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Serotonergic agonists behave as partial agonists at the dopamine D2 receptor

Rinken, A; Ferre, S; Terasmaa, A; Owman, Christer LU and Fuxe, K (1999) In NeuroReport 10(3). p.493-495
Abstract
RAT dopamine D2short receptors expressed in CHO cells were characterized by activation of [35S]GTPgammaS binding. There were no significant differences between the maximal effects seen in activation of [35S]GTPgammaS binding caused by dopaminergic agonists, but the effects of 5-HT, 8OH-DPAT and 5-methoxytryptamine amounted to 47 +/- 7%, 43 +/- 5% and 70 +/- 7% of the dopamine effect, respectively. The dopaminergic antagonist (+)butaclamol inhibited activations of both types of ligands with equal potency (pA2 = 8.9 +/- 0.1), indicating that only one type of receptor is involved. In competition with [3H]raclopride binding, dopaminergic agonists showed 53 +/- 2% of the binding sites in the GTP-dependent high-affinity state, whereas 5-HT... (More)
RAT dopamine D2short receptors expressed in CHO cells were characterized by activation of [35S]GTPgammaS binding. There were no significant differences between the maximal effects seen in activation of [35S]GTPgammaS binding caused by dopaminergic agonists, but the effects of 5-HT, 8OH-DPAT and 5-methoxytryptamine amounted to 47 +/- 7%, 43 +/- 5% and 70 +/- 7% of the dopamine effect, respectively. The dopaminergic antagonist (+)butaclamol inhibited activations of both types of ligands with equal potency (pA2 = 8.9 +/- 0.1), indicating that only one type of receptor is involved. In competition with [3H]raclopride binding, dopaminergic agonists showed 53 +/- 2% of the binding sites in the GTP-dependent high-affinity state, whereas 5-HT showed only 20 +/- 3%. Taken together, the results indicate that serotonergic agonists behave as typical partial agonists for D2 receptors with potential antiparkinsonian activity. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
NeuroReport
volume
10
issue
3
pages
493 - 495
publisher
Lippincott Williams & Wilkins
external identifiers
  • pmid:10208577
  • scopus:0033601964
ISSN
1473-558X
language
English
LU publication?
yes
id
44eece2f-0477-4541-b614-7304af31ddbd (old id 1115399)
date added to LUP
2008-07-08 09:08:24
date last changed
2017-01-01 05:05:52
@article{44eece2f-0477-4541-b614-7304af31ddbd,
  abstract     = {RAT dopamine D2short receptors expressed in CHO cells were characterized by activation of [35S]GTPgammaS binding. There were no significant differences between the maximal effects seen in activation of [35S]GTPgammaS binding caused by dopaminergic agonists, but the effects of 5-HT, 8OH-DPAT and 5-methoxytryptamine amounted to 47 +/- 7%, 43 +/- 5% and 70 +/- 7% of the dopamine effect, respectively. The dopaminergic antagonist (+)butaclamol inhibited activations of both types of ligands with equal potency (pA2 = 8.9 +/- 0.1), indicating that only one type of receptor is involved. In competition with [3H]raclopride binding, dopaminergic agonists showed 53 +/- 2% of the binding sites in the GTP-dependent high-affinity state, whereas 5-HT showed only 20 +/- 3%. Taken together, the results indicate that serotonergic agonists behave as typical partial agonists for D2 receptors with potential antiparkinsonian activity.},
  author       = {Rinken, A and Ferre, S and Terasmaa, A and Owman, Christer and Fuxe, K},
  issn         = {1473-558X},
  language     = {eng},
  number       = {3},
  pages        = {493--495},
  publisher    = {Lippincott Williams & Wilkins},
  series       = {NeuroReport},
  title        = {Serotonergic agonists behave as partial agonists at the dopamine D2 receptor},
  volume       = {10},
  year         = {1999},
}