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F r o m W i k i p e d i a , t h e f r e e e n c y c l o p e d i a
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 in the treatment of ADHD Tooltip attention-deficit hyperactivity disorder or as appetite suppressants in the treatment of obesity also behave as MRIs, although notably amphetamine (and methamphetamine), which do act to some extent as monoamine reuptake inhibitors, exerts their effects primarily as releasing agents.[3] [4] Additionally, psychostimulants acting as MRIs that affect dopamine such as cocaine and methylphenidate are often abused as recreational drugs .[5] 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 .[6]
Types of MRIs [ edit ]
There are a variety of different kinds of MRIs, of which include the following:
Specific for one monoamine transporter
Non-specific, binding to two or more monoamine transporters
Binding profiles [ edit ]
Binding profiles of MRIs at human MATs [7]
Compound
SERT Tooltip Serotonin transporter
NET Tooltip Norepinephrine transporter
DAT Tooltip Dopamine transporter
Type
Class
Amfonelic acid
ND
ND
207
DRI
Stimulant
Amineptine *[8] [9]
>100,000 (rat)
10,000 (rat)
1,000–1,400 (rat)
DRI
Stimulant
Amitriptyline
4.30
35
3,250
SNRI
TCA
Amoxapine
58
16.0
4,310
SNRI
TeCA
Amphetamine
>100,000
ND
ND
NDRA
Stimulant
D-Amphetamine
>100,000
530
2,900
NDRA
Stimulant
L-Amphetamine
>100,000
ND
ND
NRA
Stimulant
Atomoxetine
77
5
1,451
NRI
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
Escitalopram [10]
1.1
7,841
27,410
SRI
SSRI
Clomipramine
0.28
38
2,190
SNRI
TCA
Cocaethylene [11]
3,878
>10,000
555
SDRI
Stimulant
Cocaine [11]
304
779
478
SNDRI
Stimulant
Cocaine [12]
313±17 (IC 50 )
292±34 (IC 50 )
211±19 (IC 50 )
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 [13]
15
20
49
SNDRI
SNRI
(R )-Desmethylsibutramine
44
4
12
SNDRI
SNRI
(S )-Desmethylsibutramine
9,200
870
180
SNDRI
SNRI
Desoxypipradrol [14]
53,700
550
50
NDRI
Stimulant
Desvenlafaxine *[15]
47
531
ND
SNRI
SNRI
Didesmethylsibutramine [13]
20
15
45
SNDRI
SNRI
(R )-Didesmethylsibutramine
140
13
8.9
SNDRI
SNRI
(S )-Didesmethylsibutramine
4,300
62
12
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 *[16]
3.7
20
439
SNRI
SNRI
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 [11]
289
277
4.90
DRI
Stimulant
Hydroxybupropion [17]
ND
1.7 (IC 50 )
>10 (IC 50 )
NDRI
Stimulant
Imipramine
1.40
37
8,500
SNRI
TCA
Indatraline [11]
3.10
12.6
1.90
SNDRI
Stimulant
Iprindole
1,620
1,262
6,530
N/A (IA )
TCA
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
MDPV Tooltip Methylenedioxypyrovalerone [18]
3,349
26
4.1
NDRI
Stimulant
Methamphetamine
>100,000
ND
ND
NDRA
Stimulant
D-Methamphetamine
>100,000
660
2,800
NDRA
Stimulant
L-Methamphetamine
>100,000
ND
ND
NRA
Stimulant
Methylphenidate
>10,000
788
121
NDRI
Stimulant
D-Methylphenidate
>10,000
206
161
NDRI
Stimulant
L-Methylphenidate
>6,700
>10,000
2,250
NDRI
Stimulant
Mianserin
4,000
71
9,400
NRI
TeCA
Milnacipran *[16]
151
68
>100,000
SNRI
SNRI
Levomilnacipran *[19]
19.0
10.5
>100,000
SNRI
SNRI
Mirtazapine
>100,000
4,600
>100,000
N/A (IA )
TeCA
Modafinil *[20]
>50,000
136,000
4,043
DRI
Stimulant
Nefazodone
200
360
360
SNDRI
SARI
Nefopam [21]
29
33
531
SNDRI
Analgesic
Nisoxetine [11]
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 [22]
129
1.1
>10,000
NRI
Stimulant
Sertraline
0.29
420
25
SRI
SSRI
Sibutramine [13]
298–2,800
350–5,451
943–1,200
SNDRI
SNRI
Trazodone
160
8,500
7,400
SRI
SARI
Trimipramine
149
2,450
3,780
SRI
TCA
Vanoxerine [11]
73.2
79.2
4.3
DRI
Stimulant
Venlafaxine *[16]
145
1,420
3,070
SNRI
SNRI
Vilazodone *[23]
0.2
~60
ND
SRI
SMS
Viloxazine
17,300
155
>100,000
NRI
Stimulant
Vortioxetine *[24]
5.4
890 (rat)
140 (rat)
SRI
SMS
Zimelidine
152
9,400
11,700
SRI
SSRI
Values are Ki (nM ) or, in some cases (*), IC 50 Tooltip half-maximal inhibitory concentration (nM ). The smaller the value, the more strongly the drug binds to or inhibits the transporter.
