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Revision as of 20:22, 10 December 2010 editRjwilmsi (talk | contribs)Extended confirmed users, Pending changes reviewers, Rollbackers932,009 editsm Journal cites:, added 2 PMIDs, using AWB (7393)← Previous edit Latest revision as of 14:49, 27 September 2024 edit undo139.57.40.100 (talk)No edit summary 
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{{Short description|Chemical compound}}
{{drugbox
{{Drugbox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 401667456
| IUPAC_name = ''N''-ethyl]-''N''-(2-pyridyl)cyclohexanecarboxamide
| synonyms =
| image = WAY-100,635.png | image = WAY-100,635.png
| width=200 | width = 200
<!--Clinical data-->
| IUPAC_name = ''N''-ethyl]- ''N''-(2-pyridyl)cyclohexanecarboxamide
| OtherNames = | tradename =
<!--Identifiers-->
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 146714-97-8 | CAS_number = 146714-97-8
| UNII_Ref = {{fdacite|correct|FDA}}
| PubChem=5684
| UNII = 8S48P899NE
| PubChem = 5684
| IUPHAR_ligand = 80 | IUPHAR_ligand = 80
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| SMILES=O=C(C1CCCCC1)N(CCN2CCN(c3ccccc3OC)CC2)c4ncccc4
| ChEMBL = 31354
| C=25|H=34|N=4|O=2
| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}
| molecular_weight = 422.56 g/mol
| ChemSpiderID = 5482
<!--Chemical data-->
| C=25 | H=34 | N=4 | O=2
| smiles = COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4
| StdInChI_Ref = {{stdinchicite|changed|chemspider}}
| StdInChI = 1S/C25H34N4O2/c1-31-23-12-6-5-11-22(23)28-18-15-27(16-19-28)17-20-29(24-13-7-8-14-26-24)25(30)21-9-3-2-4-10-21/h5-8,11-14,21H,2-4,9-10,15-20H2,1H3
| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}
| StdInChIKey = SBPRIAGPYFYCRT-UHFFFAOYSA-N
}} }}


'''WAY-100,635''' is a ] ] and research chemical widely used in scientific studies. It was originally believed to act as a selective ] ] ], but subsequent research showed that it also acts as ] ] at the ] receptor.<ref>{{Cite journal | author = C. A. Fornal, C. W. Metzler, R. A. Gallegos, S. C. Veasey, A. C. McCreary and B. L. Jacobs | title = WAY-100635, a potent and selective 5-hydroxytryptamine1A antagonist, increases serotonergic neuronal activity in behaving cats: comparison with (S)-WAY-100135 | journal = ] | volume = 278 | issue = 2 | pages = 752&ndash;762 | year = 1996 | url = http://jpet.aspetjournals.org/cgi/content/abstract/278/2/752 | pmid = 8768728 }}</ref><ref>{{Cite journal | author = Benjamin R. Chemel, Bryan L. Roth, Blaine Armbruster, Val J. Watts and ] | title = WAY-100635 is a potent dopamine D4 receptor agonist | journal = ] | month = October | volume = 188 | issue = 2 | pages = 244–251 | year = 2006 | pmid = 16915381 | url = http://www.springerlink.com/content/vt36125287348028/ | doi = 10.1007/s00213-006-0490-4 '''WAY-100635''' is a ] ] and ] widely used in scientific studies. It was originally believed to act as a selective ] ], but subsequent research showed that it also acts as ] ] at the ] receptor.<ref>{{cite journal | vauthors = Fornal CA, Metzler CW, Gallegos RA, Veasey SC, McCreary AC, Jacobs BL | title = WAY-100635, a potent and selective 5-hydroxytryptamine1A antagonist, increases serotonergic neuronal activity in behaving cats: comparison with (S)-WAY-100135 | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 278 | issue = 2 | pages = 752–762 | date = August 1996 | pmid = 8768728 | url = http://jpet.aspetjournals.org/cgi/content/abstract/278/2/752 }}</ref><ref>{{cite journal | vauthors = Chemel BR, Roth BL, Armbruster B, Watts VJ, Nichols DE | title = WAY-100635 is a potent dopamine D4 receptor agonist | journal = Psychopharmacology | volume = 188 | issue = 2 | pages = 244–251 | date = October 2006 | pmid = 16915381 | doi = 10.1007/s00213-006-0490-4 | author2-link = Bryan Roth | s2cid = 24194034 | author5-link = David E. Nichols }}</ref><ref name="pmid19179855">{{cite journal | vauthors = Marona-Lewicka D, Nichols DE | title = WAY 100635 produces discriminative stimulus effects in rats mediated by dopamine D(4) receptor activation | journal = Behavioural Pharmacology | volume = 20 | issue = 1 | pages = 114–118 | date = February 2009 | pmid = 19179855 | doi = 10.1097/FBP.0b013e3283242f1a | s2cid = 43332577 }}</ref> It is sometimes referred to as a ] at the former receptor.<ref>{{cite journal | vauthors = Fletcher A, Forster EA, Bill DJ, Brown G, Cliffe IA, Hartley JE, Jones DE, McLenachan A, Stanhope KJ, Critchley DJ, Childs KJ, Middlefell VC, Lanfumey L, Corradetti R, Laporte AM, Gozlan H, Hamon M, Dourish CT | display-authors = 6 | title = Electrophysiological, biochemical, neurohormonal and behavioural studies with WAY-100635, a potent, selective and silent 5-HT1A receptor antagonist | journal = Behavioural Brain Research | volume = 73 | issue = 1–2 | pages = 337–353 | year = 1996 | pmid = 8788530 | doi = 10.1016/0166-4328(96)00118-0 | s2cid = 18229202 }}</ref> It is closely related to ].
