-pig ileum is inhibited by physiological concentrations of monovalent and divalent cations. SN - 0022-3565 UR - https://www.unboundmedicine.com/medline/citation/2871174/Two_bradykinin_binding_sites_with_picomolar_affinities_ L2 - https://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=2871174 DB - PRIME DP - Unbound Medicine ER -