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|+ Binding profiles of {{abbr|MRIs|monoamine reuptake inhibitors}} at human {{abbr|MATs|monoamine transporters}}<ref name="pmid9537821">{{cite journal | vauthors = Tatsumi M, Groshan K, Blakely RD, Richelson E | title = Pharmacological profile of antidepressants and related compounds at human monoamine transporters | journal = Eur. J. Pharmacol. | volume = 340 | issue = 2-3 | pages = 249–58 | year = 1997 | pmid = 9537821 | doi = | url = http://www.academia.edu/download/45762636/s0014-2999_2897_2901393-920160518-31441-t07hp6.pdf}}</ref> |
|+ Binding profiles of {{abbr|MRIs|monoamine reuptake inhibitors}} at human {{abbr|MATs|monoamine transporters}}<ref name="pmid9537821">{{cite journal | vauthors = Tatsumi M, Groshan K, Blakely RD, Richelson E | title = Pharmacological profile of antidepressants and related compounds at human monoamine transporters | journal = Eur. J. Pharmacol. | volume = 340 | issue = 2-3 | pages = 249–58 | year = 1997 | pmid = 9537821 | doi = | url = http://www.academia.edu/download/45762636/s0014-2999_2897_2901393-920160518-31441-t07hp6.pdf}}</ref> |
||
|- |
|- |
||
! Compound !! {{abbrlink|SERT|Serotonin transporter}} !! {{abbrlink|NET|Norepinephrine transporter}} !! {{abbrlink|DAT|Dopamine transporter}} !! Type |
! Compound !! {{abbrlink|SERT|Serotonin transporter}} !! {{abbrlink|NET|Norepinephrine transporter}} !! {{abbrlink|DAT|Dopamine transporter}} !! Type !! Class |
||
|- |
|- |
||
| [[Amfonelic acid]] || {{abbr|ND|No data}} || {{abbr|ND|No data}} || 207 || DRI |
| [[Amfonelic acid]] || {{abbr|ND|No data}} || {{abbr|ND|No data}} || 207 || DRI || Stimulant |
||
|- |
|- |
||
| [[Amineptine]]*<ref name="pmid3708219">{{cite journal | vauthors = Ceci A, Garattini S, Gobbi M, Mennini T | title = Effect of long term amineptine treatment on pre- and postsynaptic mechanisms in rat brain | journal = Br. J. Pharmacol. | volume = 88 | issue = 1 | pages = 269–75 | year = 1986 | pmid = 3708219 | pmc = 1917102 | doi = | url = }}</ref> || {{abbr|IA|Inactive}} (rat) || >10,000 (rat) || 1,400 (rat) || DRI |
| [[Amineptine]]*<ref name="pmid3708219">{{cite journal | vauthors = Ceci A, Garattini S, Gobbi M, Mennini T | title = Effect of long term amineptine treatment on pre- and postsynaptic mechanisms in rat brain | journal = Br. J. Pharmacol. | volume = 88 | issue = 1 | pages = 269–75 | year = 1986 | pmid = 3708219 | pmc = 1917102 | doi = | url = }}</ref> || {{abbr|IA|Inactive}} (rat) || >10,000 (rat) || 1,400 (rat) || DRI || Stimulant |
||
|- |
|- |
||
| [[Amitriptyline]] || 4.30 || 35 || 3,250 || SNRI |
| [[Amitriptyline]] || 4.30 || 35 || 3,250 || SNRI || TCA |
||
|- |
|- |
||
| [[Amoxapine]] || 58 || 16.0 || 4,310 || SNRI |
| [[Amoxapine]] || 58 || 16.0 || 4,310 || SNRI || {{abbr|TeCA|Tetracyclic antidepressant}} |
||
|- |
|- |
||
| [[Atomoxetine]] || 8.9 || 2.03 || 1,080 || SNRI |
| [[Atomoxetine]] || 8.9 || 2.03 || 1,080 || SNRI || Stimulant |
||
|- |
|- |
||
| [[Bupropion]] || 9,100 || 52,000 || 520 || NDRI |
| [[Bupropion]] || 9,100 || 52,000 || 520 || NDRI || Stimulant |
||
|- |
|- |
||
| [[Butriptyline]] || 1,360 || 5,100 || 3,940 || N/A ({{abbr|IA|inactive}}) |
| [[Butriptyline]] || 1,360 || 5,100 || 3,940 || N/A ({{abbr|IA|inactive}}) || TCA |
