Amperozide

drugbox
IUPAC_name = 4- [4,4-bis(4-fluorophenyl)butyl] -N-ethylpiperazine-1-carboxamide

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width = 240
CAS_number = 75558-90-6
synonyms = Amperozide
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PubChem = 73333
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C = 23 | H = 29 | F = 2 | N = 3 | O = 1
molecular_weight = 401.493 g/mol
smiles = CCNC(=O)N1CCN(CC1)CCCC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F
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Amperozide is an atypical antipsychotic drug which acts as a potent antagonist at the 5HT_2A receptor. [Svartengren J, Simonsson P. Receptor binding properties of amperozide. "Pharmacology and Toxicology". 1990;66 Suppl 1:8-11. PMID 2154737] It does not block dopamine receptors as with most antipsychotic drugs, [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] but does inhibit dopamine release, [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] [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] and alters the firing pattern of dopaminergic neurons. [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] It was investigated for the treatment of schizophrenia in humans, [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] 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. [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] [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] [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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