}}</ref><ref name="pmid19179855">{{cite journal |author=Marona-Lewicka D, Nichols DE |title=WAY 100635 produces discriminative stimulus effects in rats mediated by dopamine D(4) receptor activation |journal=Behav Pharmacol |volume=20 |issue=1 |pages=114–8 |year=2009 |pmid=19179855 |doi=10.1097/FBP.0b013e3283242f1a |url=}}</ref> It is sometimes referred to as a ] at the former receptor.<ref>{{Cite journal | author = A. Fletcher, E. A. Forster, D. J. Bill, G. Brown, I. A. Cliffe, J. E. Hartley, D. E. Jones, A. McLenachan, K. J. Stanhope, D. J. Critchley, K. J. Childs, V. C. Middlefell, L. Lanfumey, R. Corradetti, A. M. Laporte, H. Gozlan, M. Hamon & C. T. Dourish | title = Electrophysiological, biochemical, neurohormonal and behavioural studies with WAY-100635, a potent, selective and silent 5-HT1A receptor antagonist | journal = ] | volume = 73 | issue = 1-2 | pages = 337–333 | year = 1996 | month = | pmid = 8788530 | doi = 10.1016/0166-4328(96)00118-0 }}</ref> It is closely related to ].


In light of its only recently discovered ] activity, conclusions drawn from studies that employed WAY-100635 as a selective 5-HT<sub>1A</sub> antagonist may need to be re-evaluated. In light of its ] activity, conclusions drawn from studies that employ WAY-100635 as a selective 5-HT<sub>1A</sub> antagonist may need to be re-evaluated.<ref>{{cite journal | vauthors = Chemel BR, Roth BL, Armbruster B, Watts VJ, Nichols DE | title = WAY-100635 is a potent dopamine D4 receptor agonist | journal = Psychopharmacology | volume = 188 | issue = 2 | pages = 244–251 | date = October 2006 | pmid = 16915381 | doi = 10.1007/s00213-006-0490-4 | s2cid = 24194034 }}</ref>


== Human PET studies == == Human PET studies ==
In human PET studies WAY-100,635 shows high binding in the ], ], ] and ], while lower in ] and ].<ref>{{Cite journal In human PET studies WAY-100635 shows high binding in the ], ], ] and ], while lower in ] and ].<ref>{{cite journal | vauthors = Ito H, Halldin C, Farde L | title = Localization of 5-HT1A receptors in the living human brain using WAY-100635: PET with anatomic standardization technique | journal = Journal of Nuclear Medicine | volume = 40 | issue = 1 | pages = 102–109 | date = January 1999 | pmid = 9935065 | url = http://jnm.snmjournals.org/cgi/content/abstract/40/1/102 | name-list-style = amp }}</ref>
One study described a single case with relatively high binding in the cerebellum.<ref>{{cite journal | vauthors = Hirvonen J, Kajander J, Allonen T, Oikonen V, Någren K, Hietala J | title = Measurement of serotonin 5-HT1A receptor binding using positron emission tomography and WAY-100635-considerations on the validity of cerebellum as a reference region | journal = Journal of Cerebral Blood Flow and Metabolism | volume = 27 | issue = 1 | pages = 185–195 | date = January 2007 | pmid = 16685258 | doi = 10.1038/sj.jcbfm.9600326 | doi-access = free }}</ref>
| author = Hiroshi Ito, Christer Halldin & Lars Farde
| title = Localization of 5-HT<sub>1A</sub> receptors in the living human brain using &#91;carbonyl-<sup>11</sup>C&#93;WAY-100635: PET with anatomic standardization technique
| journal = ]
| volume = 40
| issue = 1
| pages = 102–109
| year = 1999
| month = January
| pmid = 9935065
| url = http://jnm.snmjournals.org/cgi/content/abstract/40/1/102
}}</ref>
One study described a case with relatively high binding in the cerebellum.<ref>{{Cite journal
