Author: Funahashi, Hideki ; Kanemaru-Kawazoe, Anna ; Kogoh, Yoichiro ; Nishimori, Toshikazu ; Ishida, Yasushi ; Haruta-Tsukamoto, Ayaka ; Miyahara, Yu

The roles of serotonin (5-HT) and/or noradrenaline in acute pruriceptive processing have been demonstrated using antidepressants, such as milnacipran, a serotonin and noradrenaline reuptake inhibitor, and mirtazapine, a noradrenergic and specific serotonergic antidepressant; however, the involvement of 5-HT in acute pruriceptive processing has not yet been elucidated in detail. Scratching events induced by chloroquine (CQ) were attenuated by the administration of milnacipran or mirtazapine, and these effects were reversed by a treatment with ondansetron, a 5-HT₃ antagonist, or SB26970, a 5-HT₇ antagonist. CQ-induced scratching events were also ameliorated by the intrathecal administration of 5-HT, SR572227A and RS56812 (5-HT₃ agonists), and LP211 and LP44 (5-HT₇ agonists), indicating the modulation of CQ-induced scratching events by 5-HT and noradrenaline. By contrast, histamine-induced scratching events were not markedly affected by the administration of 5-HT and 5-HT₇ agonists, whereas 5-HT₃ agonists exerted attenuating effects. Similarly, they were not clearly reversed by the administration of the 5-HT₇ antagonist, unlike a 5-HT₃ antagonist. Therefore, 5-HT is involved in the attenuating effects of milnacipran and mirtazapine on CQ- and histamine-induced scratching events, and 5-HT₃ and 5-HT₇ receptors play different roles in pruriceptive processing induced by histamine or CQ.

01 Dec 2016·International Journal of Obstetric AnesthesiaQ4 · MEDICINE

Stimulation of contractions in pregnant human myometrium is associated with 5-HT3 receptors

Q4 · MEDICINE

Article

Author: Ma, Y S ; Ni, J ; Lin, X M ; Li, P ; Diao, M ; Wan, Y L ; Zhu, Q ; Li, H

BACKGROUNDSerotonin (5-HT) is known to play an important role in regulating uterine contractions. However, the specific receptors involved have not been well characterized. We evaluated whether 5-HT3 receptors exist in human myometrium, and their effects on myometrial contractility when stimulated by a 5-HT3 agonist.METHODSFour tissue samples taken from patients undergoing hysterectomy (n=2) and elective cesarean delivery (n=2) were used to detect expression of 5-HT3 receptors on the myometrium using western blotting. For isometric tension measurement, another 12 myometrial strips obtained from patients undergoing elective cesarean delivery were randomly divided into a control group (Group CON) and an RS56812 group (Group RG). In increasing doses from 10^-7M to 10^-4M, RS56812, a 5-HT3 receptor agonist, was used to investigate the contractile effects after bonding to the 5-HT3 receptor, following which the effects of granisetron were assessed. Amplitude, interval and duration of myometrial contractions were recorded.RESULTSProteins with a molecular mass of 55kDa, consistent with 5-HT3 receptors, were detected both on non-pregnant and late-pregnant human uteri. RS56812 increased the contractile amplitude at concentrations of 10^-6M, 10^-5M and 10^-4M, achieving maximum effect at 10^-5M. A prolonged contractile interval was detected at the concentration of 10^-4M. However, RS56812 showed no significant effect on contraction duration. Granisetron did not reverse the contractile effects induced by RS56812.CONCLUSION5-HT3 receptors are expressed on non-pregnant and pregnant uteri. RS56812 enhanced myometrial contractions, but this was not affected by granisetron, the mechanism of which requires further investigation.

01 Dec 1996·NeuroReportQ4 · MEDICINE

The 5-HT3 receptor antagonist, RS-56812, enhances delayed matching performance in monkeys

Q4 · MEDICINE

Article

Author: Eglen, Richard M. ; Terry, Alvin V. Jr. ; Whiting, Roger L. ; Buccafusco, Jerry J. ; Jackson, William J. ; Prendergast, Mark A. ; Fontana, David L. ; Wong, Erik H. F.

Substantial evidence indicates that serotonin receptors are involved in the regulation of acetylcholine release in CNS regions important to mnemonic processes, and may thus be exploited pharmacologically as targets for memory improvement. In the present study, the (R) and (S) isomers of a potent serotonin (5-HT3) receptor ligand, RS-56812 were evaluated for potential memory effects in five macaques trained to perform a delayed matching-to-sample (DMTS) task. While both isomers enhanced certain aspects of task performance, the (R) isomer produced more systematic improvements. This differential sensitivity to the isomers in regard to DMTS performance appears to parallel the higher 5-HT3 receptor affinity of the R enanantiomer. The results are consistent with a potential therapeutic role for RS-56812 in disorders involving cognitive decline.

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Cognition Disorders	Discovery	US	Roche Palo Alto LLC	-

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