Amperozide is an atypical antipsychotic of the diphenylbutylpiperazine class which acts as an antagonist at the 5-HT2A 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]
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Meltzer HY, Zhang Y, Stockmeier CA (May 1992). "Effect of amperozide on rat cortical 5-HT2 and striatal and limbic dopamine D2 receptor occupancy: implications for antipsychotic action". European Journal of Pharmacology. 216 (1): 67–71. doi:10.1016/0014-2999(92)90210-u. PMID 1388121. Eriksson E (1990). "Amperozide, a putative anti-psychotic drug: uptake inhibition and release of dopamine in vitro in the rat brain". Life Sciences. 47 (23): 2111–7. doi:10.1016/0024-3205(90)90310-n. PMID 1979998. Yamamoto BK, Meltzer HY (October 1992). "The effect of the atypical antipsychotic drug, amperozide, on carrier-mediated striatal dopamine release measured in vivo". The Journal of Pharmacology and Experimental Therapeutics. 263 (1): 180–5. PMID 1403783. Grenhoff J, Tung CS, Ugedo L, Svensson TH (1990). "Effects of amperozide, a putative antipsychotic drug, on rat midbrain dopamine neurons recorded in vivo". Pharmacology & Toxicology. 66 (Suppl 1): 29–33. doi:10.1111/j.1600-0773.1990.tb01603.x. PMID 2304893. Axelsson R, Nilsson A, Christensson E, Björk A (1991). "Effects of amperozide in schizophrenia. An open study of a potent 5-HT2 receptor antagonist". Psychopharmacology. 104 (3): 287–92. doi:10.1007/bf02246025. PMID 1924636. S2CID 2507927. Kyriakis SC, Olsson NG, Martinsson K, Björk AK (September 1991). "Observations on the action of amperozide: are there social influences on sow-litter productivity?". Research in Veterinary Science. 51 (2): 169–73. doi:10.1016/0034-5288(91)90008-C. PMID 1788479. Papp I, Waller C, Biro O (October 1996). "[Practical experiences in the therapy of postweaning edema disease in piglets]". Berliner und Munchener Tierarztliche Wochenschrift. 109 (10): 385–7. PMID 8999770.