Sarizotan, a serotonin 5-HT1A receptor agonist and dopamine receptor ligand. 1. Neurochemical profile

@article{Bartoszyk2004SarizotanAS,
  title={Sarizotan, a serotonin 5-HT1A receptor agonist and dopamine receptor ligand. 1. Neurochemical profile},
  author={Gerd D. Bartoszyk and Christoph van Amsterdam and Hartmut E. Greiner and Wilfried Rautenberg and Hermann Russ and Christoph A. Seyfried},
  journal={Journal of Neural Transmission},
  year={2004},
  volume={111},
  pages={113-126}
}
Summary.Sarizotan exhibited high affinities only to serotonin 5-HT1A receptors and dopamine DA D4>D3>D2 receptors with the profile of a 5-HT1A agonist and DA antagonist demonstrated by the inhibition of cAMP-stimulation and guinea pig ileum contraction, decreased accumulation of the 5-HT precursor 5-hydroxytryptophan and increased levels of 5-HT metabolites, increased accumulation of DA precursor dihydroxyphenylalanine (DOPA) and the reduced levels of DA metabolites in intact rats. However… Expand
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References

SHOWING 1-10 OF 75 REFERENCES
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. Expand
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 motorExpand
The effect of chronic administration of sarizotan, 5-HT1A agonist/D3/D4 ligand, on haloperidol-induced repetitive jaw movements in rat model of tardive dyskinesia
TLDR
Agonism at 5-HT1A receptors may be mediating the inhibitory effect of sarizotan on RJM in rat models of tardive dyskinesia, which is known to counteract antipsychotic-induced motor side effects. Expand
Preclinical studies on LY228729: a potent and selective serotonin1A agonist.
TLDR
Results indicate that LY228729 is potent 5-HT1A agonist with bioavailability properties sufficient for clinical evaluation and with efficacy in preclinical models of anxiety, sexual disorders and motion sickness. Expand
Alterations of central serotonin and dopamine turnover in rats treated with ipsapirone and other 5-hydroxytryptamine1A agonists with potential anxiolytic properties.
Measurements of tissue levels of monoamines and their metabolites, and of the rates of 5-hydroxytryptophan and dihydroxy-phenylalanine accumulation after blockade of aromatic amino acid decarboxylaseExpand
Biochemical and functional studies on EMD 49,980: a potent, selectively presynaptic D-2 dopamine agonist with actions on serotonin systems.
TLDR
Results with various reference compounds make it unlikely that there are indirect effects, also via alpha 2-receptors in the models used and support the view that D-2 agonistic, 5-HT uptake inhibiting and5-HT1A agonistic actions are independent properties of EMD 49,980. Expand
The anticataleptic effect of 7-OH-DPAT: are dopamine D3 receptors involved?
TLDR
Results show that 7-OH-DPAT, as well as L-DOPA, a drug of choice in the therapy of Parkinson's disease, used for comparison, antagonize the catalepsy induced by reserpine, haloperidol and fluphenazine. Expand
The effect of serotonergic agents on haloperidol-induced catalepsy
  • P. Hicks
  • Medicine, Chemistry
  • Schizophrenia Research
  • 1989
TLDR
It is suggested that 5- HT-1A and 5-HT-2 receptor sites are important in the serotonergic modulation of haloperidol-induced catalepsy. Expand
Characterization of the 5-hydroxytryptamine1a receptor-mediated inhibition of forskolin-stimulated adenylate cyclase activity in guinea pig and rat hippocampal membranes.
  • M. De Vivo, S. Maayani
  • Chemistry, Medicine
  • The Journal of pharmacology and experimental therapeutics
  • 1986
TLDR
The concentration-response data show that the inhibition of forskolin-stimulated adenylate cyclase activity in guinea pig and rat hippocampal membranes is mediated by a receptor with the characteristics of the 5-HT1A binding site, and it is proposed that this response is suitable for measuring activities and affinities of drugs acting at 5- HT1A receptors. Expand
Attenuation of levodopa-induced dyskinesia by normalizing dopamine D3 receptor function
TLDR
Results indicated that the D3 receptors participated in both dyskinesia and the therapeutic action of levodopa, and that partial agonists may normalize D3 receptor function and correct side effects of levidopa therapy in patients with Parkinson disease. Expand
...
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5
...