||
|- |
|- |
||
| [[Chlorphenamine]] || 15.2 || 1,440 || 1,060 || SRI |
| [[Chlorphenamine]] || 15.2 || 1,440 || 1,060 || SRI || Antihistamine |
||
|- |
|- |
||
| [[Citalopram]] || 1.16 || 4,070 || 28,100 || SRI |
| [[Citalopram]] || 1.16 || 4,070 || 28,100 || SRI || {{abbr|SSRI|Selective serotonin reuptake inhibitor}} |
||
|- |
|- |
||
| [[Clomipramine]] || 0.28 || 38 || 2,190 || SNRI |
| [[Clomipramine]] || 0.28 || 38 || 2,190 || SNRI || TCA |
||
|- |
|- |
||
| [[Cocaethylene]]<ref name="pmid14612135">{{cite journal | vauthors = Rothman RB, Baumann MH | title = Monoamine transporters and psychostimulant drugs | journal = Eur. J. Pharmacol. | volume = 479 | issue = 1-3 | pages = 23–40 | year = 2003 | pmid = 14612135 | doi = | url = }}</ref> || 3,878 || >10,000 || 555 || SDRI |
| [[Cocaethylene]]<ref name="pmid14612135">{{cite journal | vauthors = Rothman RB, Baumann MH | title = Monoamine transporters and psychostimulant drugs | journal = Eur. J. Pharmacol. | volume = 479 | issue = 1-3 | pages = 23–40 | year = 2003 | pmid = 14612135 | doi = | url = }}</ref> || 3,878 || >10,000 || 555 || SDRI || Stimulant |
||
|- |
|- |
||
| [[Cocaine]]<ref name="pmid14612135" /> || 304 || 779 || 478 || SNDRI |
| [[Cocaine]]<ref name="pmid14612135" /> || 304 || 779 || 478 || SNDRI || Stimulant |
||
|- |
|- |
||
| [[Desipramine]] || 17.6 || 0.83 || 3,190 || SNRI |
| [[Desipramine]] || 17.6 || 0.83 || 3,190 || SNRI || TCA |
||
|- |
|- |
||
| [[Desmethylcitalopram]] || 3.6 || 1,820 || 18,300 || SRI |
| [[Desmethylcitalopram]] || 3.6 || 1,820 || 18,300 || SRI || SSRI |
||
|- |
|- |
||
| [[Desmethylsertraline]] || 3.0 || 390 || 129 || SRI |
| [[Desmethylsertraline]] || 3.0 || 390 || 129 || SRI || SSRI |
||
|- |
|- |
||
| [[Desmethylsibutramine]]<ref name="pmid12119986">{{cite journal | vauthors = Nisoli E, Carruba MO | title = An assessment of the safety and efficacy of sibutramine, an anti-obesity drug with a novel mechanism of action | journal = Obes Rev | volume = 1 | issue = 2 | pages = 127–39 | year = 2000 | pmid = 12119986 | doi = | url = }}</ref> || 15 || 20 || 49 || SNDRI |
| [[Desmethylsibutramine]]<ref name="pmid12119986">{{cite journal | vauthors = Nisoli E, Carruba MO | title = An assessment of the safety and efficacy of sibutramine, an anti-obesity drug with a novel mechanism of action | journal = Obes Rev | volume = 1 | issue = 2 | pages = 127–39 | year = 2000 | pmid = 12119986 | doi = | url = }}</ref> || 15 || 20 || 49 || SNDRI || SNRI |
||
|- |
|- |
||
| [[Desoxypipradrol]]<ref name="pmid23261499">{{cite journal | vauthors = Iversen L, Gibbons S, Treble R, Setola V, Huang XP, Roth BL | title = Neurochemical profiles of some novel psychoactive substances | journal = Eur. J. Pharmacol. | volume = 700 | issue = 1-3 | pages = 147–51 | year = 2013 | pmid = 23261499 | pmc = 3582025 | doi = 10.1016/j.ejphar.2012.12.006 | url = }}</ref> || 53,700 || 550 || 50 || NDRI |
| [[Desoxypipradrol]]<ref name="pmid23261499">{{cite journal | vauthors = Iversen L, Gibbons S, Treble R, Setola V, Huang XP, Roth BL | title = Neurochemical profiles of some novel psychoactive substances | journal = Eur. J. Pharmacol. | volume = 700 | issue = 1-3 | pages = 147–51 | year = 2013 | pmid = 23261499 | pmc = 3582025 | doi = 10.1016/j.ejphar.2012.12.006 | url = }}</ref> || 53,700 || 550 || 50 || NDRI || Stimulant |