| author = Jussi Hirvonen, Jaana Kajander, Topias Allonen, Vesa Oikonen, Kjell Nagren & Jarmo Hietala
| title = Measurement of serotonin 5-HT1A receptor binding using positron emission tomography and &#91;''carbonyl''-<sup>11</sup>C&#93;WAY-100635&mdash;considerations on the validity of cerebellum as a reference region
| journal = ]
| volume = 27
| issue = 1
| pages = 185–185
| year = 2007
| month = January
| doi = 10.1038/sj.jcbfm.9600326
| pmid = 16685258
}}</ref>


In relating its binding to subject variables one Swedish study found WAY-100,635 binding in ] brain region correlating with ] and spiritual acceptance ]s.<ref name="BorgJ2003Serotonin">{{Cite journal In relating its binding to subject variables one Swedish study found WAY-100635 binding in ] brain region correlating with ] and spiritual acceptance ]s.<ref name="BorgJ2003Serotonin">{{cite journal | vauthors = Borg J, Andrée B, Soderstrom H, Farde L | title = The serotonin system and spiritual experiences | journal = The American Journal of Psychiatry | volume = 160 | issue = 11 | pages = 1965–1969 | date = November 2003 | pmid = 14594742 | doi = 10.1176/appi.ajp.160.11.1965 | s2cid = 5911066 }}</ref>
WAY-100635 binding has also been assessed in connection with ], where there has been disagreement about the presence and direction of the 5-HT<sub>1A</sub> receptor binding.<ref>{{cite journal | vauthors = Drevets WC, Thase ME, Moses-Kolko EL, Price J, Frank E, Kupfer DJ, Mathis C | title = Serotonin-1A receptor imaging in recurrent depression: replication and literature review | journal = Nuclear Medicine and Biology | volume = 34 | issue = 7 | pages = 865–877 | date = October 2007 | pmid = 17921037 | pmc = 2702715 | doi = 10.1016/j.nucmedbio.2007.06.008 }}</ref>
| author = Jacqueline Borg, Bengt Andrée, Henrik Soderstrom, Lars Farde
In healthy subjects WAY-100635 binding has been found to decline with ],<ref name="TauscherJ2001Serotonin">{{cite journal | vauthors = Tauscher J, Verhoeff NP, Christensen BK, Hussey D, Meyer JH, Kecojevic A, Javanmard M, Kasper S, Kapur S | display-authors = 6 | title = Serotonin 5-HT1A receptor binding potential declines with age as measured by WAY-100635 and PET | journal = Neuropsychopharmacology | volume = 24 | issue = 5 | pages = 522–530 | date = May 2001 | pmid = 11282252 | doi = 10.1016/S0893-133X(00)00227-X | doi-access = free }}</ref>
| title = The Serotonin System and Spiritual Experiences
&mdash; though not all studies have found this relationship.<ref name="RabinerE2002Database">{{cite journal | vauthors = Rabiner EA, Messa C, Sargent PA, Husted-Kjaer K, Montgomery A, Lawrence AD, Bench CJ, Gunn RN, Cowen P, Grasby PM | display-authors = 6 | title = A database of WAY-100635 binding to 5-HT(1A) receptors in normal male volunteers: normative data and relationship to methodological, demographic, physiological, and behavioral variables | journal = NeuroImage | volume = 15 | issue = 3 | pages = 620–632 | date = March 2002 | pmid = 11848705 | doi = 10.1006/nimg.2001.0984 | s2cid = 42080193 }}</ref><ref name="ParseyR2002Effects">{{cite journal | vauthors = Parsey RV, Oquendo MA, Simpson NR, Ogden RT, Van Heertum R, Arango V, Mann JJ | title = Effects of sex, age, and aggressive traits in man on brain serotonin 5-HT1A receptor binding potential measured by PET using WAY-100635 | journal = Brain Research | volume = 954 | issue = 2 | pages = 173–182 | date = November 2002 | pmid = 12414100 | doi = 10.1016/S0006-8993(02)03243-2 | s2cid = 20650203 }}</ref>
