Open main menu
Home
Random
Recent changes
Special pages
Community portal
Preferences
About Wikipedia
Disclaimers
Incubator escapee wiki
Search
User menu
Talk
Dark mode
Contributions
Create account
Log in
Editing
Modafinil
(section)
Warning:
You are not logged in. Your IP address will be publicly visible if you make any edits. If you
log in
or
create an account
, your edits will be attributed to your username, along with other benefits.
Anti-spam check. Do
not
fill this in!
===Pharmacodynamics=== {| class="wikitable floatright" |+ Modafinil activity profile |- ! Site !! Potency !! Type !! Species !! Refs |- | {{Abbrlink|DAT|Dopamine transporter}} || {{Val|1.8|-|2.6|u=μM}}<br />{{Val|4.8|u=μM}}<br />{{Val|6.4|u=μM}}<br />{{Val|4.0|u=μM}}|| K<sub>i</sub><br />K<sub>i</sub><br />IC<sub>50</sub><sup>a</sup><br />IC<sub>50</sub><sup>a</sup> || Human<br />Rat<br />Human<br />Rat || <ref name="pmid19197004">{{cite journal | vauthors = Zolkowska D, Jain R, Rothman RB, Partilla JS, Roth BL, Setola V, Prisinzano TE, Baumann MH | title = Evidence for the involvement of dopamine transporters in behavioral stimulant effects of modafinil | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 329 | issue = 2 | pages = 738–746 | date = May 2009 | pmid = 19197004 | pmc = 2672878 | doi = 10.1124/jpet.108.146142 | author5-link = Bryan Roth }}</ref><ref name="pmid34423920">{{cite journal | vauthors = Krief S, Berrebi-Bertrand I, Nagmar I, Giret M, Belliard S, Perrin D, Uguen M, Robert P, Lecomte JM, Schwartz JC, Finance O, Ligneau X | title = Pitolisant, a wake-promoting agent devoid of psychostimulant properties: Preclinical comparison with amphetamine, modafinil, and solriamfetol | journal = Pharmacology Research & Perspectives | volume = 9 | issue = 5 | pages = e00855 | date = October 2021 | pmid = 34423920 | pmc = 8381683 | doi = 10.1002/prp2.855 }}</ref><br /><ref name="pmid19197004" /><br /><ref name="pmid29115823">{{cite journal | vauthors = Murillo-Rodríguez E, Barciela Veras A, Barbosa Rocha N, Budde H, Machado S | title = An Overview of the Clinical Uses, Pharmacology, and Safety of Modafinil | journal = ACS Chemical Neuroscience | volume = 9 | issue = 2 | pages = 151–158 | date = February 2018 | pmid = 29115823 | doi = 10.1021/acschemneuro.7b00374 }}</ref><ref name="pmid22537794">{{cite journal | vauthors = Loland CJ, Mereu M, Okunola OM, Cao J, Prisinzano TE, Mazier S, Kopajtic T, Shi L, Katz JL, Tanda G, Newman AH | title = R-modafinil (armodafinil): a unique dopamine uptake inhibitor and potential medication for psychostimulant abuse | journal = Biological Psychiatry | volume = 72 | issue = 5 | pages = 405–413 | date = September 2012 | pmid = 22537794 | pmc = 3413742 | doi = 10.1016/j.biopsych.2012.03.022 }}</ref><br /><ref name="pmid19197004" /> |- | {{Abbrlink|NET|Norepinephrine transporter}} || >{{Val|10|u=μM}}<br />>{{Val|92|u=μM}}<br />{{Val|35.6|u=μM}}<br />{{Val|136|u=μM}} || K<sub>i</sub><br />K<sub>i</sub><br />IC<sub>50</sub><sup>a</sup><br />IC<sub>50</sub><sup>a</sup> || Human<br />Rat<br />Human<br />Rat || <ref name="pmid19197004" /><ref name="pmid34423920" /><br /><ref name="pmid19197004" /><br /><ref name="pmid29115823" /><ref name="pmid22537794" /><br /><ref name="pmid19197004" /> |- | {{Abbrlink|SERT|Serotonin transporter}} || >{{Val|10|u=μM}}<br />{{Val|46.6|u=μM}}<br />>{{Val|500|u=μM}}<br />>{{Val|50|u=μM}} || K<sub>i</sub><br />K<sub>i</sub><br />IC<sub>50</sub><sup>a</sup><br />IC<sub>50</sub><sup>a</sup> || Human<br />Rat<br />Human<br />Rat || <ref name="pmid19197004" /><ref name="pmid34423920" /><br /><ref name="pmid19197004" /><br /><ref name="pmid29115823" /><ref name="pmid22537794" /><br /><ref name="pmid19197004" /> |- | [[Dopamine D2 receptor|D<sub>2</sub>]] || >{{Val|10|u=μM}}<br />{{Val|16|u=μM}}<sup>b</sup><br />{{Val|120|u=μM}}<sup>b</sup> || K<sub>i</sub><br />K<sub>i</sub><br />EC<sub>50</sub><sup>a</sup> || Human<br />Rat<br />Rat|| <ref name="pmid19197004" /><br /><ref name="pmid19391150">{{cite journal | vauthors = Seeman P, Guan HC, Hirbec H | title = Dopamine D2High receptors stimulated by phencyclidines, lysergic acid diethylamide, salvinorin A, and modafinil | journal = Synapse | volume = 63 | issue = 8 | pages = 698–704 | date = August 2009 | pmid = 19391150 | doi = 10.1002/syn.20647 | s2cid = 17758902 }}</ref><br /><ref name="pmid19391150" /> |- class="sortbottom" | colspan="5" style="width:1px; background:#eaecf0; text-align:center;"| '''Footnotes:''' <sup>a</sup> = Functional activity, not binding inhibition. <sup>b</sup> = [[Armodafinil]] at D<sub>2</sub><sup>High</sup>. '''Notes:''' No activity at a variety of other assessed targets.<ref name="pmid19197004" /> |} The precise [[mechanism of action]] of modafinil for narcolepsy and other sleep disorders remains unclear.<ref name="Drugs.com-Monograph-2023"/><ref name="pmid32032921">{{cite journal | vauthors = Thorpy MJ, Bogan RK | title = Update on the pharmacologic management of narcolepsy: mechanisms of action and clinical implications | journal = Sleep Medicine | volume = 68 | pages = 97–109 | date = April 2020 | pmid = 32032921 | doi = 10.1016/j.sleep.2019.09.001 | s2cid = 203405397 }}</ref><ref name="Stahl-2017">{{cite book | vauthors=Stahl SM | title=Prescriber's Guide: Stahl's Essential Psychopharmacology | date=March 2017 | publisher=Cambridge University Press | location=Cambridge, United Kingdom | isbn=978-1-108-22874-9 | pages=491–495 | edition=6th | chapter=Modafinil }}</ref><ref name="pmid19300566">{{cite journal | vauthors = Gerrard P, Malcolm R | title = Mechanisms of modafinil: A review of current research | journal = Neuropsychiatric Disease and Treatment | volume = 3 | issue = 3 | pages = 349–364 | date = June 2007 | pmid = 19300566 | pmc = 2654794 }}</ref> Although modafinil may have interactions with neurotransmitter systems, its exact mode of action is not fully understood.<ref name="pmid32032921"/><ref name="pmid28646346">{{cite book | vauthors = Lazarus M, Chen JF, Huang ZL, Urade Y, Fredholm BB | chapter = Adenosine and Sleep | title = Handbook of Experimental Pharmacology | volume = 253 | pages = 359–381 | date = 2019 | pmid = 28646346 | doi = 10.1007/164_2017_36 | isbn = 978-3-030-11270-7 }}</ref> From laboratory research, modafinil has little to no affinity for [[Serotonin transporter|serotonin]] or [[norepinephrine transporter]]s and does not directly interact with these systems.<ref name="pmid30285371"/><ref name="pmid19300566"/> However, studies have shown that elevated concentrations of norepinephrine and serotonin can occur as an indirect effect following modafinil administration due to increased extracellular dopamine activity.<ref name="pmid19300566"/><ref name="pmid30285371"/> Unlike traditional psychostimulant drugs,<ref name="pmid38725665"/> such as [[cocaine]] or [[amphetamine]], modafinil shows low potential for causing euphoria due to differences in how it interacts with dopamine transporters at a cellular level.<ref name="pmid32032921"/><ref name="pmid19300566"/><ref name="pmid28646346"/> In addition to its influence on [[dopaminergic pathways]], modafinil may impact other neurotransmitter systems, such as [[orexin]] ([[hypocretin]]).<ref name="pmid19300566"/> Orexin neurons are involved in promoting wakefulness and regulating arousal states. Modafinil may increase signaling within hypothalamic orexin pathways, potentially contributing to its wake-promoting effects.<ref name="pmid30285371"/><ref name="pmid19300566"/>
Edit summary
(Briefly describe your changes)
By publishing changes, you agree to the
Terms of Use
, and you irrevocably agree to release your contribution under the
CC BY-SA 4.0 License
and the
GFDL
. You agree that a hyperlink or URL is sufficient attribution under the Creative Commons license.
Cancel
Editing help
(opens in new window)