||
|- |
|- |
||
| [[Desvenlafaxine]]*<ref name="pmid16675639">{{cite journal | vauthors = Deecher DC, Beyer CE, Johnston G, Bray J, Shah S, Abou-Gharbia M, Andree TH | title = Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor | journal = J. Pharmacol. Exp. Ther. | volume = 318 | issue = 2 | pages = 657–65 | year = 2006 | pmid = 16675639 | doi = 10.1124/jpet.106.103382 | url = }}</ref> || 47 || 531 || {{abbr|ND|No data}} || SNRI |
| [[Desvenlafaxine]]*<ref name="pmid16675639">{{cite journal | vauthors = Deecher DC, Beyer CE, Johnston G, Bray J, Shah S, Abou-Gharbia M, Andree TH | title = Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor | journal = J. Pharmacol. Exp. Ther. | volume = 318 | issue = 2 | pages = 657–65 | year = 2006 | pmid = 16675639 | doi = 10.1124/jpet.106.103382 | url = }}</ref> || 47 || 531 || {{abbr|ND|No data}} || SNRI || SNRI |
||
|- |
|- |
||
| [[Dextroamphetamine]] || >100,000 || 530 || 2,900 || {{abbr|NDRA|Norepinephrine–dopamine releasing agent}} |
| [[Dextroamphetamine]] || >100,000 || 530 || 2,900 || {{abbr|NDRA|Norepinephrine–dopamine releasing agent}} || Stimulant |
||
|- |
|- |
||
| [[Dextromethamphetamine]] || >100,000 || 660 || 2,800 || |
| [[Dextromethamphetamine]] || >100,000 || 660 || 2,800 || NDRA || Stimulant |
||
|- |
|- |
||
| [[Didesmethylsibutramine]]<ref name="pmid12119986" /> || 20 || 15 || 45 || SNDRI |
| [[Didesmethylsibutramine]]<ref name="pmid12119986" /> || 20 || 15 || 45 || SNDRI || SNRI |
||
|- |
|- |
||
| [[Diphenhydramine]] || 3,800 || 960 || 2,200 || N/A ({{abbr|IA|inactive}}) |
| [[Diphenhydramine]] || 3,800 || 960 || 2,200 || N/A ({{abbr|IA|inactive}}) || Antihistamine |
||
|- |
|- |
||
| [[Dosulepin|Dosulepin (dothiepin)]] || 8.6 || 46 || 5,310 || SNRI |
| [[Dosulepin|Dosulepin (dothiepin)]] || 8.6 || 46 || 5,310 || SNRI || TCA |
||
|- |
|- |
||
| [[Doxepin]] || 68 || 29.5 || 12,100 || SNRI |
| [[Doxepin]] || 68 || 29.5 || 12,100 || SNRI || TCA |
||
|- |
|- |
||
| [[Duloxetine]]*<ref name="pmid14744476">{{cite journal | vauthors = Vaishnavi SN, Nemeroff CB, Plott SJ, Rao SG, Kranzler J, Owens MJ | title = Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity | journal = Biol. Psychiatry | volume = 55 | issue = 3 | pages = 320–2 | year = 2004 | pmid = 14744476 | doi = | url = }}</ref> || 3.7 || 20 || 439 || SNRI |
| [[Duloxetine]]*<ref name="pmid14744476">{{cite journal | vauthors = Vaishnavi SN, Nemeroff CB, Plott SJ, Rao SG, Kranzler J, Owens MJ | title = Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity | journal = Biol. Psychiatry | volume = 55 | issue = 3 | pages = 320–2 | year = 2004 | pmid = 14744476 | doi = | url = }}</ref> || 3.7 || 20 || 439 || SNRI || SNRI |
||
|- |
|- |
||
| [[Escitalopram]]<ref name="pmid12232544">{{cite journal | vauthors = Owens JM, Knight DL, Nemeroff CB | title = [Second generation SSRIS: human monoamine transporter binding profile of escitalopram and R-fluoxetine] | language = French | journal = Encephale | volume = 28 | issue = 4 | pages = 350–5 | year = 2002 | pmid = 12232544 | doi = | url = }}</ref> || 1.1 || 7,841 || 27,410 || SRI |
