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… 
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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
TLDR
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.
Pharmacological Profile of 2-Bromoterguride at Human Dopamine D2, Porcine Serotonin 5-Hydroxytryptamine 2A, and α2C-Adrenergic Receptors, and Its Antipsychotic-Like Effects in Rats
TLDR
2-bromoterguride may be a strong candidate for the treatment of schizophrenia with a lower risk to induce EPS because of its in vitro and in vivo properties.
Proterguride, a highly potent dopamine receptor agonist promising for transdermal administration in Parkinson's disease: interactions with alpha(1)-, 5-HT(2)- and H(1)-receptors.
TLDR
The results are discussed focussing on the relevance of action at 5-HT(2B) receptors as well as their significance for a transdermal administration of proterguride.
Neuroprotective effects of the novel D3/D2 receptor agonist and antiparkinson agent, S32504, in vitro against 1-methyl-4-phenylpyridinium (MPP+) and in vivo against 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP): a comparison to ropinirole
TLDR
It is demonstrated that S32504 robustly, concentration-dependently and completely protects terminally differentiated SH-SY5Y cells against 1-methyl-4-phenylpyridinium (MPP+)-induced cell death in vitro, and robustly protects dopaminergic neurones against the neurotoxic effects of MPP(+) and MPTP in in vitro and in vivo models, respectively.
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.
TLDR
The results extend the notion of agonist-directed trafficking of receptor signalling to all the 5-HT2-receptor family and indicate that measures of Gq/11 activation versus calcium release may be useful to identify more effective therapeutic drugs with limited side effects.
Agonism at 5-HT2B receptors is not a class effect of the ergolines.
TLDR
Researchers study 5-HT2B receptor-mediated relaxation in porcine pulmonary arteries to five ergolines which are used as antiparkinsonian drugs and find that agonism at 5- HT2B receptors seems not to be a class effect of the ergoline.
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
TLDR
It is concluded that the bulky N(6) substituent of cabergoline is responsible for 5- HT2AR and 5-HT2BR agonism and the increased ERK1/2 phosphorylation and production of extracellular matrix by Cabergoline are mediated by 5-ht2ARs.
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
TLDR
S32504 and, less potently, pramipexole show robust, stereospecific, and long-lasting neuroprotective effects against MPP + toxicity that involve D 3 receptors that reflect downstream recruitment of BDNF and via a PK3-AKT pathway.
Antidepressant-like properties of the anti-Parkinson agent, piribedil, in rodents: mediation by dopamine D2 receptors
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…
An in vivo pharmacological evaluation of pardoprunox (SLV308) — A novel combined dopamine D2/D3 receptor partial agonist and 5-HT1A receptor agonist with efficacy in experimental models of Parkinson's disease
TLDR
It is demonstrated that pardoprunox possesses dopamine D2/3 partial agonist effects, 5-HT1A agonists effects and reduces parkinsonism in animal models.
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References

SHOWING 1-10 OF 80 REFERENCES
Differential Actions of Antiparkinson Agents at Multiple Classes of Monoaminergic Receptor. II. Agonist and Antagonist Properties at Subtypes of Dopamine D2-Like Receptor and α1/α2-Adrenoceptor
TLDR
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.
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
TLDR
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.
Inverse Agonist Properties of Antipsychotic Agents at Cloned, Human (h) Serotonin (5-HT)1B and h5-HT1D Receptors
TLDR
With the exception of ziprasidone, all antipsychotics were inverse agonists at h5-HT1B and h5 -HT1D receptors, although they differed markedly in their potency at these sites as compared to hD2 receptors.
Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors
TLDR
The present data suggest that roxindole activates mainly D3 vs. D2 or D4 receptors and 5-HT1A vs. 5- HT1B or 5,HT1D receptors, and Activation of D3 and/or 5-ht1A receptors may contribute to its potential antidepressant properties.
The serotonin 5-HT2C receptor is a prominent serotonin receptor in basal ganglia: evidence from functional studies on serotonin-mediated phosphoinositide hydrolysis.
TLDR
Results indicate that 5-HT2A- and 5- HT2C-linked PLC activity can be discerned in brain regions possessing both receptor subtypes using membranes prepared from previously frozen tissue.
Antagonism of 5-hydroxytryptamine(2a) receptors attenuates the behavioral effects of cocaine in rats.
TLDR
It is suggested that 5-HT2A receptors play an important role in the behavioral effects of cocaine and that they should be considered a viable target for analysis in the search for pharmacotherapies useful in the treatment of cocaine dependence.
Contrasting mechanisms of action and sensitivity to antipsychotics of phencyclidine versus amphetamine: importance of nucleus accumbens 5‐HT2A sites for PCP‐induced locomotion in the rat
TLDR
PCP‐induced locomotion (PLOC) was potently blocked by the selective serotonin (5‐HT)2A vs. D2 antagonists, SR46349, MDL100,907, ritanserin and fananserin, which barely affected amphetamine‐induced Locomotion (ALOC), which is, correspondingly, more potents blocked than ALOC by antipsychotics displaying marked affinity at 5‐HT2A receptors.
Serotonergic mechanisms in neuroleptic-induced catalepsy in the rat
  • M. Wadenberg
  • Psychology, Medicine
    Neuroscience & Biobehavioral Reviews
  • 1996
The present paper reviews a series of experiments aimed at elucidating the interaction between specific dopamine (DA) and 5-hydroxytryptamine (5-HT) receptors in the mediation of extrapyramidal motor…
Characterization of phospholipase C activity at h5-HT2C compared with h5-HT2B receptors: influence of novel ligands upon membrane-bound levels of [3H]phosphatidylinositols
TLDR
This rapid and innovative method for determination of PLC activity permitted characterization of an extensive range of novel ligands at h5-HT2C receptors, including Ro600332, Ro600175 and BW723C86, which showed "full" efficacy at h3HPI sites and antagonist potency and binding affinity were highly correlated.
Serotonin 5-HT1A agonist improves motor complications in rodent and primate parkinsonian models
TLDR
Drugs acting to stimulate 5-HT1A receptors could prove useful in the treatment of the motor response complications in parkinsonian patients.
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