See also [ edit ]
References [ edit ]
^ Richard Finkel; Michelle Alexia Clark; Pamela C. Champe; Luigi X. Cubeddu (16 July 2008). Lippincott's Illustrated Reviews: Pharmacology . Lippincott Williams & Wilkins. p. 141. ISBN 978-0-7817-7155-9 . Retrieved 12 May 2012 .
^ Walker, Q. David; Morris, Sarah E.; Arrant, Andrew E.; Nagel, Jacqueline M.; Parylak, Sarah; Zhou, Guiying; Caster, Joseph M.; Kuhn, Cynthia M. (October 2010). "Dopamine Uptake Inhibitors but Not Dopamine Releasers Induce Greater Increases in Motor Behavior and Extracellular Dopamine in Adolescent Rats Than in Adult Male Rats" . The Journal of Pharmacology and Experimental Therapeutics . 335 (1 ): 124–132. doi :10.1124/jpet.110.167320 . ISSN 0022-3565 . PMC 2957786 . PMID 20605908 .
^ Stefan Offermanns; Walter Rosenthal (2008). Encyclopedia of Molecular Pharmacology . Springer. p. 1039. ISBN 978-3-540-38916-3 . Retrieved 12 May 2012 .
^ Pedro Ruiz; Eric C. Strain (15 April 2011). Lowinson and Ruiz's Substance Abuse: A Comprehensive Textbook . Lippincott Williams & Wilkins. p. 55. ISBN 978-1-60547-277-5 . Retrieved 12 May 2012 .
^ Hadlock GC, Webb KM, McFadden LM, et al. (November 2011). "4-Methylmethcathinone (mephedrone): neuropharmacological effects of a designer stimulant of abuse" . The Journal of Pharmacology and Experimental Therapeutics . 339 (2 ): 530–6. doi :10.1124/jpet.111.184119 . PMC 3200001 . PMID 21810934 .
^ Tatsumi M, Groshan K, Blakely RD, Richelson E (1997). "Pharmacological profile of antidepressants and related compounds at human monoamine transporters" (PDF) . Eur. J. Pharmacol . 340 (2–3): 249–58. doi :10.1016/s0014-2999(97 )01393-9 . PMID 9537821 . [dead link ]
^ Ceci A, Garattini S, Gobbi M, Mennini T (1986). "Effect of long term amineptine treatment on pre- and postsynaptic mechanisms in rat brain" . Br. J. Pharmacol . 88 (1 ): 269–75. doi :10.1111/j.1476-5381.1986.tb09495.x . PMC 1917102 . PMID 3708219 .
^ Garattini S, Mennini T (1989). "Pharmacology of amineptine: synthesis and updating". Clin Neuropharmacol . 12 Suppl 2: S13–8. doi :10.1097/00002826-198912002-00003 . PMID 2698268 . S2CID 10947713 .
^ Owens JM, Knight DL, Nemeroff CB (2002). "[Second generation SSRIS: human monoamine transporter binding profile of escitalopram and R-fluoxetine]". Encephale (in French). 28 (4 ): 350–5. PMID 12232544 .
^ a b c d e f Rothman RB, Baumann MH (2003). "Monoamine transporters and psychostimulant drugs". Eur. J. Pharmacol . 479 (1–3): 23–40. doi :10.1016/j.ejphar.2003.08.054 . PMID 14612135 .
^ http://www.emcdda.europa.eu/system/files/publications/1814/TDAS15001ENN.pdf [bare URL PDF ]
^ a b c Nisoli E, Carruba MO (2000). "An assessment of the safety and efficacy of sibutramine, an anti-obesity drug with a novel mechanism of action". Obes Rev . 1 (2 ): 127–39. doi :10.1046/j.1467-789x.2000.00020.x . PMID 12119986 . S2CID 20553857 .