| [[Escitalopram]]<ref name="pmid12232544">{{cite journal | vauthors = Owens JM, Knight DL, Nemeroff CB | title = [Second generation SSRIS: human monoamine transporter binding profile of escitalopram and R-fluoxetine] | language = French | journal = Encephale | volume = 28 | issue = 4 | pages = 350–5 | year = 2002 | pmid = 12232544 | doi = | url = }}</ref> || 1.1 || 7,841 || 27,410 || SRI || SSRI |
||
|- |
|- |
||
| [[Etoperidone]] || 890 || 20,000 || 52,000 || SRI |
| [[Etoperidone]] || 890 || 20,000 || 52,000 || SRI || {{abbr|SARI|Serotonin antagonist and reuptake inhibitor}} |
||
|- |
|- |
||
| [[Femoxetine]] || 11.0 || 760 || 2,050 || SRI |
| [[Femoxetine]] || 11.0 || 760 || 2,050 || SRI || SSRI |
||
|- |
|- |
||
| [[Fluoxetine]] || 0.81 || 240 || 3,600 || SRI |
| [[Fluoxetine]] || 0.81 || 240 || 3,600 || SRI || SSRI |
||
|- |
|- |
||
| [[Fluvoxamine]] || 2.2 || 1,300 || 9,200 || SRI |
| [[Fluvoxamine]] || 2.2 || 1,300 || 9,200 || SRI || SSRI |
||
|- |
|- |
||
| [[GBR-12935]]<ref name="pmid14612135" /> || 289 || 277 || 4.90 || DRI |
| [[GBR-12935]]<ref name="pmid14612135" /> || 289 || 277 || 4.90 || DRI || Stimulant |
||
|- |
|- |
||
| [[Imipramine]] || 1.40 || 37 || 8,500 || SNRI |
| [[Imipramine]] || 1.40 || 37 || 8,500 || SNRI || TCA |
||
|- |
|- |
||
| [[Indatraline]]<ref name="pmid14612135" /> || 3.10 || 12.6 || 1.90 || SNDRI |
| [[Indatraline]]<ref name="pmid14612135" /> || 3.10 || 12.6 || 1.90 || SNDRI || Stimulant |
||
|- |
|- |
||
| [[Iprindole]] || 1,620 || 1,262 || 6,530 || N/A ({{abbr|IA|inactive}}) |
| [[Iprindole]] || 1,620 || 1,262 || 6,530 || N/A ({{abbr|IA|inactive}}) || TCA |
||
|- |
|- |
||
| [[Levomilnacipran]]*<ref name="pmid23499664">{{cite journal | vauthors = Auclair AL, Martel JC, Assié MB, Bardin L, Heusler P, Cussac D, Marien M, Newman-Tancredi A, O'Connor JA, Depoortère R | title = Levomilnacipran (F2695), a norepinephrine-preferring SNRI: profile in vitro and in models of depression and anxiety | journal = Neuropharmacology | volume = 70 | issue = | pages = 338–47 | year = 2013 | pmid = 23499664 | doi = 10.1016/j.neuropharm.2013.02.024 | url = }}</ref> || 19.0 || 10.5 || >100,000 || SNRI |
| [[Levomilnacipran]]*<ref name="pmid23499664">{{cite journal | vauthors = Auclair AL, Martel JC, Assié MB, Bardin L, Heusler P, Cussac D, Marien M, Newman-Tancredi A, O'Connor JA, Depoortère R | title = Levomilnacipran (F2695), a norepinephrine-preferring SNRI: profile in vitro and in models of depression and anxiety | journal = Neuropharmacology | volume = 70 | issue = | pages = 338–47 | year = 2013 | pmid = 23499664 | doi = 10.1016/j.neuropharm.2013.02.024 | url = }}</ref> || 19.0 || 10.5 || >100,000 || SNRI || SNRI |
||
|- |
|- |
||
| [[Lofepramine]] || 70 || 5.4 || 18,000 || SNRI |
| [[Lofepramine]] || 70 || 5.4 || 18,000 || SNRI || TCA |
||
|- |
|- |
||
| [[Maprotiline]] || 5,800 || 11.1 || 1,000 || NRI |
| [[Maprotiline]] || 5,800 || 11.1 || 1,000 || NRI || TeCA |
||
|- |
|- |
||
| [[Mazindol]] || 39 || 0.45 || 8.1 || NDRI |
| [[Mazindol]] || 39 || 0.45 || 8.1 || NDRI || Stimulant |
||
|- |
|- |
||
| [[Methylphenidate]] || 44,000 || 234 || 24 || NDRI |
| [[Methylphenidate]] || 44,000 || 234 || 24 || NDRI || Stimulant |
||
|- |
|- |
||
| [[Mianserin]] || 4,000 || 71 || 9,400 || NRI |
| [[Mianserin]] || 4,000 || 71 || 9,400 || NRI || TeCA |
||
|- |