| journal = ]
| volume = 160
| issue = 11
| month = November
| year = 2003
| pages = 1965&ndash;1969
| url = http://ajp.psychiatryonline.org/cgi/content/full/160/11/1965
| doi = 10.1176/appi.ajp.160.11.1965
| pmid=14594742
}}</ref>
WAY-100,635 binding has also been assessed in connection with ], where there has been disagreement about the presence and direction of the 5-HT<sub>1A</sub> receptor binding.<ref>{{Cite journal
| author = Wayne C. Drevets, Michael E. Thase, Eydie L. Moses-Kolko, Julie Price, Ellen Frank, David J. Kupfer and Chester Mathis
| title = Serotonin-1A receptor imaging in recurrent depression: replication and literature review
| journal = ]
| year = 2007
| month = October
| volume = 34
| issue = 7
| pages = 865&ndash;877
| pmid = 17921037
| doi = 10.1016/j.nucmedbio.2007.06.008
| pmc = 2702715
}}</ref>
In healthy subjects WAY-100,635 binding has been found to decline with ],<ref name="TauscherJ2001Serotonin">{{Cite journal
| author = Johannes Tauscher, N. Paul L. G. Verhoeff, Bruce K. Christensen, Doug Hussey, Jeffrey H. Meyer, Alex Kecojevic, Mahan Javanmard, Siegfried Kasper
and Shitij Kapur
| title = Serotonin 5-HT<sub>1A</sub> Receptor Binding Potential Declines with Age as Measured by WAY-100635 and PET
| journal = ]
| volume = 24
| issue = 5
| month = May
| year = 2001
| pages = 522&ndash;530
| doi = 10.1016/S0893-133X(00)00227-X
}}</ref>
&mdash; though not all studies have found this relationship.<ref name="RabinerE2002Database">{{Cite journal
| author = Rabiner EA, Messa C, Sargent PA, Husted-Kjaer K, Montgomery A, Lawrence AD, Bench CJ, Gunn RN, Cowen P, Grasby PM.
| title = A database of WAY-100635 binding to 5-HT<sub>1A</sub> receptors in normal male volunteers: normative data and relationship to methodological, demographic, physiological, and behavioral variables
| journal = ]
| year = 2002
| month = March
| volume = 15
| issue = 3
| pages = 620&ndash;632
| pmid = 11848705
| doi = 10.1006/nimg.2001.0984
}}</ref><ref name="ParseyR2002Effects">{{Cite journal
| author = R. V. Parsey, M. A. Oquendo, N. R. Simpson, R. T. Ogden, R. Van Heertum, V. Arango V, J. J. Mann
| title = Effects of sex, age, and aggressive traits in man on brain serotonin 5-HT1A receptor binding potential measured by PET using WAY-100635
| journal = ]
| year = 2002
| month = November
| volume = 954
| issue = 2
| pages = 173&ndash;182
| pmid = 12414100
| doi = 10.1016/S0006-8993(02)03243-2
}}</ref>


{| class="wikitable" {| class="wikitable"
Line 143: Line 81:
| Positive correlation in the ] and ] | Positive correlation in the ] and ]
| 12 males | 12 males
| <ref>{{cite journal | vauthors = Lundberg J, Borg J, Halldin C, Farde L | title = A PET study on regional coexpression of 5-HT1A receptors and 5-HTT in the human brain | journal = Psychopharmacology | volume = 195 | issue = 3 | pages = 425–433 | date = December 2007 | pmid = 17874074 | doi = 10.1007/s00213-007-0928-3 | s2cid = 22272672 }}</ref>
| <ref>{{Cite journal
| author = Johan Lundberg, Jacqueline Borg, Christer Halldin and Lars Farde
| title = A PET study on regional coexpression of 5-HT<sub>1A</sub> receptors and 5-HTT in the human brain
| journal = ]
| volume = 195
| issue = 3
| month = December
| year = 2007
| doi = 10.1007/s00213-007-0928-3
| pages = 425&ndash;433
}}</ref>
|- |-
! Genetic variation !! Result !! Subjects !! Ref. ! Genetic variation !! Result !! Subjects !! Ref.
