Differential Actions of Antiparkinson Agents at Multiple Classes of Monoaminergic Receptor. III. Agonist and Antagonist Properties at Serotonin, 5-HT1 and 5-HT2, Receptor Subtypes
@article{NewmanTancredi2002DifferentialAO, title={Differential Actions of Antiparkinson Agents at Multiple Classes of Monoaminergic Receptor. III. Agonist and Antagonist Properties at Serotonin, 5-HT1 and 5-HT2, Receptor Subtypes}, author={Adrian Newman-Tancredi and Didier Cussac and Yann Quentric and Manuelle Touzard and Laurence Verri{\`e}le and Nathalie Carpentier and Mark J Millan}, journal={Journal of Pharmacology and Experimental Therapeutics}, year={2002}, volume={303}, pages={815 - 822} }
Although certain antiparkinson agents interact with serotonin (5-HT) receptors, little information is available concerning functional actions. Herein, we characterized efficacies of apomorphine, bromocriptine, cabergoline, lisuride, piribedil, pergolide, roxindole, and terguride at human (h)5-HT1A, h5-HT1B, and h5-HT1D receptors [guanosine 5′-O-(3-[35S]thio)triphosphate ([35S]GTPγS) binding], and at h5-HT2A, h5-HT2B, and h5-HT2C receptors (depletion of membrane-bound [3H]phosphatydilinositol…
176 Citations
Differential Actions of Antiparkinson Agents at Multiple Classes of Monoaminergic Receptor. I. A Multivariate Analysis of the Binding Profiles of 14 Drugs at 21 Native and Cloned Human Receptor Subtypes
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An innovative multivariate analysis revealed marked heterogeneity in binding profiles of antiparkinson agents at diverse receptors implicated in the etiology and/or treatment of Parkinson's disease.
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Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells.
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Agonism at 5-HT2B receptors is not a class effect of the ergolines.
- Biology, MedicineEuropean journal of pharmacology
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The Bulky N(6) Substituent of Cabergoline Is Responsible for Agonism of This Drug at 5-Hydroxytryptamine (5-HT)2A and 5-HT2B Receptors and Thus Is a Determinant of Valvular Heart Disease
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Involvement of dopamine D2/D3 receptors and BDNF in the neuroprotective effects of S32504 and pramipexole against 1-methyl-4-phenylpyridinium in terminally differentiated SH-SY5Y cells
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Antidepressant-like properties of the anti-Parkinson agent, piribedil, in rodents: mediation by dopamine D2 receptors
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The dopamine D2/D3 receptor agonist and &agr;2 adrenergic receptor antagonist, piribedil, is used clinically as monotherapy and as an adjunct to L-3,4-dihydroxyphenylalanine in the treatment of…
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In conclusion, antiparkinson agents display diverse agonist and antagonist properties at multiple subtypes of D2-like receptor and α1/α2-AR, actions, which likely contribute to their contrasting functional profiles.
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An innovative multivariate analysis revealed marked heterogeneity in binding profiles of antiparkinson agents at diverse receptors implicated in the etiology and/or treatment of Parkinson's disease.
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