|- |
||
| [[Milnacipran]]*<ref name="pmid14744476" /> || 151 || 68 || >100,000 || SNRI |
| [[Milnacipran]]*<ref name="pmid14744476" /> || 151 || 68 || >100,000 || SNRI || SNRI |
||
|- |
|- |
||
| [[Mirtazapine]] || >100,000 || 4,600 || >100,000 || N/A ({{abbr|IA|inactive}}) |
| [[Mirtazapine]] || >100,000 || 4,600 || >100,000 || N/A ({{abbr|IA|inactive}}) || TeCA |
||
|- |
|- |
||
| [[Modafinil]]*<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 = J. Pharmacol. Exp. Ther. | volume = 329 | issue = 2 | pages = 738–46 | year = 2009 | pmid = 19197004 | pmc = 2672878 | doi = 10.1124/jpet.108.146142 | url = }}</ref> || >50,000 || 136,000 || 4,043 || DRI |
| [[Modafinil]]*<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 = J. Pharmacol. Exp. Ther. | volume = 329 | issue = 2 | pages = 738–46 | year = 2009 | pmid = 19197004 | pmc = 2672878 | doi = 10.1124/jpet.108.146142 | url = }}</ref> || >50,000 || 136,000 || 4,043 || DRI || Stimulant |
||
|- |
|- |
||
| [[Nefazodone]] || 200 || 360 || 360 || SNDRI |
| [[Nefazodone]] || 200 || 360 || 360 || SNDRI || SARI |
||
|- |
|- |
||
| [[Nefopam]]<ref name="pmid22711801">{{cite journal | vauthors = Gregori-Puigjané E, Setola V, Hert J, Crews BA, Irwin JJ, Lounkine E, Marnett L, Roth BL, Shoichet BK | title = Identifying mechanism-of-action targets for drugs and probes | journal = Proc. Natl. Acad. Sci. U.S.A. | volume = 109 | issue = 28 | pages = 11178–83 | year = 2012 | pmid = 22711801 | pmc = 3396511 | doi = 10.1073/pnas.1204524109 | url = }}</ref> || 29 || 33 || 531 || SNDRI |
| [[Nefopam]]<ref name="pmid22711801">{{cite journal | vauthors = Gregori-Puigjané E, Setola V, Hert J, Crews BA, Irwin JJ, Lounkine E, Marnett L, Roth BL, Shoichet BK | title = Identifying mechanism-of-action targets for drugs and probes | journal = Proc. Natl. Acad. Sci. U.S.A. | volume = 109 | issue = 28 | pages = 11178–83 | year = 2012 | pmid = 22711801 | pmc = 3396511 | doi = 10.1073/pnas.1204524109 | url = }}</ref> || 29 || 33 || 531 || SNDRI || Analgesic |
||
|- |
|- |
||
| [[Nisoxetine]]<ref name="pmid14612135" /> || 427 || 2.3 || 1,235 || NRI |
| [[Nisoxetine]]<ref name="pmid14612135" /> || 427 || 2.3 || 1,235 || NRI || Stimulant |
||
|- |
|- |
||
| [[Nomifensine]] || 1,010 || 15.6 || 56 || NDRI |
| [[Nomifensine]] || 1,010 || 15.6 || 56 || NDRI || Stimulant |
||
|- |
|- |
||
| [[Norfluoxetine]] || 1.47 || 1,426 || 420 || SRI |
| [[Norfluoxetine]] || 1.47 || 1,426 || 420 || SRI || SSRI |
||
|- |
|- |
||
| [[Nortriptyline]] || 18 || 4.37 || 1,140 || SNRI |
| [[Nortriptyline]] || 18 || 4.37 || 1,140 || SNRI || TCA |
||
|- |
|- |
||
| [[Oxaprotiline]] || 3,900 || 4.9 || 4,340 || NRI |
| [[Oxaprotiline]] || 3,900 || 4.9 || 4,340 || NRI || TeCA |
||
|- |
|- |
||
| [[Paroxetine]] || 0.13 || 40 || 490 || SRI |
| [[Paroxetine]] || 0.13 || 40 || 490 || SRI || SSRI |
||
|- |
|- |
||
| [[Protriptyline]] || 19.6 || 1.41 || 2,100 || SNRI |
| [[Protriptyline]] || 19.6 || 1.41 || 2,100 || SNRI || TCA |
||
|- |
|- |
||
| [[Reboxetine]]<ref name="pmid12665410">{{cite journal | vauthors = Bymaster FP, McNamara RK, Tran PV | title = New approaches to developing antidepressants by enhancing monoaminergic neurotransmission | journal = Expert Opin Investig Drugs | volume = 12 | issue = 4 | pages = 531–43 | year = 2003 | pmid = 12665410 | doi = 10.1517/13543784.12.4.531 | url = }}</ref> || 129 || 1.1 || >10,000 || NRI |
