词条 | Amperozide |
释义 |
| verifiedrevid = 444367960 | IUPAC_name = 4-[4,4-bis(4-fluorophenyl)butyl]-N-ethylpiperazine-1-carboxamide | image = Amperozide.svg | width = 270 | tradename = | pregnancy_category = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 75558-90-6 | ATCvet = yes | ATC_prefix = N05 | ATC_suffix = AX90 | PubChem = 73333 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 66062 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 0M2W3TAG39 | 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 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C23H29F2N3O/c1-2-26-23(29)28-16-14-27(15-17-28)13-3-4-22(18-5-9-20(24)10-6-18)19-7-11-21(25)12-8-19/h5-12,22H,2-4,13-17H2,1H3,(H,26,29) | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = NNAIYOXJNVGUOM-UHFFFAOYSA-N }}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] See also
References1. ^Svartengren J, Simonsson P. Receptor binding properties of amperozide. Pharmacology and Toxicology. 1990;66 Suppl 1:8-11. {{PMID|2154737}} {{Antipsychotics}}{{Serotonergics}}{{Piperazines}}{{nervous-system-drug-stub}}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. 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}} 4 : 5-HT2A antagonists|Fluoroarenes|Piperazines|Ureas |
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