Amperozide: Difference between revisions

{{drugbox

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = 0M2W3TAG39

| verifiedrevid = 437132384

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

| image = Amperozide.png

| smiles1 = Fc1ccc(cc1)C(c2ccc(F)cc2)CCCN3CCN(C(=O)NCC)CC3

| CAS_number = 75558-90-6

| ATCvet = yes

| ATC_prefix = N05

| ATC_suffix = AX90

| PubChem = 73333

| ChEMBL_Ref = {{ebicite|correct|EBI}}

| ChEMBL = 1079935

| 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

| bioavailability =

| protein_bound =

| metabolism =

| elimination_half-life =

| excretion =

| pregnancy_category =

| legal_status =

| routes_of_administration =

'''Amperozide''' is an [[atypical antipsychotic]] of the [[diphenylbutylpiperazine]] class which acts as an [[Antagonist (pharmacology)|antagonist]] at the [[5-HT2A receptor|5-HT_2A]] [[receptor (biochemistry)|receptor]].<ref>Svartengren J, Simonsson P. Receptor binding properties of amperozide. ''Pharmacology and Toxicology''. 1990;66 Suppl 1:8-11. PMID 2154737</ref> It does not block [[dopamine receptor]]s as with most antipsychotic drugs,<ref>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</ref> but does inhibit dopamine release,<ref>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</ref><ref>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</ref> and alters the firing pattern of dopaminergic neurons.<ref>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</ref> It was investigated for the treatment of [[schizophrenia]] in humans,<ref>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</ref> 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.<ref>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</ref><ref>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</ref><ref>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</ref>

[[Category:Diphenylbutylpiperazines]]

[[Category:Organofluorides]]