Serotonergic agonists behave as partial agonists at the dopamine D2 receptor
(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)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/1115399
- author
- Rinken, A ; Ferre, S ; Terasmaa, A ; Owman, Christer LU and Fuxe, K
- organization
- publishing date
- 1999
- 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
- 2016-04-01 12:23:10
- date last changed
- 2022-01-27 02:59:51
@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}}, }