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词条 Naphthylpiperazine
释义

  1. See also

  2. References

{{Drugbox
| IUPAC_name = 1-(naphthalen-1-yl)piperazine
| image = Naphthylpiperazine.png
| width = 125px
| alt = Skeletal formula of naphthylpiperazine
| image2 = Naphthylpiperazine-3D-balls.png
| width2 = 140
| alt2 = Ball-and-stick model of the naphthylpiperazine molecule
| tradename =
| pregnancy_category =
| legal_status = Uncontrolled
| routes_of_administration = Oral
| bioavailability =
| metabolism =
| elimination_half-life =
| excretion =
| CAS_number = 57536-86-4
| ATC_prefix = none
| ATC_suffix =
| PubChem = 1342
| IUPHAR_ligand = 3
| ChemSpiderID = 1302
| C=14 | H=16 | N=2
| molecular_weight = 212.29 g/mol
| smiles = c2cc(c1ccccc1c2)N3CCNCC3
}}

1-(1-Naphthyl)piperazine (1-NP) is a drug which is a phenylpiperazine derivative. It acts as a non-selective, mixed serotonergic agent, exerting partial agonism at the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F receptors,[1][2][3] while antagonizing the 5-HT2A, 5-HT2B, and 5-HT2C receptors.[4][5][6] It has also been shown to possess high affinity for the 5-HT3, 5-HT5A, 5-HT6, and 5-HT7 receptors,[7][8][9][10] and may bind to 5-HT4 and the SERT as well.[11][12] In animals it produces effects including hyperphagia,[13][14][15] hyperactivity,[16][17] and anxiolysis,[17][18][19][20] of which are all likely mediated predominantly or fully by blockade of the 5-HT2C receptor.