Line 160: Line 88:
| No difference found | No difference found
| 35 | 35
| <ref name="DavidS2005Functional">{{cite journal | vauthors = David SP, Murthy NV, Rabiner EA, Munafó MR, Johnstone EC, Jacob R, Walton RT, Grasby PM | display-authors = 6 | title = A functional genetic variation of the serotonin (5-HT) transporter affects 5-HT1A receptor binding in humans | journal = The Journal of Neuroscience | volume = 25 | issue = 10 | pages = 2586–2590 | date = March 2005 | pmid = 15758168 | pmc = 1942077 | doi = 10.1523/JNEUROSCI.3769-04.2005 }}</ref>
| <ref name="DavidS2005Functional">{{Cite journal
| author = Sean P. David, Naga Venkatesha Murthy, Eugenii A. Rabiner, Marcus R. Munafó, Elaine C. Johnstone, Robyn Jacob, Robert T. Walton & Paul M. Grasby
| title = A functional genetic variation of the serotonin (5-HT) transporter affects 5-HT1A receptor binding in humans
| journal = ]
| year = 2005
| month = March
| volume = 25
| issue = 10
| pages = 2586&ndash;2590
| url = http://www.jneurosci.org/cgi/content/full/25/10/2586
| pmid = 15758168
| doi = 10.1523/JNEUROSCI.3769-04.2005
| pmc = 1942077
}}</ref>
|- |-
| ].] polymorphism | ].] polymorphism
Line 185: Line 100:
| Reduction in ] and ] | Reduction in ] and ]
| 12+8 | 12+8
| <ref>{{cite journal | vauthors = Drevets WC, Frank E, Price JC, Kupfer DJ, Holt D, Greer PJ, Huang Y, Gautier C, Mathis C | display-authors = 6 | title = PET imaging of serotonin 1A receptor binding in depression | journal = Biological Psychiatry | volume = 46 | issue = 10 | pages = 1375–1387 | date = November 1999 | pmid = 10578452 | doi = 10.1016/S0006-3223(99)00189-4 | s2cid = 719822 }}</ref>
| <ref>{{Cite journal
| author = Wayne C. Drevets, Ellen Frank, Julie C. Price, David J. Kupfer, Daniel Holt, Phil J. Greer, Yiyun Huang, Clara Gautier and Chester Mathis
| title = Pet imaging of serotonin 1A receptor binding in depression
| journal = ]
| volume = 46
| issue = 10
| month = November
| year = 1999
| pages = 1375&ndash;1387
| doi = 10.1016/S0006-3223(99)00189-4
}}</ref>
|- |-
| ] (medicated and unmedicated) | ] (medicated and unmedicated)
| Reduction in "many of the regions examined" | Reduction in "many of the regions examined"
| 25+18 | 25+18
| <ref>{{cite journal | vauthors = Sargent PA, Kjaer KH, Bench CJ, Rabiner EA, Messa C, Meyer J, Gunn RN, Grasby PM, Cowen PJ | display-authors = 6 | title = Brain serotonin1A receptor binding measured by positron emission tomography with WAY-100635: effects of depression and antidepressant treatment | journal = Archives of General Psychiatry | volume = 57 | issue = 2 | pages = 174–180 | date = February 2000 | pmid = 10665620 | doi = 10.1001/archpsyc.57.2.174 | doi-access = }}</ref>
| <ref>{{Cite journal
| author = Peter A. Sargent, Karen Husted Kjaer, Christopher J. Bench, Eugenii A. Rabiner, Cristina Messa, Jeff Meyer, Roger N. Gunn, Paul M. Grasby, Philip J. Cowen
| title = Brain Serotonin<sub>1A</sub> Receptor Binding Measured by Positron Emission Tomography With WAY-100635. Effects of Depression and Antidepressant Treatment
| journal = Archieves of General Psychiatry
| volume = 57
| issue = 2
| pages = 174&ndash;180
| month = February
| year = 2000
| url = http://archpsyc.highwire.org/cgi/content/abstract/57/2/174
| doi = 10.1001/archpsyc.57.2.174
}}</ref>
|- |-
| ] in treated and untreated patients | ] in treated and untreated patients
| Reducing in binding in ] in both treated and untreated. Reduced binding in global postsynaptic regions for untreated, while no or little reduction for treated. | Reducing in binding in ] in both treated and untreated. Reduced binding in global postsynaptic regions for untreated, while no or little reduction for treated.
