| 词条 | Pipamperone |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 464207244 | IUPAC_name = 1-[4-(4-fluorophenyl)-4-oxobutyl]-4-piperidin-1-ylpiperidine-4-carboxamide | image = Pipamperone.svg | width = 250 | tradename = | Drugs.com = {{drugs.com|international|pipamperone}} | pregnancy_AU = | pregnancy_US = | legal_status = | routes_of_administration = Oral | bioavailability = | metabolism = | elimination_half-life = 17-22 hours | excretion = | CAS_number_Ref = {{cascite|changed|??}} | CAS_number = 1893-33-0 | ATC_prefix = N05 | ATC_suffix = AD05 | ATC_supplemental = | PubChem = 4830 | IUPHAR_ligand = 92 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 4664 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 5402501F0W | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D02622 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 440294 | synonyms = McN-JR 3345; R-3345 | C=21 | H=30 | F=1 | N=3 | O=2 | molecular_weight = 375.480 g/mol | smiles = Fc1ccc(cc1)C(=O)CCCN3CCC(C(=O)N)(N2CCCCC2)CC3 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C21H30FN3O2/c22-18-8-6-17(7-9-18)19(26)5-4-12-24-15-10-21(11-16-24,20(23)27)25-13-2-1-3-14-25/h6-9H,1-5,10-16H2,(H2,23,27) | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = AXKPFOAXAHJUAG-UHFFFAOYSA-N |drug_name=|alt=|caption=|type=|MedlinePlus=|licence_EU=|pregnancy_category=|licence_US=}}Pipamperone (INN, USAN, BAN), also known as carpiperone and floropipamide or fluoropipamide, and as floropipamide hydrochloride (JAN), is a typical antipsychotic of the butyrophenone family used in the treatment of schizophrenia[1][2] and as a sleep aid for depression.[3] It is or has been marketed under brand names including Dipiperon, Dipiperal, Piperonil, Piperonyl, and Propitan.[2] Pipamperone was discovered at Janssen Pharmaceutica in 1961, and entered clinical trials in the United States in 1963.[4] Pharmacology{{clear left}}Pipamperone acts as an antagonist of the 5-HT2A,[5] 5-HT2B,[6] 5-HT2C[7] D2,[5] D3,[8] D4,[5][9] α1-adrenergic,[8] and α2-adrenergic receptors.[8] It shows much higher affinity for the 5-HT2A and D4 receptors over the D2 receptor (15-fold in the case of the D4 receptor, and even higher in the case of the 5-HT2A receptor),[5][8][10] being regarded as "highly selective" for the former two sites at low doses.[10][11] Pipamperone has low and likely insignificant affinity for the H1 and mACh receptors, as well as for other serotonin and dopamine receptors.[8] Pipamperone is considered to have been a forerunner to the atypical antipsychotics, if not an atypical antipsychotic itself, due to its prominent serotonin antagonism.[12][13][14] It is also used to normalise mood and sleep patterns and has antianxiety effects in neurotic patients.[15] Antidepressant effectsLow-dose pipamperone (5 mg twice daily) has been found to accelerate and enhance the antidepressant effect of citalopram (40 mg once daily), in a combination (citalopram/pipamperone) referred to as PipCit (code name PNB-01).[10][16] See also
References1. ^{{cite book|author1=Dr. Ian Morton|author2=I.K. Morton|author3=Judith M. Hall|title=Concise Dictionary of Pharmacological Agents: Properties and Synonyms|url=https://books.google.com/books?id=mqaOMOtk61IC&pg=PA222|date=31 October 1999|publisher=Springer Science & Business Media|isbn=978-0-7514-0499-9|pages=222–}} {{Antipsychotics}}{{Navboxes2. ^1 {{cite book|author=J. Elks|title=The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies|url=https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA985|date=14 November 2014|publisher=Springer|isbn=978-1-4757-2085-3|pages=985–}} 3. ^{{cite journal | vauthors = Ansoms C, Backer-Dierick GD, Vereecken JL | title = Sleep disorders in patients with severe mental depression: double-blind placebo-controlled evaluation of the value of pipamperone (Dipiperon) | journal = Acta Psychiatrica Scandinavica | volume = 55 | issue = 2 | pages = 116–22 | date = February 1977 | pmid = 320830 | doi = 10.1111/j.1600-0447.1977.tb00147.x }} 4. ^{{cite book|author=David Healy|title=The Creation of Psychopharmacology|url=https://books.google.com/books?id=6O2rPJnyhj0C&pg=PA251|date=1 July 2009|publisher=Harvard University Press|isbn=978-0-674-03845-5|pages=251–}} 5. ^1 2 3 {{cite journal | vauthors = Schotte A, Janssen PF, Gommeren W, Luyten WH, Van Gompel P, Lesage AS, De Loore K, Leysen JE | title = Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding | journal = Psychopharmacology | volume = 124 | issue = 1–2 | pages = 57–73 | date = March 1996 | pmid = 8935801 | doi = 10.1007/bf02245606 | url = http://link.springer.de/link/service/journals/00213/bibs/61241-2/61240057.htm }} 6. ^{{cite journal | vauthors = Wainscott DB, Lucaites VL, Kursar JD, Baez M, Nelson DL | title = Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 276 | issue = 2 | pages = 720–7 | date = February 1996 | pmid = 8632342 | doi = | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8632342 }} 7. ^{{cite journal | vauthors = Prinssen EP, Koek W, Kleven MS | title = The effects of antipsychotics with 5-HT(2C) receptor affinity in behavioral assays selective for 5-HT(2C) receptor antagonist properties of compounds | journal = European Journal of Pharmacology | volume = 388 | issue = 1 | pages = 57–67 | date = January 2000 | pmid = 10657547 | doi = 10.1016/s0014-2999(99)00859-6 | url = http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(99)00859-6 }} 8. ^1 2 3 4 {{cite book|author1=Bart A. Ellenbroek|author2=Alexander R. Cools|title=Atypical Antipsychotics|url=https://books.google.com/books?id=08kGCAAAQBAJ&pg=PA62|date=6 December 2012|publisher=Birkhäuser|isbn=978-3-0348-8448-8|pages=62–}} 9. ^{{cite journal | vauthors = Van Craenenbroeck K, Gellynck E, Lintermans B, Leysen JE, Van Tol HH, Haegeman G, Vanhoenacker P | title = Influence of the antipsychotic drug pipamperone on the expression of the dopamine D4 receptor | journal = Life Sciences | volume = 80 | issue = 1 | pages = 74–81 | date = December 2006 | pmid = 16978659 | doi = 10.1016/j.lfs.2006.08.024 }} 10. ^1 2 {{cite journal | vauthors = Wade AG, Crawford GM, Nemeroff CB, Schatzberg AF, Schlaepfer T, McConnachie A, Haazen L, Buntinx E | title = Citalopram plus low-dose pipamperone versus citalopram plus placebo in patients with major depressive disorder: an 8-week, double-blind, randomized study on magnitude and timing of clinical response | journal = Psychological Medicine | volume = 41 | issue = 10 | pages = 2089–97 | date = October 2011 | pmid = 21349239 | doi = 10.1017/S0033291711000158 }} 11. ^{{cite book|author=Michael S. Lidow|title=Neurotransmitter Receptors in Actions of Antipsychotic Medications|url=https://books.google.com/books?id=HIHLBQAAQBAJ&pg=PA88|date=22 June 2000|publisher=CRC Press|isbn=978-1-4200-4177-4|pages=88–}} 12. ^{{cite journal | vauthors = Awouters FH, Lewi PJ | title = Forty years of antipsychotic Drug research--from haloperidol to paliperidone--with Dr. Paul Janssen | journal = Arzneimittel-Forschung | volume = 57 | issue = 10 | pages = 625–32 | year = 2007 | pmid = 18074755 | doi = 10.1055/s-0031-1296660 }} 13. ^{{cite journal | vauthors = Vanden Bussche G, Gelders YG, Heylen SL | title = [Development of new antipsychotic drugs] | language = Spanish | journal = Acta Psiquiatrica y Psicologica de America Latina | volume = 36 | issue = 1–2 | pages = 13–25 | year = 1990 | pmid = 2127339 | doi = }} 14. ^{{cite journal | vauthors = Niemegeers CJ, Awouters F, Janssen PA | title = [Serotonin antagonism involved in the antipsychotic effect. Confirmation with ritanserine and risperidone] | language = French | journal = L'Encephale | volume = 16 | issue = 2 | pages = 147–51 | year = 1990 | pmid = 1693560 | doi = }} 15. ^{{Cite book|url=https://books.google.com/?id=oK7tCAAAQBAJ&pg=PA36&lpg=PA36&dq=pipamperone+mania#v=onepage&q=pipamperone%20mania&f=false|title=Psychotropic Agents: Part I: Antipsychotics and Antidepressants|date=2012-12-06|publisher=Springer Science & Business Media|isbn=9783642675386|language=en}} 16. ^{{cite journal | vauthors = Kirk R | title = Clinical trials in CNS--SMi's eighth annual conference | journal = IDrugs | volume = 13 | issue = 2 | pages = 66–9 | date = February 2010 | pmid = 20127552 | doi = }} | title = Pharmacodynamics | titlestyle = background:#ccccff | list1 ={{Adrenergic receptor modulators}}{{Dopamine receptor modulators}}{{Serotonin receptor modulators}} }} 15 : 5-HT2A antagonists|5-HT2B antagonists|5-HT2C antagonists|Alpha-1 blockers|Alpha-2 blockers|Carboxamides|Belgian inventions|Butyrophenone antipsychotics|D2 antagonists|D3 antagonists|D4 antagonists|Janssen Pharmaceutica|Fluoroarenes|Piperidines|Typical antipsychotics |
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