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Ricasetron
Systematic (IUPAC) name
endo-N-(8-methyl-8-azabicyclo[3.2.1]oct-3yl)-2,3-dihydro-3,3-dimethyl-indole-1-carboxamide
Identifiers
CAS number 117086-68-7
ATC code none
PubChem 71785
Chemical data
Formula C 19H27N3O 
Mol. mass 313.436 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

Ricasetron (BRL-46470) is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor.[1] It has antiemetic effects as with other 5-HT3 antagonists,[2] and also has anxiolytic effects significantly stronger than other related drugs,[3] and with less side effects than benzodiazepine anxiolytics.[4][5] However it has never been developed for medical use.

References

  1. ^ Newberry NR, Watkins CJ, Sprosen TS, Blackburn TP, Grahame-Smith DG, Leslie RA (August 1993). "BRL 46470 potently antagonizes neural responses activated by 5-HT3 receptors". Neuropharmacology 32 (8): 729–35. PMID 8413836.  
  2. ^ Bermudez J, Sanger GJ (June 1994). "Prolonged anti-emetic activity and 5-HT3-receptor antagonism by BRL 46470 in conscious ferrets". The Journal of Pharmacy and Pharmacology 46 (6): 520–1. PMID 7932054.  
  3. ^ Blackburn TP, Baxter GS, Kennett GA, King FD, Piper DC, Sanger GJ, Thomas DR, Upton N, Wood MD (1993). "BRL 46470A: a highly potent, selective and long acting 5-HT3 receptor antagonist with anxiolytic-like properties". Psychopharmacology 110 (3): 257–64. PMID 7831418.  
  4. ^ Link CG, Leigh TJ, Dennison JK (April 1993). "The effects of BRL 46470A, a novel 5-HT3 receptor antagonist, and lorazepam on psychometric performance and the EEG". British Journal of Clinical Pharmacology 35 (4): 395–9. PMID 8485019.  
  5. ^ de Souza Silva M, Guimarães FS, Graeff FG, Tomaz C (December 1993). "Absence of amnestic effect of an anxiolytic 5-HT3 antagonist (BRL 46470A) injected into basolateral amygdala, as opposed to diazepam". Behavioural Brain Research 59 (1-2): 141–5. PMID 8155281.  
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