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Upregulation of a non-ETA receptor in human arteries in vitro

Adner, Mikael LU ; Erlinge, David LU ; Nilsson, Lars and Edvinsson, Leif (1995) In Journal of Cardiovascular Pharmacology 26(Suppl. 3). p.314-316
Abstract
Receptor turnover may be a crucial part in the physiology of endothelin (ET). Incubation of vessel segments could be a possible method to demonstrate this. The aim was to study contractile responses of human omental arteries to different ET agonists at various periods after incubation at 37 degrees C in 5% CO2 and air. The maximum effect (Emax; percentage of contraction to 60 mM K+ buffer solution) and the potency of ET-1 were unaltered (pD2 = 8.82 +/- 0.06). The selective ETB agonist IRL 1620 demonstrated a negligible Emax in nonincubated segments (2.4 +/- 0.9%). After only 1 day of incubation the Emax was 51 +/- 23%, and it reached 114 +/- 53% after 5 days. The pD2 of IRL 1620 was stable throughout the incubation time (7.23 +/- 0.08).... (More)
Receptor turnover may be a crucial part in the physiology of endothelin (ET). Incubation of vessel segments could be a possible method to demonstrate this. The aim was to study contractile responses of human omental arteries to different ET agonists at various periods after incubation at 37 degrees C in 5% CO2 and air. The maximum effect (Emax; percentage of contraction to 60 mM K+ buffer solution) and the potency of ET-1 were unaltered (pD2 = 8.82 +/- 0.06). The selective ETB agonist IRL 1620 demonstrated a negligible Emax in nonincubated segments (2.4 +/- 0.9%). After only 1 day of incubation the Emax was 51 +/- 23%, and it reached 114 +/- 53% after 5 days. The pD2 of IRL 1620 was stable throughout the incubation time (7.23 +/- 0.08). ET-3 showed a moderate Emax in nonincubated segments (55 +/- 18%), with a pD2 of 6.68 +/- 0.24. However, subsequent incubation revealed an increase of pD2 to 8.60 +/- 0.20 on the fifth day. The maximum contraction increased to 206 +/- 44%; this is equal to the contraction obtained in paired experiments with ET-1 (215 +/- 18%). These findings indicate modulation of endothelin receptor expression after incubation of vessel segments, and suggest the gradual appearance of a non-ETA receptor. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Journal of Cardiovascular Pharmacology
volume
26
issue
Suppl. 3
pages
314 - 316
publisher
Lippincott Williams & Wilkins
external identifiers
  • pmid:8587399
ISSN
1533-4023
language
English
LU publication?
yes
id
f19f4e8e-760d-4243-84ae-f0a99a85ede7 (old id 1109146)
date added to LUP
2008-07-25 14:20:57
date last changed
2016-04-15 18:35:05
@article{f19f4e8e-760d-4243-84ae-f0a99a85ede7,
  abstract     = {Receptor turnover may be a crucial part in the physiology of endothelin (ET). Incubation of vessel segments could be a possible method to demonstrate this. The aim was to study contractile responses of human omental arteries to different ET agonists at various periods after incubation at 37 degrees C in 5% CO2 and air. The maximum effect (Emax; percentage of contraction to 60 mM K+ buffer solution) and the potency of ET-1 were unaltered (pD2 = 8.82 +/- 0.06). The selective ETB agonist IRL 1620 demonstrated a negligible Emax in nonincubated segments (2.4 +/- 0.9%). After only 1 day of incubation the Emax was 51 +/- 23%, and it reached 114 +/- 53% after 5 days. The pD2 of IRL 1620 was stable throughout the incubation time (7.23 +/- 0.08). ET-3 showed a moderate Emax in nonincubated segments (55 +/- 18%), with a pD2 of 6.68 +/- 0.24. However, subsequent incubation revealed an increase of pD2 to 8.60 +/- 0.20 on the fifth day. The maximum contraction increased to 206 +/- 44%; this is equal to the contraction obtained in paired experiments with ET-1 (215 +/- 18%). These findings indicate modulation of endothelin receptor expression after incubation of vessel segments, and suggest the gradual appearance of a non-ETA receptor.},
  author       = {Adner, Mikael and Erlinge, David and Nilsson, Lars and Edvinsson, Leif},
  issn         = {1533-4023},
  language     = {eng},
  number       = {Suppl. 3},
  pages        = {314--316},
  publisher    = {Lippincott Williams & Wilkins},
  series       = {Journal of Cardiovascular Pharmacology},
  title        = {Upregulation of a non-ETA receptor in human arteries in vitro},
  volume       = {26},
  year         = {1995},
}