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)* antipsychotics** typicals (chlorpromazine, fluphenazine, loxapine, thioridazine, etc.
)* antipsychotics** typicals (chlorpromazine, fluphenazine, loxapine, thioridazine, etc.
Dernière mise à jour : 2016-03-03
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many atypical antipsychotics block 5-ht2c receptors, but their clinical use is limited by multiple undesirable actions on various neurotransmitters and receptors.
many atypical antipsychotics block 5-ht2c receptors, but their clinical use is limited by multiple undesirable actions on various neurotransmitters and receptors.
Dernière mise à jour : 2016-03-03
Fréquence d'utilisation : 1
Qualité :
== effects ==when the receptor is activated to open the ion channel by agonists, the following effects are observed:* cns: nausea and vomiting center in brain stem, anxiety, seizure propensity* pns: neuronal excitation (in autonomic, nociceptive neurons), emesis== agonists ==agonists for the receptor include:* 2-methyl-5-ht* ethanol* alpha-methyltryptamine* ibogaine* bufotenin* varenicline* chlorophenylbiguanide* quipazine* rs-56812: potent and selective 5-ht3 partial agonist, 1000x selectivity over other serotonin receptors* sr-57227* ym-31636== antagonists ==antagonists for the receptor (sorted by their respective therapeutic application) include:* antiemetics** as-8112** granisetron** ondansetron** tropisetron* gastroprokinetics** alosetron** batanopride** metoclopramide (high doses)** renzapride** zacopride** m1, the major active metabolite of mosapride* antidepressants** mianserin** mirtazapine** vortioxetine* antipsychotics** clozapine** olanzapine** quetiapine* others** lamotrigine (epilepsy and bipolar disorder)** memantine (alzheimer's disease medication)** menthol** 3-tropanyl indole-3-carboxylate== positive allosteric modulators ==these agents are not agonists at the receptor, but increase the affinity or efficacy of the receptors for an agonist:* 5-chloroindole== discovery ==identification of the 5-ht3 receptor did not take place until 1986 because of a lack of selective pharmacological tool.
==effects==when the receptor is activated to open the ion channel by agonists, the following effects are observed:* cns: nausea and vomiting center in brain stem, anxiety, seizure propensity* pns: neuronal excitation (in autonomic, nociceptive neurons), emesis==agonists==agonists for the receptor include:* 2-methyl-5-ht* ethanol* alpha-methyltryptamine* ibogaine* bufotenin* varenicline* chlorophenylbiguanide* quipazine* rs-56812: potent and selective 5-ht3 partial agonist, 1000x selectivity over other serotonin receptors* sr-57227* ym-31636==antagonists==antagonists for the receptor (sorted by their respective therapeutic application) include:* antiemetics** as-8112** granisetron** ondansetron** tropisetron* gastroprokinetics** alosetron** batanopride** metoclopramide (high doses)** renzapride** zacopride** m1, the major active metabolite of mosapride* antidepressants** mianserin** mirtazapine** vortioxetine* antipsychotics** clozapine** olanzapine** quetiapine* others** lamotrigine (epilepsy and bipolar disorder)** memantine (alzheimer's disease medication)** menthol** 3-tropanyl indole-3-carboxylate==positive allosteric modulators==these agents are not agonists at the receptor, but increase the affinity or efficacy of the receptors for an agonist:* 5-chloroindole==discovery==identification of the 5-ht3 receptor did not take place until 1986 because of a lack of selective pharmacological tool.
Dernière mise à jour : 2016-03-03
Fréquence d'utilisation : 1
Qualité :