| 词条 | Piquindone |
| 释义 |
| IUPAC_name = (4aS,8aS)-3-ethyl-2,6-dimethyl-1,4a,5,6,7,8,8a,9-octahydro-4H-pyrrolo[2,3-g]isoquinolin-4-one | image = Piquindone.png | tradename = | pregnancy_category = | legal_status = Uncontrolled | routes_of_administration = Oral | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number = 78541-97-6 | CAS_supplemental = 83784-19-4 (hydrochloride) | ATC_prefix = none | ATC_suffix = | PubChem = 121903 | ChemSpiderID = 108751 | ChEMBL = 1192678 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = O1C9WXY65C | C=15 | H=22 | N=2 | O=1 | molecular_weight = 246.35 g/mol | smiles = O=C2c1c([nH]c(c1CC)C)C[C@H]3[C@H]2CN(CC3)C }}Piquindone (Ro 22-1319) is an atypical antipsychotic with a tricyclic structure that was developed in the 1980s but was never marketed.[1][2][3] It acts as a selective D2 receptor antagonist,[4][5][6] though based on its effects profile its selectivity may be considered controversial. Unlike most other D2 receptor ligands, piquindone displays Na2+-dependent binding, a property it shares with tropapride, zetidoline, and metoclopramide.[7] In clinical trials piquindone was found to possess moderate efficacy in treating positive symptoms of schizophrenia, and notably, was also modestly effective for negative symptoms, though this was just under statistical significance.[1] Additionally, relative to haloperidol, it was found to possesses significantly fewer extrapyramidal symptoms and had a much lower propensity for inducing tardive dyskinesia, indicating its atypical nature.[1][3] In addition to psychosis, piquindone has also been found to be effective in the treatment of Tourette's syndrome in numerous clinical studies.[8][9][10][11] See also
References1. ^1 2 {{cite journal |vauthors=Cohen JD, Van Putten T, Marder S, Berger PA, Stahl SM | title = The efficacy of piquindone, a new atypical neuroleptic, in the treatment of the positive and negative symptoms of schizophrenia | journal = Journal of Clinical Psychopharmacology | volume = 7 | issue = 5 | pages = 324–9 |date=October 1987 | pmid = 2890671 | doi = 10.1097/00004714-198710000-00006| url = }} {{Antipsychotics}}{{Dopaminergics}}{{Tricyclics}}2. ^{{cite journal |vauthors=Olson GL, Cheung HC, Morgan KD, etal | title = A dopamine receptor model and its application in the design of a new class of rigid pyrrolo[2,3-g]isoquinoline antipsychotics | journal = Journal of Medicinal Chemistry | volume = 24 | issue = 9 | pages = 1026–34 |date=September 1981 | pmid = 6116805 | doi = 10.1021/jm00141a002| url = }} 3. ^1 {{cite journal |vauthors=Davidson AB, Boff E, MacNeil DA, Wenger J, Cook L | title = Pharmacological effects of Ro 22-1319: a new antipsychotic agent | journal = Psychopharmacology | volume = 79 | issue = 1 | pages = 32–9 | year = 1983 | pmid = 6132425 | doi = 10.1007/BF00433013| url = }} 4. ^{{cite journal |vauthors=Nakajima T, Iwata K | title = [3H]Ro 22-1319 (piquindone) binds to the D2 dopaminergic receptor subtype in a sodium-dependent manner | journal = Molecular Pharmacology | volume = 26 | issue = 3 | pages = 430–8 |date=November 1984 | pmid = 6149457 | doi = | url = http://molpharm.aspetjournals.org/cgi/pmidlookup?view=long&pmid=6149457}} 5. ^{{cite journal |vauthors=Pugh MT, O'Boyle KM, Molloy AG, Waddington JL | title = Effects of the putative D-1 antagonist SCH 23390 on stereotyped behaviour induced by the D-2 agonist RU24213 | journal = Psychopharmacology | volume = 87 | issue = 3 | pages = 308–12 | year = 1985 | pmid = 2934758 | doi = 10.1007/BF00432713| url = }} 6. ^{{cite journal |vauthors=Molloy AG, O'Boyle KM, Pugh MT, Waddington JL | title = Locomotor behaviors in response to new selective D-1 and D-2 dopamine receptor agonists, and the influence of selective antagonists | journal = Pharmacology Biochemistry and Behavior | volume = 25 | issue = 1 | pages = 249–53 |date=July 1986 | pmid = 3529126 | doi = 10.1016/0091-3057(86)90262-5| url = http://linkinghub.elsevier.com/retrieve/pii/0091-3057(86)90262-5}} 7. ^{{cite journal |vauthors=Collin S, Vercauteren DP, Vanderveken D, Evrard G, Durant F | title = Structural requirements of Na+-dependent antidopaminergic agents: Tropapride, Piquindone, Zetidoline, and Metoclopramide. Comparison with Na+-independent ligands | journal = Journal of Computer-aided Molecular Design | volume = 3 | issue = 1 | pages = 39–53 |date=March 1989 | pmid = 2715795 | doi = 10.1007/BF01590994| url = }} 8. ^{{cite journal |vauthors=Uhr SB, Berger PA, Pruitt B, Stahl SM | title = Treatment of Tourette's syndrome with RO22-1319, a D-2-receptor antagonist | journal = The New England Journal of Medicine | volume = 311 | issue = 15 | pages = 989 |date=October 1984 | pmid = 6147753 | doi = 10.1056/NEJM198410113111517| url = }} 9. ^{{cite journal |vauthors=Uhr SB, Pruitt B, Berger PA, Stahl SM | title = Case report of four patients with Tourette syndrome treated with piquindone, a D2 receptor antagonist | journal = Journal of Clinical Psychopharmacology | volume = 6 | issue = 2 | pages = 128–30 |date=April 1986 | pmid = 2871057 | doi = 10.1097/00004714-198604000-00028| url = }} 10. ^{{cite journal |vauthors=Uhr SB, Pruitt B, Berger PA, Stahl SM | title = Improvement of symptoms in Tourette syndrome by piquindone, a novel dopamine-2 receptor antagonist | journal = International Clinical Psychopharmacology | volume = 1 | issue = 3 | pages = 216–20 |date=July 1986 | pmid = 3549873 | doi = 10.1097/00004850-198607000-00004| url = }} 11. ^{{cite journal |vauthors=Jiménez-Jiménez FJ, García-Ruiz PJ | title = Pharmacological options for the treatment of Tourette's disorder | journal = Drugs | volume = 61 | issue = 15 | pages = 2207–20 | year = 2001 | pmid = 11772131 | doi = 10.2165/00003495-200161150-00005| url = http://content.wkhealth.com/linkback/openurl?issn=0012-6667&volume=61&issue=15&spage=2207}} 2 : Atypical antipsychotics|Pyrroloisoquinolines |
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