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Cerebrovascular serotonergic receptors mediating vasoconstriction: further evidence for the existence of 5-HT2 receptors in rat and 5-HT1-like receptors in guinea-pig basilar arteries

Chang, J Y and Owman, Christer LU (1989) In Acta Physiologica Scandinavica 136(1). p.59-67
Abstract
Pharmacological experiments were carried out on isolated basilar arteries (BA) from the brain vasculature of guinea-pig and rat in order to characterize post-junctional serotonergic receptors mediating contraction by the use of selective agonists and antagonists. The sensitivity to 5-HT was higher, but the intrinsic activity lower, in guinea-pig compared to rat vessels. The contractile potency of the 5-HT1 agonists, 5-carboxamidotryptamine (5-CT), was three times higher than 5-HT in guinea-pig but 16 times lower in rat BA. In arteries from both species the 5-HT1A agonist, 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT), only caused weak contraction. In rat BA, where the serotonergic contractile receptors are ketanserin-sensitive,... (More)
Pharmacological experiments were carried out on isolated basilar arteries (BA) from the brain vasculature of guinea-pig and rat in order to characterize post-junctional serotonergic receptors mediating contraction by the use of selective agonists and antagonists. The sensitivity to 5-HT was higher, but the intrinsic activity lower, in guinea-pig compared to rat vessels. The contractile potency of the 5-HT1 agonists, 5-carboxamidotryptamine (5-CT), was three times higher than 5-HT in guinea-pig but 16 times lower in rat BA. In arteries from both species the 5-HT1A agonist, 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT), only caused weak contraction. In rat BA, where the serotonergic contractile receptors are ketanserin-sensitive, mesulergine inhibited the contraction in doses high enough to block 5-HT2 receptors, and also propranolol slightly inhibited the contraction, probably due to its binding to these receptors. Methiothepin, a potent antagonist of the 5-HT1-like receptors, affected the contraction in a non-competitive manner. The antagonist profile was different in guinea-pig BA: propranolol was ineffective, mesulergine caused a slight, non-surmountable inhibition, whereas methiothepin acted as a true, competitive antagonist. The data support previous suggestions that the serotonergic contraction in rat BA is mediated by 5-HT2 receptors, whereas the present data show that 5-HT1-like receptors predominate in guinea-pig BA. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Acta Physiologica Scandinavica
volume
136
issue
1
pages
59 - 67
publisher
Wiley-Blackwell
external identifiers
  • pmid:2570505
  • scopus:0024603919
ISSN
0001-6772
language
English
LU publication?
yes
id
5c780e21-071f-4219-96ca-35fd5089ade7 (old id 1104681)
date added to LUP
2008-08-06 13:30:08
date last changed
2017-01-15 04:13:16
@article{5c780e21-071f-4219-96ca-35fd5089ade7,
  abstract     = {Pharmacological experiments were carried out on isolated basilar arteries (BA) from the brain vasculature of guinea-pig and rat in order to characterize post-junctional serotonergic receptors mediating contraction by the use of selective agonists and antagonists. The sensitivity to 5-HT was higher, but the intrinsic activity lower, in guinea-pig compared to rat vessels. The contractile potency of the 5-HT1 agonists, 5-carboxamidotryptamine (5-CT), was three times higher than 5-HT in guinea-pig but 16 times lower in rat BA. In arteries from both species the 5-HT1A agonist, 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT), only caused weak contraction. In rat BA, where the serotonergic contractile receptors are ketanserin-sensitive, mesulergine inhibited the contraction in doses high enough to block 5-HT2 receptors, and also propranolol slightly inhibited the contraction, probably due to its binding to these receptors. Methiothepin, a potent antagonist of the 5-HT1-like receptors, affected the contraction in a non-competitive manner. The antagonist profile was different in guinea-pig BA: propranolol was ineffective, mesulergine caused a slight, non-surmountable inhibition, whereas methiothepin acted as a true, competitive antagonist. The data support previous suggestions that the serotonergic contraction in rat BA is mediated by 5-HT2 receptors, whereas the present data show that 5-HT1-like receptors predominate in guinea-pig BA.},
  author       = {Chang, J Y and Owman, Christer},
  issn         = {0001-6772},
  language     = {eng},
  number       = {1},
  pages        = {59--67},
  publisher    = {Wiley-Blackwell},
  series       = {Acta Physiologica Scandinavica},
  title        = {Cerebrovascular serotonergic receptors mediating vasoconstriction: further evidence for the existence of 5-HT2 receptors in rat and 5-HT1-like receptors in guinea-pig basilar arteries},
  volume       = {136},
  year         = {1989},
}