Serotonin 3 receptor antagonists

In connection with a study of potential serotonin receptor antagonists, some decahydrocyclazin-6-ones and -6-ols have been synthesized from acyclic precursors <1992SC3115> (Scheme 115), but those esters derived from the latter (both epimers) which have been tested to date as potential 5-HT3 receptor antagonists have shown little biological activity <1993EJM869>. 

Milnacipran is currently available for use as an antidepressant in several countries outside the U.S. It is also under clinical development to assess its potential role in the treatment of fibromyalgia syndrome [62,63]. In a rat model of neuropathic pain, milnacipran, administered intrathecally, produced dose-dependent anti-allodynic effects at doses between 3 and 100 gg for up to 7h [64], The anti-allodynic effect of 30 gg of milnacipran was attenuated by intrathecal coadministration of a serotonin receptor antagonist or a norepinephrine receptor... 

HT3 antagonist serotonin receptor antagonist type 3... 

As first choice treatment a well-established antihistamine such as meclozine is recommended. Promethazine is another antihistamine which reduces nausea, but sedation is a not always desired adverse effect. Metoclopramide increases intestinal motility and could be used short term also early in pregnancy. A neuroleptic such as prochlorperazine reduces nausea but should only be used for shortterm treatment due to the risk of extrapyramidal adverse reactions. Serotonin receptor antagonists can be used in post-operahve nausea and during treatment with cytostatics. 

Nausea that accompanies the administration of cancer chemotherapy agents was resistant to drug intervention until the introduction of the serotonin receptor antagonist odansetron (see Chapter 13). The benzimidazolone-based compound itasetron (57-6) has much the same activity as its tricylcic predecessor. Condensation of 2-nitrophenyl-isocyanate (57-1) with the bridged bycyclic diamine (57-2) leads to the addition... 

Ondansetron (Zofran, Zofran ODT) [Anriemeric/5-HT Antagonist] Uses N/V Action Serotonin receptor antagonist Dose Adults. 

Serotonin Receptor Antagonists Serotonin receptor antagonists include ... 

Key Words 5-Hydroxytryptamine serotonin receptor antagonist knockout autoradiography thermoregulation hippocampus behavior electrophysiology depression oleamide. 

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