| [[Reboxetine]]<ref name="pmid12665410">{{cite journal | vauthors = Bymaster FP, McNamara RK, Tran PV | title = New approaches to developing antidepressants by enhancing monoaminergic neurotransmission | journal = Expert Opin Investig Drugs | volume = 12 | issue = 4 | pages = 531–43 | year = 2003 | pmid = 12665410 | doi = 10.1517/13543784.12.4.531 | url = }}</ref> || 129 || 1.1 || >10,000 || NRI || Stimulant |
||
|- |
|- |
||
| [[Sertraline]] || 0.29 || 420 || 25 || SRI |
| [[Sertraline]] || 0.29 || 420 || 25 || SRI || SSRI |
||
|- |
|- |
||
| [[Sibutramine]]<ref name="pmid12119986" /> || 298 || 5,451 || 943 || SNDRI |
| [[Sibutramine]]<ref name="pmid12119986" /> || 298 || 5,451 || 943 || SNDRI || SNRI |
||
|- |
|- |
||
| [[Trazodone]] || 160 || 8,500 || 7,400 || SRI |
| [[Trazodone]] || 160 || 8,500 || 7,400 || SRI || SARI |
||
|- |
|- |
||
| [[Trimipramine]] || 149 || 2,450 || 3,780 || SRI |
| [[Trimipramine]] || 149 || 2,450 || 3,780 || SRI || TCA |
||
|- |
|- |
||
| [[Vanoxerine]]<ref name="pmid14612135" /> || 73.2 || 79.2 || 4.3 || DRI |
| [[Vanoxerine]]<ref name="pmid14612135" /> || 73.2 || 79.2 || 4.3 || DRI || Stimulant |
||
|- |
|- |
||
| [[Venlafaxine]]*<ref name="pmid14744476" /> || 145 || 1,420 || 3,070 || SNRI |
| [[Venlafaxine]]*<ref name="pmid14744476" /> || 145 || 1,420 || 3,070 || SNRI || SNRI |
||
|- |
|- |
||
| [[Vilazodone]]*<ref name="pmid12183683">{{cite journal | vauthors = Page ME, Cryan JF, Sullivan A, Dalvi A, Saucy B, Manning DR, Lucki I | title = Behavioral and neurochemical effects of 5-(4-[4-(5-Cyano-3-indolyl)-butyl)-butyl]-1-piperazinyl)-benzofuran-2-carboxamide (EMD 68843): a combined selective inhibitor of serotonin reuptake and 5-hydroxytryptamine(1A) receptor partial agonist | journal = J. Pharmacol. Exp. Ther. | volume = 302 | issue = 3 | pages = 1220–7 | year = 2002 | pmid = 12183683 | doi = 10.1124/jpet.102.034280 | url = }}</ref> || 0.2 || ~60 || {{abbr|ND|No data}} || SRI |
| [[Vilazodone]]*<ref name="pmid12183683">{{cite journal | vauthors = Page ME, Cryan JF, Sullivan A, Dalvi A, Saucy B, Manning DR, Lucki I | title = Behavioral and neurochemical effects of 5-(4-[4-(5-Cyano-3-indolyl)-butyl)-butyl]-1-piperazinyl)-benzofuran-2-carboxamide (EMD 68843): a combined selective inhibitor of serotonin reuptake and 5-hydroxytryptamine(1A) receptor partial agonist | journal = J. Pharmacol. Exp. Ther. | volume = 302 | issue = 3 | pages = 1220–7 | year = 2002 | pmid = 12183683 | doi = 10.1124/jpet.102.034280 | url = }}</ref> || 0.2 || ~60 || {{abbr|ND|No data}} || SRI || {{abbr|SMS|Serotonin modulator and stimulator}} |
||
|- |
|- |
||
| [[Viloxazine]] || 17,300 || 155 || >100,000 || NRI |
| [[Viloxazine]] || 17,300 || 155 || >100,000 || NRI || Stimulant |
||
|- |
|- |
||
| [[Vortioxetine]]*<ref name="pmid21486038">{{cite journal | vauthors = Bang-Andersen B, Ruhland T, Jørgensen M, Smith G, Frederiksen K, Jensen KG, Zhong H, Nielsen SM, Hogg S, Mørk A, Stensbøl TB | title = Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder | journal = J. Med. Chem. | volume = 54 | issue = 9 | pages = 3206–21 | year = 2011 | pmid = 21486038 | doi = 10.1021/jm101459g | url = }}</ref> || 5.4 || 890 (rat) || 140 (rat) || SRI |