| 9+7+19 | 9+7+19
| <ref>{{cite journal | vauthors = Nash JR, Sargent PA, Rabiner EA, Hood SD, Argyropoulos SV, Potokar JP, Grasby PM, Nutt DJ | display-authors = 6 | title = Serotonin 5-HT1A receptor binding in people with panic disorder: positron emission tomography study | journal = The British Journal of Psychiatry | volume = 193 | issue = 3 | pages = 229–234 | date = September 2008 | pmid = 18757983 | doi = 10.1192/bjp.bp.107.041186 | doi-access = free }}</ref>
| <ref>{{Cite journal
| author = Jon R. Nash, Peter A. Sargent, Eugenii A. Rabiner, Sean D. Hood, Paul M. Grasby & David J. Nutt
| title = Serotonin 5-HT<sub>1A</sub> receptor binding in people with panic disorder: positron emission tomography study
| journal = ]
| year = 2008
| volume = 193
| pages = 229&ndash;234
| doi = 10.1192/bjp.bp.107.041186
| url = http://bjp.rcpsych.org/cgi/content/full/193/3/229
}}</ref>
|- |-
| ] | ]
| Decrease in right ] | Decrease in right ]
| 10+10 | 10+10
| <ref>{{cite journal | vauthors = Lanctôt KL, Hussey DF, Herrmann N, Black SE, Rusjan PM, Wilson AA, Houle S, Kozloff N, Verhoeff NP, Kapur S | display-authors = 6 | title = A positron emission tomography study of 5-hydroxytryptamine-1A receptors in Alzheimer disease | journal = The American Journal of Geriatric Psychiatry | volume = 15 | issue = 10 | pages = 888–898 | date = October 2007 | pmid = 17567932 | doi = 10.1097/JGP.0b013e3180488325 }}</ref>
| <ref>{{Cite journal
| author = Krista L. Lanctôt, Doug F. Hussey, Nathan Herrmann, , Sandra E. Black, Pablo M. Rusjan, Alan A. Wilson, Sylvain Houle, Nicole Kozloff, Nicholaas Paul L.G. Verhoeff, and Shitij Kapur
| title = A positron emission tomography study of 5-hydroxytryptamine-1A receptors in Alzheimer disease
| journal = ]
| year = 2007
| month = October
| volume = 15
| issue = 10
| pages = 888&ndash;898
| pmid = 17567932
| url = http://ajgponline.org/cgi/content/abstract/15/10/888
| doi = 10.1097/JGP.0b013e3180488325
}}</ref>
|} |}


===Radioligands=== ===Radioligands===
Labeled with the ] ] it is used as a ] in ] (PET) studies to determine ] binding in the ].<ref>{{Cite journal Labeled with the ] ] it is used as a ] in ] (PET) studies to determine ] binding in the ].<ref>{{cite journal | vauthors = Pike VW, McCarron JA, Lammerstma AA, Hume SP, Poole K, Grasby PM, Malizia A, Cliffe IA, Fletcher A, Bench CJ | display-authors = 6 | title = First delineation of 5-HT1A receptors in human brain with PET and WAY-100635 | journal = European Journal of Pharmacology | volume = 283 | issue = 1–3 | pages = R1–R3 | date = September 1995 | pmid = 7498295 | doi = 10.1016/0014-2999(95)00438-Q }}</ref>
WAY-100635 may be labeled in different ways with carbon-11:
| author = Victor W. Pike, Julie A. McCarron, Adriaan A. Lammerstma, Susan P. Hume, Keith Poole, Paul M. Grasby, Andrea Malizia, Ian A. Cliffe, Allan Fletcher & Christopher J. Bench
As WAY-100635 or WAY-100635, with WAY-100635 regarded as "far superior".<ref>{{cite journal | vauthors = Pike VW, McCarron JA, Lammertsma AA, Osman S, Hume SP, Sargent PA, Bench CJ, Cliffe IA, Fletcher A, Grasby PM | display-authors = 6 | title = Exquisite delineation of 5-HT1A receptors in human brain with PET and WAY-100635 | journal = European Journal of Pharmacology | volume = 301 | issue = 1–3 | pages = R5–R7 | date = April 1996 | pmid = 8773468 | doi = 10.1016/0014-2999(96)00079-9 }}</ref>
| title = First delineation of 5-HT<sub>1A</sub> receptors in human brain with PET and WAY-100635
