d‐Arg[Hyp3‐Thi5‐d‐Tic7‐Tic8]‐bradykinin, a potent antagonist of smooth muscle BK2 receptors and BK3 receptors

S. G. Farmer; R. M. Burch; D. J. Kyle; J. A. Martin; S. N. Meeker; J. Togo

doi:10.1111/j.1476-5381.1991.tb12251.x

d‐Arg[Hyp³‐Thi⁵‐d‐Tic⁷‐Tic⁸]‐bradykinin, a potent antagonist of smooth muscle BK₂ receptors and BK₃ receptors

S. G. Farmer, R. M. Burch, D. J. Kyle, J. A. Martin, S. N. Meeker, J. Togo

Research output: Contribution to journal › Article › peer-review

39 Scopus citations

Abstract

d‐Arg[Hyp³‐Thi⁵‐d‐Tic⁷‐Tic⁸]‐bradykinin (NPC 16731) inhibited bradykinin (BK) binding and BK‐induced contraction in guinea‐pig ileum, being markedly more potent than d‐Phe⁷‐BK analogues as a BK₂ receptor antagonist. In isolated trachea NPC 16731, unlike other BK₂ antagonists, inhibited BK binding and BK‐induced contraction, and ⁴⁵Ca²⁺ efflux in tracheal smooth muscle cells. That NPC 16731 potently inhibits BK effects in trachea provides further evidence for the existence of the airway BK₃ receptor. 1991 British Pharmacological Society

Original language	English (US)
Pages (from-to)	785-787
Number of pages	3
Journal	British Journal of Pharmacology
Volume	102
Issue number	4
DOIs	https://doi.org/10.1111/j.1476-5381.1991.tb12251.x
State	Published - Apr 1991
Externally published	Yes

Keywords

BK receptor
BK receptor
Bradykinin
Ca efflux
antagonist
bradykinin binding
contraction
ileum
smooth muscle
trachea

ASJC Scopus subject areas

Pharmacology

Access to Document

10.1111/j.1476-5381.1991.tb12251.x

Cite this

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title = "d‐Arg[Hyp3‐Thi5‐d‐Tic7‐Tic8]‐bradykinin, a potent antagonist of smooth muscle BK2 receptors and BK3 receptors",

abstract = "d‐Arg[Hyp3‐Thi5‐d‐Tic7‐Tic8]‐bradykinin (NPC 16731) inhibited bradykinin (BK) binding and BK‐induced contraction in guinea‐pig ileum, being markedly more potent than d‐Phe7‐BK analogues as a BK2 receptor antagonist. In isolated trachea NPC 16731, unlike other BK2 antagonists, inhibited BK binding and BK‐induced contraction, and 45Ca2+ efflux in tracheal smooth muscle cells. That NPC 16731 potently inhibits BK effects in trachea provides further evidence for the existence of the airway BK3 receptor. 1991 British Pharmacological Society",

keywords = "BK receptor, BK receptor, Bradykinin, Ca efflux, antagonist, bradykinin binding, contraction, ileum, smooth muscle, trachea",

author = "Farmer, {S. G.} and Burch, {R. M.} and Kyle, {D. J.} and Martin, {J. A.} and Meeker, {S. N.} and J. Togo",

year = "1991",

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doi = "10.1111/j.1476-5381.1991.tb12251.x",

language = "English (US)",

volume = "102",

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journal = "British Journal of Pharmacology",

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publisher = "Wiley-Blackwell",

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TY - JOUR

T1 - d‐Arg[Hyp3‐Thi5‐d‐Tic7‐Tic8]‐bradykinin, a potent antagonist of smooth muscle BK2 receptors and BK3 receptors

AU - Farmer, S. G.

AU - Burch, R. M.

AU - Kyle, D. J.

AU - Martin, J. A.

AU - Meeker, S. N.

AU - Togo, J.

PY - 1991/4

Y1 - 1991/4

N2 - d‐Arg[Hyp3‐Thi5‐d‐Tic7‐Tic8]‐bradykinin (NPC 16731) inhibited bradykinin (BK) binding and BK‐induced contraction in guinea‐pig ileum, being markedly more potent than d‐Phe7‐BK analogues as a BK2 receptor antagonist. In isolated trachea NPC 16731, unlike other BK2 antagonists, inhibited BK binding and BK‐induced contraction, and 45Ca2+ efflux in tracheal smooth muscle cells. That NPC 16731 potently inhibits BK effects in trachea provides further evidence for the existence of the airway BK3 receptor. 1991 British Pharmacological Society

AB - d‐Arg[Hyp3‐Thi5‐d‐Tic7‐Tic8]‐bradykinin (NPC 16731) inhibited bradykinin (BK) binding and BK‐induced contraction in guinea‐pig ileum, being markedly more potent than d‐Phe7‐BK analogues as a BK2 receptor antagonist. In isolated trachea NPC 16731, unlike other BK2 antagonists, inhibited BK binding and BK‐induced contraction, and 45Ca2+ efflux in tracheal smooth muscle cells. That NPC 16731 potently inhibits BK effects in trachea provides further evidence for the existence of the airway BK3 receptor. 1991 British Pharmacological Society

KW - BK receptor

KW - Bradykinin

KW - Ca efflux

KW - antagonist

KW - bradykinin binding

KW - contraction

KW - ileum

KW - smooth muscle

KW - trachea

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