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Amperozide
Systematic (IUPAC) name
4-[4,4-bis(4-fluorophenyl)butyl]-N-ethylpiperazine-1-carboxamide
Identifiers
CAS number 75558-90-6
ATCvet code QN05AX90
PubChem 73333
Chemical data
Formula C 23H29F2N3O 
Mol. mass 401.493 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

Amperozide is an atypical antipsychotic drug which acts as a potent antagonist at the 5HT2A receptor.[1] It does not block dopamine receptors as with most antipsychotic drugs,[2] but does inhibit dopamine release,[3][4] and alters the firing pattern of dopaminergic neurons.[5] It was investigated for the treatment of schizophrenia in humans,[6] but never adopted clinically, its main use is instead in veterinary medicine, primarily in intensively farmed pigs, for decreasing aggression and stress and thereby increasing feeding and productivity.[7][8][9]

References

  1. ^ Svartengren J, Simonsson P. Receptor binding properties of amperozide. Pharmacology and Toxicology. 1990;66 Suppl 1:8-11. PMID 2154737
  2. ^ Meltzer HY, Zhang Y, Stockmeier CA. Effect of amperozide on rat cortical 5-HT2 and striatal and limbic dopamine D2 receptor occupancy: implications for antipsychotic action. European Journal of Pharmacology. 1992 May 27;216(1):67-71. PMID 1388121
  3. ^ Eriksson E. Amperozide, a putative anti-psychotic drug: uptake inhibition and release of dopamine in vitro in the rat brain. Life Sciences. 1990;47(23):2111-7. PMID 1979998
  4. ^ Yamamoto BK, Meltzer HY. The effect of the atypical antipsychotic drug, amperozide, on carrier-mediated striatal dopamine release measured in vivo. Journal of Pharmacology and Experimental Therapeutics. 1992 Oct;263(1):180-5. PMID 1403783
  5. ^ Grenhoff J, Tung CS, Ugedo L, Svensson TH. Effects of amperozide, a putative antipsychotic drug, on rat midbrain dopamine neurons recorded in vivo. Pharmacology and Toxicology. 1990;66 Suppl 1:29-33. PMID 2304893
  6. ^ Axelsson R, Nilsson A, Christensson E, Björk A. Effects of amperozide in schizophrenia. An open study of a potent 5-HT2 receptor antagonist. Psychopharmacology (Berlin). 1991;104(3):287-92. PMID 1924636
  7. ^ Kyriakis SC, Martinsson K, Olsson NG, Bjork A. Thin sow syndrome (TSS): the effect of amperozide. British Veterinary Journal. 1990 Sep-Oct;146(5):463-7. PMID 2224491
  8. ^ Kyriakis SC, Olsson NG, Martinsson K, Björk AK. Observations on the action of amperozide: are there social influences on sow-litter productivity? Research in Veterinary Science. 1991 Sep;51(2):169-73. PMID 1788479
  9. ^ Papp I, Waller C, Biro O. Practical experiences in the therapy of postweaning edema disease in piglets. Berliner und Munchener Tierarztliche Wochenschrift. (German) 1996 Oct;109(10):385-7. PMID 8999770







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