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Bradykinin receptor types and B2 subtypes.
Life Sci. 1994; 55(10):735-49.LS

Abstract

Bradykinin, desArg9BK, some agonist analogues and several antagonists have been tested in isolated organs in order to identify bradykinin B2 receptor subtypes. The initial pharmacological characterization was made in the rabbit jugular vein and the guinea pig ileum, two widely used B2 preparations which have shown marked differences in their sensitivities to both agonists and antagonists. The study has then been extended to peripheral tissues (stomach, colon, urinary bladder) of four species (the rat, guinea pig, rabbit and man) and to isolated vessels (rabbit jugular vein, rabbit vena cava, guinea pig pulmonary artery, rat portal vein) in order to determine if pharmacologic receptor subtypes may be related to species. It has been shown that B2 receptors in rat and guinea pig tissues belong to a similar pharmacological entity, a receptor which is different from that mediating the responses of rabbit and human tissues. Agonists order of potency ([Hyp3]BK > BK > [Aib7]BK) obtained in the rabbit jugular vein is different from that found in the guinea pig ileum (BK < or = [Aib7]BK > [Hyp3]BK). Affinities of competitive antagonists (for instance DArg[Hyp3,DPhe7,Leu8]BK) in rabbit tissues are higher than in guinea pig and rat tissues by at least 2 log units, while the non peptidic compound WIN 64338 is more active (also by two log units) in guinea pig than in human and rabbit tissues. The non competitive long-acting antagonist HOE 140 is very potent and equally active in the four species. Some antagonists (peptides without unnatural residues, peptides with unnatural residues, non peptides) have been shown to be specific for kinin receptors and selective for the B2. Altogether, the present results a) confirm the existence of two B2 receptor subtypes, b) suggest that receptor subtypes may be species dependent and c) indicate that the B2 receptor subtype found in the rabbit is similar to that found in man.

Authors+Show Affiliations

Department of Pharmacology, Medical School Université de Sherbrooke, Québec, Canada.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't
Review

Language

eng

PubMed ID

8072371

Citation

Regoli, D, et al. "Bradykinin Receptor Types and B2 Subtypes." Life Sciences, vol. 55, no. 10, 1994, pp. 735-49.
Regoli D, Gobeil F, Nguyen QT, et al. Bradykinin receptor types and B2 subtypes. Life Sci. 1994;55(10):735-49.
Regoli, D., Gobeil, F., Nguyen, Q. T., Jukic, D., Seoane, P. R., Salvino, J. M., & Sawutz, D. G. (1994). Bradykinin receptor types and B2 subtypes. Life Sciences, 55(10), 735-49.
Regoli D, et al. Bradykinin Receptor Types and B2 Subtypes. Life Sci. 1994;55(10):735-49. PubMed PMID: 8072371.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Bradykinin receptor types and B2 subtypes. AU - Regoli,D, AU - Gobeil,F, AU - Nguyen,Q T, AU - Jukic,D, AU - Seoane,P R, AU - Salvino,J M, AU - Sawutz,D G, PY - 1994/1/1/pubmed PY - 1994/1/1/medline PY - 1994/1/1/entrez SP - 735 EP - 49 JF - Life sciences JO - Life Sci VL - 55 IS - 10 N2 - Bradykinin, desArg9BK, some agonist analogues and several antagonists have been tested in isolated organs in order to identify bradykinin B2 receptor subtypes. The initial pharmacological characterization was made in the rabbit jugular vein and the guinea pig ileum, two widely used B2 preparations which have shown marked differences in their sensitivities to both agonists and antagonists. The study has then been extended to peripheral tissues (stomach, colon, urinary bladder) of four species (the rat, guinea pig, rabbit and man) and to isolated vessels (rabbit jugular vein, rabbit vena cava, guinea pig pulmonary artery, rat portal vein) in order to determine if pharmacologic receptor subtypes may be related to species. It has been shown that B2 receptors in rat and guinea pig tissues belong to a similar pharmacological entity, a receptor which is different from that mediating the responses of rabbit and human tissues. Agonists order of potency ([Hyp3]BK > BK > [Aib7]BK) obtained in the rabbit jugular vein is different from that found in the guinea pig ileum (BK < or = [Aib7]BK > [Hyp3]BK). Affinities of competitive antagonists (for instance DArg[Hyp3,DPhe7,Leu8]BK) in rabbit tissues are higher than in guinea pig and rat tissues by at least 2 log units, while the non peptidic compound WIN 64338 is more active (also by two log units) in guinea pig than in human and rabbit tissues. The non competitive long-acting antagonist HOE 140 is very potent and equally active in the four species. Some antagonists (peptides without unnatural residues, peptides with unnatural residues, non peptides) have been shown to be specific for kinin receptors and selective for the B2. Altogether, the present results a) confirm the existence of two B2 receptor subtypes, b) suggest that receptor subtypes may be species dependent and c) indicate that the B2 receptor subtype found in the rabbit is similar to that found in man. SN - 0024-3205 UR - https://www.unboundmedicine.com/medline/citation/8072371/Bradykinin_receptor_types_and_B2_subtypes_ L2 - https://linkinghub.elsevier.com/retrieve/pii/0024-3205(94)00557-5 DB - PRIME DP - Unbound Medicine ER -