Labeled with ] WAY-100635 may also be used in ].<ref>{{cite journal | vauthors = Hume SP, Ashworth S, Opacka-Juffry J, Ahier RG, Lammertsma AA, Pike VW, Cliffe IA, Fletcher A, White AC | display-authors = 6 | title = Evaluation of WAY-100635 as an in vivo radioligand for 5-HT1A receptors in rat brain | journal = European Journal of Pharmacology | volume = 271 | issue = 2–3 | pages = 515–523 | date = December 1994 | pmid = 7705452 | doi = 10.1016/0014-2999(94)90813-3 }}</ref>
| journal = ]
WAY-100635 has higher 5-HT1A affinity than ].<ref>{{cite journal | vauthors = Burnet PW, Eastwood SL, Harrison PJ | title = WAY-100635 for 5-HT1A receptor autoradiography in human brain: a comparison with 8-OH-DPAT and demonstration of increased binding in the frontal cortex in schizophrenia | journal = Neurochemistry International | volume = 30 | issue = 6 | pages = 565–574 | date = June 1997 | pmid = 9152998 | doi = 10.1016/S0197-0186(96)00124-6 | s2cid = 21135585 }}</ref>
| volume = 283

| month = September
==Other actions==
| year = 1995
WAY-100635 has also been found to increase the analgesic effects of ] drugs in a dose-dependent manner, in contrast to 5-HT<sub>1A</sub> agonists such as ] which were found to reduce opioid analgesia.<ref name="pmid15109976">{{cite journal | vauthors = Bardin L, Colpaert FC | title = Role of spinal 5-HT(1A) receptors in morphine analgesia and tolerance in rats | journal = European Journal of Pain | volume = 8 | issue = 3 | pages = 253–261 | date = June 2004 | pmid = 15109976 | doi = 10.1016/j.ejpain.2003.09.002 | s2cid = 25580572 }}</ref><ref name="pmid17393145">{{cite journal | vauthors = Berrocoso E, De Benito MD, Mico JA | title = Role of serotonin 5-HT1A and opioid receptors in the antiallodynic effect of tramadol in the chronic constriction injury model of neuropathic pain in rats | journal = Psychopharmacology | volume = 193 | issue = 1 | pages = 97–105 | date = July 2007 | pmid = 17393145 | doi = 10.1007/s00213-007-0761-8 | s2cid = 21898521 }}</ref> However, since 5-HT<sub>1A</sub> agonists were also found to reduce opioid-induced ] and WAY-100635 was found to block this effect,<ref name="pmid10640309">{{cite journal | vauthors = Sahibzada N, Ferreira M, Wasserman AM, Taveira-DaSilva AM, Gillis RA | title = Reversal of morphine-induced apnea in the anesthetized rat by drugs that activate 5-hydroxytryptamine(1A) receptors | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 292 | issue = 2 | pages = 704–713 | date = February 2000 | pmid = 10640309 }}</ref> it is likely that 5-HT<sub>1A</sub> antagonists might worsen this side effect of opioids. Paradoxically, chronic administration of the very high efficacy 5-HT<sub>1A</sub> agonist ] results in potent analgesia following an initial period of ], an effect most likely linked to desensitisation and/or downregulation of 5-HT<sub>1A</sub> receptors (i.e. analogous to a 5-HT<sub>1A</sub> antagonist-like effect).<ref name="pmid15528450">{{cite journal | vauthors = Bardin L, Assié MB, Pélissou M, Royer-Urios I, Newman-Tancredi A, Ribet JP, Sautel F, Koek W, Colpaert FC | display-authors = 6 | title = <nowiki>Dual, hyperalgesic, and analgesic effects of the high-efficacy 5-hydroxytryptamine 1A (5-HT1A) agonist F 13640 -methyl}piperidin-1-yl]methanone, fumaric acid salt]: relationship with 5-HT1A receptor occupancy and kinetic parameters</nowiki> | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 312 | issue = 3 | pages = 1034–1042 | date = March 2005 | pmid = 15528450 | doi = 10.1124/jpet.104.077669 | s2cid = 42446435 }}</ref><ref name="pmid16921393">{{cite journal | vauthors = Assié MB, Lomenech H, Ravailhe V, Faucillon V, Newman-Tancredi A | title = Rapid desensitization of somatodendritic 5-HT1A receptors by chronic administration of the high-efficacy 5-HT1A agonist, F13714: a microdialysis study in the rat | journal = British Journal of Pharmacology | volume = 149 | issue = 2 | pages = 170–178 | date = September 2006 | pmid = 16921393 | pmc = 2013794 | doi = 10.1038/sj.bjp.0706859 }}</ref><ref name="pmid18809418">{{cite journal | vauthors = Buritova J, Berrichon G, Cathala C, Colpaert F, Cussac D | title = Region-specific changes in 5-HT1A agonist-induced Extracellular signal-Regulated Kinases 1/2 phosphorylation in rat brain: a quantitative ELISA study | journal = Neuropharmacology | volume = 56 | issue = 2 | pages = 350–361 | date = February 2009 | pmid = 18809418 | doi = 10.1016/j.neuropharm.2008.09.004 | s2cid = 45068116 }}</ref> As with other 5-HT<sub>1A</sub> silent antagonists such as ] and ], WAY-100635 can also induce a ] in rodents.<ref>Fox MA, Stein AR, French HT, Murphy DL. Functional interactions between 5-HT2A and presynaptic 5-HT1A receptor-based responses in mice genetically deficient in the serotonin 5-HT transporter (SERT). ''Br J Pharmacol''. 2010 Feb;159(4):879-87. {{cite journal | vauthors = Fox MA, Stein AR, French HT, Murphy DL | title = Functional interactions between 5-HT2A and presynaptic 5-HT1A receptor-based responses in mice genetically deficient in the serotonin 5-HT transporter (SERT) | journal = British Journal of Pharmacology | volume = 159 | issue = 4 | pages = 879–887 | date = February 2010 | pmid = 20128812 | pmc = 2829213 | doi = 10.1111/j.1476-5381.2009.00578.x }}</ref>
| pages = R1–R3
| doi = 10.1016/0014-2999(95)00438-Q|issue=s 1-3
| pmid=7498295
}}</ref>
WAY-100,635 may be labeled in different ways with carbon-11:
As WAY-100,635 or WAY-100,635, with WAY-100635 regarded as "far superior".<ref>{{Cite journal
| author = Victor W. Pike, Julie A. McCarron, Adriaan A. Lammertsma, Safiye Osman, Susan P. Hume, Peter A. Sargent, Christopher J. Bench, Ian A. Cliffe, Alan Fletcher and Paul M. Grasby
| title = Exquisite delineation of 5-HT<sub>1A</sub> receptors in human brain with PET and WAY-100635
| journal = ]
| volume = 301
| issue = 1-3
| month = April
| year = 1996
| pages = R5–R7
| doi = 10.1016/0014-2999(96)00079-9
}}</ref>
Labeled with ] WAY-100,635 may also be used in ].<ref>{{Cite journal
| author = Susan P. Hume, Sharon Ashworth, Jolanta Opacka-Juffry, Randal G. Ahier, Adriaan A. Lammertsma, Victor W. Pike, Ian A. Cliffe, Allan Fletcher and Alan C. White
| title = Evaluation of WAY-100635 as an in vivo radioligand for 5-HT<sub>1A</sub> receptors in rat brain
| journal = ]
| volume = 271
| issue = 2-3
| month = December
| year = 1994
| pages = 515&ndash;523
| doi = 10.1016/0014-2999(94)90813-3
}}</ref>
WAY-100,635 has higher 5-HT1A affinity than ].<ref>{{Cite journal
| author = P. W. J. Burnet, S. L. Eastwood & P. J. Harrison
| title = WAY-100635 for 5-HT<sub>1A</sub> receptor autoradiography in human brain: a comparison with 8-OH-DPAT and demonstration of increased binding in the frontal cortex in schizophrenia
| journal = ]
| year = 1997
| month = June
| volume = 30
| issue = 6
| pages = 565&ndash;574
| pmid = 9152998
| doi = 10.1016/S0197-0186(96)00124-6
}}</ref>


== See also == == See also ==
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** ] ** ]
** ] ** ]
** ]


== External links == == External links ==
* {{Cite web * {{Cite web
| url = http://www.turkupetcentre.net/analysis/doc/tracer/way100635.html | url = http://www.turkupetcentre.net/analysis/doc/tracer/way100635.html
| title = Quantification of (carbonyl-<sup>11</sup>C)WAY-100635 PET studies | title = Quantification of (carbonyl-<sup>11</sup>C)WAY-100635 PET studies
| author = Vesa Oikonen | author = Vesa Oikonen
| publisher = Turku PET center | publisher = Turku PET center
| year = 2007 | year = 2007
}} }}


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] ]
] ]
] ]
] ]
] ]
]