Amperozide: Difference between revisions

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==Overview==


'''Amperozide''' is an [[atypical antipsychotic]] of the [[diphenylbutylpiperazine]] class which acts as an [[Antagonist (pharmacology)|antagonist]] at the [[5-HT2A receptor|5-HT<sub>2A</sub>]] [[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>
'''Amperozide''' is an [[atypical antipsychotic]] of the [[diphenylbutylpiperazine]] class which acts as an [[Antagonist (pharmacology)|antagonist]] at the [[5-HT2A receptor|5-HT<sub>2A</sub>]] [[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>
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{{Antipsychotics}}
{{Antipsychotics}}
{{Serotonergics}}
{{Piperazines}}


[[Category:5-HT2A antagonists]]
 
[[Category:Drug]]
[[Category:Piperazines]]
[[Category:Piperazines]]
[[Category:Organofluorides]]
[[Category:Organofluorides]]
[[Category:Ureas]]
[[Category:Ureas]]

Latest revision as of 17:34, 18 August 2015

Amperozide
Clinical data
ATCvet code
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC23H29F2N3O
Molar mass401.493 g/mol
3D model (JSmol)
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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

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

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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