See also

  • Substituted piperazine
  • Diphenylpiperazine
  • Phenylpiperazine

References

1. ^{{cite journal |vauthors=Schoeffter P, Hoyer D | title = Interaction of arylpiperazines with 5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D receptors: do discriminatory 5-HT1B receptor ligands exist? | journal = Naunyn-Schmiedeberg's Archives of Pharmacology | volume = 339 | issue = 6 | pages = 675–83 |date=June 1989 | pmid = 2770889 | doi = 10.1007/bf00168661| url = }}
2. ^{{cite journal |vauthors=Bai F, Yin T, Johnstone EM, etal | title = Molecular cloning and pharmacological characterization of the guinea pig 5-HT1E receptor | journal = European Journal of Pharmacology | volume = 484 | issue = 2–3 | pages = 127–39 |date=January 2004 | pmid = 14744596 | doi = 10.1016/j.ejphar.2003.11.019| url = http://linkinghub.elsevier.com/retrieve/pii/S0014299903026633}}
3. ^{{cite journal |vauthors=Adham N, Kao HT, Schecter LE, etal | title = Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 90 | issue = 2 | pages = 408–12 |date=January 1993 | pmid = 8380639 | pmc = 45671 | doi = 10.1073/pnas.90.2.408| url = }}
4. ^{{cite journal |vauthors=Conn PJ, Sanders-Bush E | title = Relative efficacies of piperazines at the phosphoinositide hydrolysis-linked serotonergic (5-HT-2 and 5-HT-1c) receptors | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 242 | issue = 2 | pages = 552–7 |date=August 1987 | pmid = 3039120 | doi = | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=3039120}}
5. ^{{cite journal |vauthors=McKune CM, Watts SW | title = Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 297 | issue = 1 | pages = 88–95 |date=April 2001 | pmid = 11259531 | doi = | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=11259531}}
6. ^{{cite journal |vauthors=Kursar JD, Nelson DL, Wainscott DB, Baez M | title = Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor | journal = Molecular Pharmacology | volume = 46 | issue = 2 | pages = 227–34 |date=August 1994 | pmid = 8078486 | doi = | url = http://molpharm.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8078486}}
7. ^{{cite journal |vauthors=Glennon RA, Ismaiel AE, McCarthy BG, Peroutka SJ | title = Binding of arylpiperazines to 5-HT3 serotonin receptors: results of a structure-affinity study | journal = European Journal of Pharmacology | volume = 168 | issue = 3 | pages = 387–92 |date=September 1989 | pmid = 2583244 | doi = 10.1016/0014-2999(89)90802-9| url = }}
8. ^{{cite journal | author = Wesołowska A | title = In the search for selective ligands of 5-HT5, 5-HT6 and 5-HT7 serotonin receptors | journal = Polish Journal of Pharmacology | volume = 54 | issue = 4 | pages = 327–41 | year = 2002 | pmid = 12523486 | doi = | url = }}
9. ^{{cite journal |vauthors=Lee M, Rangisetty JB, Pullagurla MR, etal | title = 1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands | journal = Bioorganic & Medicinal Chemistry Letters | volume = 15 | issue = 6 | pages = 1707–11 |date=March 2005 | pmid = 15745826 | doi = 10.1016/j.bmcl.2005.01.031 | url = http://linkinghub.elsevier.com/retrieve/pii/S0960-894X(05)00078-8}}
10. ^{{cite journal |vauthors=Bard JA, Zgombick J, Adham N, Vaysse P, Branchek TA, Weinshank RL | title = Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase | journal = The Journal of Biological Chemistry | volume = 268 | issue = 31 | pages = 23422–6 |date=November 1993 | pmid = 8226867 | doi = | url = http://www.jbc.org/cgi/pmidlookup?view=long&pmid=8226867}}
11. ^{{cite journal |vauthors=Curtet S, Soulier JL, Zahradnik I, etal | title = New arylpiperazine derivatives as antagonists of the human cloned 5-HT(4) receptor isoforms | journal = Journal of Medicinal Chemistry | volume = 43 | issue = 20 | pages = 3761–9 |date=October 2000 | pmid = 11020291| doi = 10.1021/jm0009538}}
12. ^{{cite journal |vauthors=Perrone R, Berardi F, Colabufo NA, etal | title = Design and synthesis of long-chain arylpiperazines with mixed affinity for serotonin transporter (SERT) and 5-HT(1A) receptor | journal = The Journal of Pharmacy and Pharmacology | volume = 57 | issue = 10 | pages = 1319–27 |date=October 2005 | pmid = 16259761 | doi = 10.1211/jpp.57.10.0011 | url = http://openurl.ingenta.com/content/nlm?genre=article&issn=0022-3573&volume=57&issue=10&spage=1319&aulast=Perrone}}
13. ^{{cite journal |vauthors=Kennett GA, Curzon G | title = Evidence that hypophagia induced by mCPP and TFMPP requires 5-HT1C and 5-HT1B receptors; hypophagia induced by RU 24969 only requires 5-HT1B receptors | journal = Psychopharmacology | volume = 96 | issue = 1 | pages = 93–100 | year = 1988 | pmid = 2906446 | doi = 10.1007/BF02431539| url = }}
14. ^{{cite journal |vauthors=Gibson EL, Kennedy AJ, Curzon G | title = d-Fenfluramine- and d-norfenfluramine-induced hypophagia: differential mechanisms and involvement of postsynaptic 5-HT receptors | journal = European Journal of Pharmacology | volume = 242 | issue = 1 | pages = 83–90 |date=September 1993 | pmid = 8223940 | doi = 10.1016/0014-2999(93)90013-8| url = http://linkinghub.elsevier.com/retrieve/pii/0014-2999(93)90013-8}}
15. ^{{cite journal |vauthors=Schechter LE, Simansky KJ | title = 1-(2,5-Dimethoxy-4-iodophenyl)-2-aminopropane (DOI) exerts an anorexic action that is blocked by 5-HT2 antagonists in rats | journal = Psychopharmacology | volume = 94 | issue = 3 | pages = 342–6 | year = 1988 | pmid = 3128809 | doi = 10.1007/bf00174687| url = }}
16. ^{{cite journal |vauthors=Perveen T, Rafiq R, Haider S, Haleem DJ | title = Increased serotonergic functions following administration of 1-(1-naphthyl) piperazine in propranolol injected rats | journal = Pakistan Journal of Pharmaceutical Sciences | volume = 19 | issue = 3 | pages = 194 |date=July 2006 | pmid = 16935825 | doi = | url = }}
17. ^1 {{cite journal | author = Kennett GA | title = 5-HT1C receptor antagonists have anxiolytic-like actions in the rat social interaction model | journal = Psychopharmacology | volume = 107 | issue = 2–3 | pages = 379–84 | year = 1992 | pmid = 1352056 | doi = 10.1007/BF02245165| url = }}
18. ^{{cite journal |vauthors=Pruus K, Rudisaar R, Vaarmann A, Matto V, Allikmets L | title = 1-(1-naphthyl)-piperazine, a mixed 5-HT1A and 5-HT2A/2C receptor ligand, elicits an anxiolytic-like effect in the open-field test without changes in 5-HT metabolism | journal = Methods and Findings in Experimental and Clinical Pharmacology | volume = 24 | issue = 3 | pages = 151–7 |date=April 2002 | pmid = 12087877 | doi = 10.1358/mf.2002.24.3.802300| url = http://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summaryn_pr?p_JournalId=6&p_RefId=802300}}
19. ^{{cite journal |vauthors=Gibson EL, Barnfield AM, Curzon G | title = Evidence that mCPP-induced anxiety in the plus-maze is mediated by postsynaptic 5-HT2C receptors but not by sympathomimetic effects | journal = Neuropharmacology | volume = 33 | issue = 3–4 | pages = 457–65 | year = 1994 | pmid = 7984284 | doi = 10.1016/0028-3908(94)90076-0| url = }}
20. ^{{cite journal |vauthors=Kennett GA, Pittaway K, Blackburn TP | title = Evidence that 5-HT2c receptor antagonists are anxiolytic in the rat Geller-Seifter model of anxiety | journal = Psychopharmacology | volume = 114 | issue = 1 | pages = 90–6 |date=February 1994 | pmid = 7846211 | doi = 10.1007/BF02245448| url = }}
{{Anxiolytics}}{{Serotonergics}}{{Piperazines}}

4 : Naphthalenes|Piperazines|Serotonin antagonists|Serotonin receptor agonists
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