Molecular pharmacology of niaprazine

@article{Scherman1988MolecularPO,
  title={Molecular pharmacology of niaprazine},
  author={Daniel Scherman and Michel Hamon and Henri Gozlan and J. P. Henry and Ariane Lesage and M{\'a}r M{\'a}sson and Jean Francois Rumigny},
  journal={Progress in Neuro-Psychopharmacology and Biological Psychiatry},
  year={1988},
  volume={12},
  pages={989-1001}
}
  • D. Scherman, M. Hamon, J. Rumigny
  • Published 31 December 1988
  • Biology, Chemistry
  • Progress in Neuro-Psychopharmacology and Biological Psychiatry
4-[18F]Fluorophenylpiperazines by Improved Hartwig-Buchwald N-Arylation of 4-[18F]fluoroiodobenzene, Formed via Hypervalent λ3-Iodane Precursors: Application to Build-Up of the Dopamine D4 Ligand [18F]FAUC 316
Substituted phenylpiperazines are often neuropharmacologically active compounds and in many cases are essential pharmacophores of neuroligands for different receptors such as D2-like dopaminergic,
Designer Drug (DD) abuse in Poland; a review of the psychoactive and toxic properties of substances found from seizures of illegal drug products and the legal consequences thereof. Part II--piperazines/piperidines, phenylethylamines, tryptamines and miscellaneous 'others'.
TLDR
These two articles may help suitable legislation to be rapidly devised to make the prohibition of DDs permanent whenever deemed necessary, as well as providing an up-to-date reference source for those engaged in the DD issue.
N,N'-Bisoxalamides Enhance the Catalytic Activity in Cu-Catalyzed Coupling of (Hetero)Aryl Bromides with Anilines and Secondary Amines.
TLDR
High selectivity is achieved in CuI/BFMO-catalyzed direct monoarylation of piperazine with (hetero)aryl bromides to afford pharmaceutically important building blocks.
1-Benzylpiperazine and other piperazine-based stimulants
Toxicology of Specific Substances

References

SHOWING 1-10 OF 28 REFERENCES
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
  • Biology, Chemistry
    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.
Biochemical and pharmacological studies of RO 1-9569 (tetrabenazine), a nonindole tranquilizing agent with reserpine-like effects.
TLDR
It is concluded that Ro 1-9569 and reserpine compete for the same receptor sites, and the sedative effect of the drug seems to be related to the change in brain serotonin rather than norepinephrine.
Evidence that blood pressure reduction by serotonin antagonists is related to alpha receptor blockade in spontaneously hypertensive rats.
TLDR
Blood pressure reduction more closely paralleled the in vitro and in vivo potency of these agents toward vascular alpha rather than 5HT2 receptors.
Niaprazine, a selective brain catecholamine depletor
Ketanserin binds to the monoamine transporter of chromaffin granules and of synaptic vesicles.
TLDR
It is concluded that nonspecific displaceable binding sites of [3H]ketanserin previously described in the striatum are tetrabenazine binding sites associated with the synaptic vesicle monoamine transporter.
Are antihistamines sedative via a blockade of brain H1 receptors?
TLDR
Both the presence of histaminergic fibres innerving the telencephalon via the lateral hypothalamic area and the fact that brain histamine concentration or histamine turnover exhibited cirw d i a n variations, might suggest a role of histamine on wakefulness and sleep.
Properties of [3H]haloperidol and [3H]dopamine binding associated with dopamine receptors in calf brain membranes.
TLDR
Regional variations in [3 H]dopamine and [ 3 H]haloperidol binding are parallel and correspond to regional differences in dopaminergic innervation, and drug specificity does not appear to differ between limbic and striatal areas.
...
...