Release of endothelium‐derived hyperpolarizing factor (EDHF) by M3 receptor stimulation in guinea‐pig coronary artery

Anna K.M. Hammarström, Helena C. Parkington, Harold A. Coleman

Research output: Contribution to journalArticleResearchpeer-review

33 Citations (Scopus)

Abstract

The muscarinic receptor subtype(s) involved in the release of endothelium‐derived hyperpolarizing factor (EDHF) were studied in the guinea‐pig coronary artery by recording the membrane potential in the smooth muscle cells with intracellular microelectrodes. Acetylcholine (ACh, pD2 6.68) was 10 times more potent than the M2 agonist, oxotremorine (pD2 5.65) and 500 fold more potent than the M1 agonist, McN‐A‐343 (pD2 3.95) in evoking the EDHF hyperpolarization. The M3 muscarinic antagonist, 4‐diphenylacetoxy‐N‐methylpiperidine methiodide (4‐DAMP) was the most potent (pA2 9.5) in inhibiting the release of EDHF evoked by ACh, being more potent than pirenzepine (pA2 6.7), and AFDX‐116 (pA2 6.1) which preferentially block M1 and M2 receptors, respectively. These results suggest that EDHF is released from the endothelium of the guinea‐pig coronary artery upon the activation of the muscarinic M3 receptor subtype. 1995 British Pharmacological Society

Original languageEnglish
Pages (from-to)717-722
Number of pages6
JournalBritish Journal of Pharmacology
Volume115
Issue number5
DOIs
Publication statusPublished - 1 Jan 1995

Keywords

  • Coronary artery
  • EDHF
  • endothelium
  • hyperpolarization
  • M receptors
  • muscarinic receptors

Cite this

@article{5c4da88c8e3a450695febd3bdc8ed1e4,
title = "Release of endothelium‐derived hyperpolarizing factor (EDHF) by M3 receptor stimulation in guinea‐pig coronary artery",
abstract = "The muscarinic receptor subtype(s) involved in the release of endothelium‐derived hyperpolarizing factor (EDHF) were studied in the guinea‐pig coronary artery by recording the membrane potential in the smooth muscle cells with intracellular microelectrodes. Acetylcholine (ACh, pD2 6.68) was 10 times more potent than the M2 agonist, oxotremorine (pD2 5.65) and 500 fold more potent than the M1 agonist, McN‐A‐343 (pD2 3.95) in evoking the EDHF hyperpolarization. The M3 muscarinic antagonist, 4‐diphenylacetoxy‐N‐methylpiperidine methiodide (4‐DAMP) was the most potent (pA2 9.5) in inhibiting the release of EDHF evoked by ACh, being more potent than pirenzepine (pA2 6.7), and AFDX‐116 (pA2 6.1) which preferentially block M1 and M2 receptors, respectively. These results suggest that EDHF is released from the endothelium of the guinea‐pig coronary artery upon the activation of the muscarinic M3 receptor subtype. 1995 British Pharmacological Society",
keywords = "Coronary artery, EDHF, endothelium, hyperpolarization, M receptors, muscarinic receptors",
author = "Hammarstr{\"o}m, {Anna K.M.} and Parkington, {Helena C.} and Coleman, {Harold A.}",
year = "1995",
month = "1",
day = "1",
doi = "10.1111/j.1476-5381.1995.tb14992.x",
language = "English",
volume = "115",
pages = "717--722",
journal = "British Journal of Pharmacology",
issn = "1476-5381",
publisher = "Wiley-Blackwell",
number = "5",

}

Release of endothelium‐derived hyperpolarizing factor (EDHF) by M3 receptor stimulation in guinea‐pig coronary artery. / Hammarström, Anna K.M.; Parkington, Helena C.; Coleman, Harold A.

In: British Journal of Pharmacology, Vol. 115, No. 5, 01.01.1995, p. 717-722.

Research output: Contribution to journalArticleResearchpeer-review

TY - JOUR

T1 - Release of endothelium‐derived hyperpolarizing factor (EDHF) by M3 receptor stimulation in guinea‐pig coronary artery

AU - Hammarström, Anna K.M.

AU - Parkington, Helena C.

AU - Coleman, Harold A.

PY - 1995/1/1

Y1 - 1995/1/1

N2 - The muscarinic receptor subtype(s) involved in the release of endothelium‐derived hyperpolarizing factor (EDHF) were studied in the guinea‐pig coronary artery by recording the membrane potential in the smooth muscle cells with intracellular microelectrodes. Acetylcholine (ACh, pD2 6.68) was 10 times more potent than the M2 agonist, oxotremorine (pD2 5.65) and 500 fold more potent than the M1 agonist, McN‐A‐343 (pD2 3.95) in evoking the EDHF hyperpolarization. The M3 muscarinic antagonist, 4‐diphenylacetoxy‐N‐methylpiperidine methiodide (4‐DAMP) was the most potent (pA2 9.5) in inhibiting the release of EDHF evoked by ACh, being more potent than pirenzepine (pA2 6.7), and AFDX‐116 (pA2 6.1) which preferentially block M1 and M2 receptors, respectively. These results suggest that EDHF is released from the endothelium of the guinea‐pig coronary artery upon the activation of the muscarinic M3 receptor subtype. 1995 British Pharmacological Society

AB - The muscarinic receptor subtype(s) involved in the release of endothelium‐derived hyperpolarizing factor (EDHF) were studied in the guinea‐pig coronary artery by recording the membrane potential in the smooth muscle cells with intracellular microelectrodes. Acetylcholine (ACh, pD2 6.68) was 10 times more potent than the M2 agonist, oxotremorine (pD2 5.65) and 500 fold more potent than the M1 agonist, McN‐A‐343 (pD2 3.95) in evoking the EDHF hyperpolarization. The M3 muscarinic antagonist, 4‐diphenylacetoxy‐N‐methylpiperidine methiodide (4‐DAMP) was the most potent (pA2 9.5) in inhibiting the release of EDHF evoked by ACh, being more potent than pirenzepine (pA2 6.7), and AFDX‐116 (pA2 6.1) which preferentially block M1 and M2 receptors, respectively. These results suggest that EDHF is released from the endothelium of the guinea‐pig coronary artery upon the activation of the muscarinic M3 receptor subtype. 1995 British Pharmacological Society

KW - Coronary artery

KW - EDHF

KW - endothelium

KW - hyperpolarization

KW - M receptors

KW - muscarinic receptors

UR - http://www.scopus.com/inward/record.url?scp=0029069879&partnerID=8YFLogxK

U2 - 10.1111/j.1476-5381.1995.tb14992.x

DO - 10.1111/j.1476-5381.1995.tb14992.x

M3 - Article

VL - 115

SP - 717

EP - 722

JO - British Journal of Pharmacology

JF - British Journal of Pharmacology

SN - 1476-5381

IS - 5

ER -