| [[Vortioxetine]]*<ref name="pmid21486038">{{cite journal | vauthors = Bang-Andersen B, Ruhland T, Jørgensen M, Smith G, Frederiksen K, Jensen KG, Zhong H, Nielsen SM, Hogg S, Mørk A, Stensbøl TB | title = Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder | journal = J. Med. Chem. | volume = 54 | issue = 9 | pages = 3206–21 | year = 2011 | pmid = 21486038 | doi = 10.1021/jm101459g | url = }}</ref> || 5.4 || 890 (rat) || 140 (rat) || SRI || SMS |
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| [[Zimelidine]] || 152 || 9,400 || 11,700 || SRI |
| [[Zimelidine]] || 152 || 9,400 || 11,700 || SRI || SSRI |
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| colspan="7" | Values are K<sub>i</sub> (nM) or, in some cases (*), {{abbrlink|IC<sub>50</sub>|half-maximal inhibitory concentration}} (nM). The smaller the |
| colspan="7" | Values are K<sub>i</sub> (nM) or, in some cases (*), {{abbrlink|IC<sub>50</sub>|half-maximal inhibitory concentration}} (nM). The smaller the value, the more<br />strongly the drug binds to or inhibits the transporter. |
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Amonoamine reuptake inhibitor (MRI)[1] is a drug that acts as a reuptake inhibitor of one or more of the three major monoamine neurotransmitters serotonin, norepinephrine, and dopamine by blocking the action of one or more of the respective monoamine transporters (MATs), which include the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). This in turn results in an increase in the synaptic concentrations of one or more of these neurotransmitters and therefore an increase in monoaminergic neurotransmission.
The majority of currently approved antidepressants act predominantly or exclusively as MRIs, including the selective serotonin reuptake inhibitors (SSRIs), serotonin–norepinephrine reuptake inhibitors (SNRIs), and almost all of the tricyclic antidepressants (TCAs).[2] Many psychostimulants used either as in the treatment of ADHDTooltip attention-deficit hyperactivity disorder or as appetite suppressants in the treatment of obesity also behave as MRIs.[3] Additionally, psychostimulants acting as MRIs that affect dopamine such as cocaine and methylphenidate are often abusedasrecreational drugs.[4] As a result, many of them have become controlled substances, which in turn has resulted in the clandestine synthesis of a vast array of designer drugs for the purpose of bypassing drug laws; a prime example of such is the mixed monoamine reuptake inhibitor and releasing agent mephedrone.[5]
There are a variety of different kinds of MRIs, of which include the following:
Compound | SERTTooltip Serotonin transporter | NETTooltip Norepinephrine transporter | DATTooltip Dopamine transporter | Type | Class | |
---|---|---|---|---|---|---|
Amfonelic acid | ND | ND | 207 | DRI | Stimulant | |
Amineptine*[7] | IA (rat) | >10,000 (rat) | 1,400 (rat) | DRI | Stimulant | |
Amitriptyline | 4.30 | 35 | 3,250 | SNRI | TCA | |
Amoxapine | 58 | 16.0 | 4,310 | SNRI | TeCA | |
Atomoxetine | 8.9 | 2.03 | 1,080 | SNRI | Stimulant | |
Bupropion | 9,100 | 52,000 | 520 | NDRI | Stimulant | |
Butriptyline | 1,360 | 5,100 | 3,940 | N/A (IA) | TCA | |
