Effects of long-term administration of the 5-hydroxytryptamine1B receptor antagonist AR-A000002 to guinea pigs

@article{Stenfors2004EffectsOL,
  title={Effects of long-term administration of the 5-hydroxytryptamine1B receptor antagonist AR-A000002 to guinea pigs},
  author={Carina Stenfors and Charlotte Ahlgren and Hong Yu and M Wed{\'e}n and Lars-Gunnar Larsson and Svante B. Ross},
  journal={Psychopharmacology},
  year={2004},
  volume={172},
  pages={333-340}
}
RationaleRecently a new 5-hydroxytryptamine1B (5-HT1B)-receptor antagonist, AR-A000002, was described. It was shown that this compound dose dependently increased 5-HT metabolism and release in guinea pig brain following a single injection.ObjectivesThe present study investigated effects of 3 weeks twice-daily treatment of guinea pigs with the 5-HT1B-receptor antagonist AR-A000002 on the serotonergic neurons and receptor densities.MethodsGuinea pigs were injected subcutaneously with AR-A000002… 
7 Citations

The immunization with peptide 189–205, a derivative of serotonin receptor subtypes 1B, changes the sensetivity of adenylyl cyclase to hormones in the rat brain

The aim of this work was to study the effect of multiple (during 12 months) immunization of rats with BSA-conjugated peptide 189–205 corresponding to the second extracellular loop of rat HT1BR on

Development of PET radioligands synthesized from in-target produced [11C]methane

It is shown that in-target produced [C]CH4 makes it possible for the routine C-labeling of PET radioligands with high SA, which can to the greatest extent be attributed to[C]CO2 being more sensitive to isotopic dilution from CO2 in the air.

Regioisomerism in the synthesis of a chiral aminotetralin drug compound: unraveling mechanistic details and diastereomer-specific in-depth NMR investigations.

A deep insight into the structural features of the current 2-aminotetralin family was obtained, which is emphasized by the definition of a novel "0.2 ppm rule" allowing the absolute configuration at tetralin C-2 to be determined.

References

SHOWING 1-10 OF 28 REFERENCES

Down-regulation of dopamine D-2, 5-HT2 receptors and β-adrenoceptors in rat brain after prolonged treatment with a new potential antidepressant, Lu 19-005

The down-regulation of DA D-2 receptors was accompanied by tolerance to d-amphetamine-induced hypermotility (after low doses) and stereotyped licking or biting (after a high dose) and the effect of prolonged treatment with other antidepressant drugs was discussed.

Combined Administration of a 5‐Hydroxytryptamine (5‐HT)1D Antagonist and a 5‐HT Reuptake Inhibitor Synergistically Increases 5‐HT Release in Guinea Pig Hypothalamus In Vivo

In vivo microdialysis in guinea pig hypothalamus was used to study the effect of serotonin subtype 1D autoreceptor blockade on the increase in extracellular 5‐HT levels produced by a selective5‐HT reuptake inhibitor (SSRI), indicating that the effects of an SSRI on terminal 5-HT are significantly enhanced by coadministration of a 5‐ HT1D antagonist.

Synergism between 5-HT1B/1D and 5-HT1A receptor antagonists on turnover and release of 5-HT in guinea-pig brain in vivo

Extracellular 5-HIAA seems to be a better marker than 5-HT itself for the evoked5-HT release when the reuptake mechanism is intact and the synergistic effect of the two receptor antagonists on the 5-ht turnover and the terminal release of 5- HT indicate somatodendritic 5-HCIAA release and stimulation of inhibitory 6-HT1A receptors at this level.

Behavioral Pharmacology of AR-A000002, a Novel, Selective 5-Hydroxytryptamine1B Antagonist

Data suggest utility for 5-HT1B antagonists in the treatment of both anxiety and affective disorders.

WAY-100635, a potent and selective 5-hydroxytryptamine1A antagonist, increases serotonergic neuronal activity in behaving cats: comparison with (S)-WAY-100135.

The results obtained with WAY-100635 confirm the previous findings obtained with spiperone and further support the hypothesis that 5-HT1A autoreceptor-mediated feedback inhibition operates under physiological conditions.

Interaction between a selective 5‐HT1A receptor antagonist and an SSRI in vivo: effects on 5‐HT cell firing and extracellular 5‐HT

Pretreatment with the selective 5‐HT1A receptor antagonist, WAY 100635, blocked the inhibitory effect of paroxetine on5‐HT neuronal activity in the DRN and, at the same time, markedly enhanced the effect ofParoxetines on extracellular 5‐ HT in the FCx.