Chlorphenamine | 15.2 | 1,440 | 1,060 | SRI | Antihistamine | |
Citalopram | 1.16 | 4,070 | 28,100 | SRI | SSRI | |
Clomipramine | 0.28 | 38 | 2,190 | SNRI | TCA | |
Cocaethylene[8] | 3,878 | >10,000 | 555 | SDRI | Stimulant | |
Cocaine[8] | 304 | 779 | 478 | SNDRI | Stimulant | |
Desipramine | 17.6 | 0.83 | 3,190 | SNRI | TCA | |
Desmethylcitalopram | 3.6 | 1,820 | 18,300 | SRI | SSRI | |
Desmethylsertraline | 3.0 | 390 | 129 | SRI | SSRI | |
Desmethylsibutramine[9] | 15 | 20 | 49 | SNDRI | SNRI | |
Desoxypipradrol[10] | 53,700 | 550 | 50 | NDRI | Stimulant | |
Desvenlafaxine*[11] | 47 | 531 | ND | SNRI | SNRI | |
Dextroamphetamine | >100,000 | 530 | 2,900 | NDRA | Stimulant | |
Dextromethamphetamine | >100,000 | 660 | 2,800 | NDRA | Stimulant | |
Didesmethylsibutramine[9] | 20 | 15 | 45 | SNDRI | SNRI | |
Diphenhydramine | 3,800 | 960 | 2,200 | N/A (IA) | Antihistamine | |
Dosulepin (dothiepin) | 8.6 | 46 | 5,310 | SNRI | TCA | |
Doxepin | 68 | 29.5 | 12,100 | SNRI | TCA | |
Duloxetine*[12] | 3.7 | 20 | 439 | SNRI | SNRI | |
Escitalopram[13] | 1.1 | 7,841 | 27,410 | SRI | SSRI | |
Etoperidone | 890 | 20,000 | 52,000 | SRI | SARI | |
Femoxetine | 11.0 | 760 | 2,050 | SRI | SSRI | |
Fluoxetine | 0.81 | 240 | 3,600 | SRI | SSRI | |
Fluvoxamine | 2.2 | 1,300 | 9,200 | SRI | SSRI | |
GBR-12935[8] | 289 | 277 | 4.90 | DRI | Stimulant | |
Imipramine | 1.40 | 37 | 8,500 | SNRI | TCA | |
Indatraline[8] | 3.10 | 12.6 | 1.90 | SNDRI | Stimulant | |
Iprindole | 1,620 | 1,262 | 6,530 | N/A (IA) | TCA | |
Levomilnacipran*[14] | 19.0 | 10.5 | >100,000 | SNRI | SNRI | |
Lofepramine | 70 | 5.4 | 18,000 | SNRI | TCA | |
Maprotiline | 5,800 | 11.1 | 1,000 | NRI | TeCA | |
Mazindol | 39 | 0.45 | 8.1 | NDRI | Stimulant | |
Methylphenidate | 44,000 | 234 | 24 | NDRI | Stimulant | |
Mianserin | 4,000 | 71 | 9,400 | NRI | TeCA | |
Milnacipran*[12] | 151 | 68 | >100,000 | SNRI | SNRI | |
Mirtazapine | >100,000 | 4,600 | >100,000 | N/A (IA) | TeCA | |
Modafinil*[15] | >50,000 | 136,000 | 4,043 | DRI | Stimulant | |
Nefazodone | 200 | 360 | 360 | SNDRI | SARI | |
Nefopam[16] | 29 | 33 | 531 | SNDRI | Analgesic | |
Nisoxetine[8] | 427 | 2.3 | 1,235 | NRI | Stimulant | |
Nomifensine | 1,010 | 15.6 | 56 | NDRI | Stimulant | |
Norfluoxetine | 1.47 | 1,426 | 420 | SRI | SSRI | |
Nortriptyline | 18 | 4.37 | 1,140 | SNRI | TCA | |
Oxaprotiline | 3,900 | 4.9 | 4,340 | NRI | TeCA | |
Paroxetine | 0.13 | 40 | 490 | SRI | SSRI | |
Protriptyline | 19.6 | 1.41 | 2,100 | SNRI | TCA | |
Reboxetine[17] | 129 | 1.1 | >10,000 | NRI | Stimulant | |
Sertraline | 0.29 | 420 | 25 | SRI | SSRI | |
Sibutramine[9] | 298 | 5,451 | 943 | SNDRI | SNRI | |
Trazodone | 160 | 8,500 | 7,400 | SRI | SARI | |
Trimipramine | 149 | 2,450 | 3,780 | SRI | TCA | |
Vanoxerine[8] | 73.2 | 79.2 | 4.3 | DRI | Stimulant | |
Venlafaxine*[12] | 145 | 1,420 | 3,070 | SNRI | SNRI | |
Vilazodone*[18] | 0.2 | ~60 | ND | SRI | SMS | |
Viloxazine | 17,300 | 155 | >100,000 | NRI | Stimulant | |
Vortioxetine*[19] | 5.4 | 890 (rat) | 140 (rat) | SRI | SMS | |
Zimelidine | 152 | 9,400 | 11,700 | SRI | SSRI | |
Values are Ki (nM) or, in some cases (*), IC50Tooltip half-maximal inhibitory concentration (nM). The smaller the value, the more strongly the drug binds to or inhibits the transporter. |