^ Iversen L, Gibbons S, Treble R, Setola V, Huang XP, Roth BL (2013). "Neurochemical profiles of some novel psychoactive substances" . Eur. J. Pharmacol . 700 (1–3): 147–51. doi :10.1016/j.ejphar.2012.12.006 . PMC 3582025 . PMID 23261499 .
^ Deecher DC, Beyer CE, Johnston G, Bray J, Shah S, Abou-Gharbia M, Andree TH (2006). "Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor". J. Pharmacol. Exp. Ther . 318 (2 ): 657–65. doi :10.1124/jpet.106.103382 . PMID 16675639 . S2CID 15063064 .
^ a b c Vaishnavi SN, Nemeroff CB, Plott SJ, Rao SG, Kranzler J, Owens MJ (2004). "Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity". Biol. Psychiatry . 55 (3 ): 320–2. doi :10.1016/j.biopsych.2003.07.006 . PMID 14744476 . S2CID 29448095 .
^ Damaj, MI; Carroll, FI; Eaton, JB; Navarro, HA; Blough, BE; Mirza, S; Lukas, RJ; Martin, BR (September 2004). "Enantioselective effects of hydroxy metabolites of bupropion on behavior and on function of monoamine transporters and nicotinic receptors". Molecular Pharmacology . 66 (3 ): 675–82. doi :10.1124/mol.104.001313 . PMID 15322260 . S2CID 1577336 .
^ Baumann MH, Partilla JS, Lehner KR, Thorndike EB, Hoffman AF, Holy M, Rothman RB, Goldberg SR, Lupica CR, Sitte HH, Brandt SD, Tella SR, Cozzi NV, Schindler CW (2013). "Powerful cocaine-like actions of 3,4-methylenedioxypyrovalerone (MDPV), a principal constituent of psychoactive 'bath salts' products" . Neuropsychopharmacology . 38 (4 ): 552–62. doi :10.1038/npp.2012.204 . PMC 3572453 . PMID 23072836 .
^ Auclair AL, Martel JC, Assié MB, Bardin L, Heusler P, Cussac D, Marien M, Newman-Tancredi A, O'Connor JA, Depoortère R (2013). "Levomilnacipran (F2695), a norepinephrine-preferring SNRI: profile in vitro and in models of depression and anxiety" . Neuropharmacology . 70 : 338–47. doi :10.1016/j.neuropharm.2013.02.024 . PMID 23499664 .
^ Zolkowska D, Jain R, Rothman RB, Partilla JS, Roth BL, Setola V, Prisinzano TE, Baumann MH (2009). "Evidence for the involvement of dopamine transporters in behavioral stimulant effects of modafinil" . J. Pharmacol. Exp. Ther . 329 (2 ): 738–46. doi :10.1124/jpet.108.146142 . PMC 2672878 . PMID 19197004 .
^ Gregori-Puigjané E, Setola V, Hert J, Crews BA, Irwin JJ, Lounkine E, Marnett L, Roth BL, Shoichet BK (2012). "Identifying mechanism-of-action targets for drugs and probes" . Proc. Natl. Acad. Sci. U.S.A . 109 (28 ): 11178–83. Bibcode :2012PNAS..10911178G . doi :10.1073/pnas.1204524109 . PMC 3396511 . PMID 22711801 .
^ Bymaster FP, McNamara RK, Tran PV (2003). "New approaches to developing antidepressants by enhancing monoaminergic neurotransmission". Expert Opin Investig Drugs . 12 (4 ): 531–43. doi :10.1517/13543784.12.4.531 . PMID 12665410 . S2CID 20039451 .
^ Page ME, Cryan JF, Sullivan A, Dalvi A, Saucy B, Manning DR, Lucki I (2002). "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". J. Pharmacol. Exp. Ther . 302 (3 ): 1220–7. doi :10.1124/jpet.102.034280 . PMID 12183683 . S2CID 12020750 .
^ Bang-Andersen B, Ruhland T, Jørgensen M, Smith G, Frederiksen K, Jensen KG, Zhong H, Nielsen SM, Hogg S, Mørk A, Stensbøl TB (2011). "Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder". J. Med. Chem . 54 (9 ): 3206–21. doi :10.1021/jm101459g . PMID 21486038 .
External links [ edit ]
t
e
DAT Tooltip Dopamine transporter (DRIs Tooltip Dopamine reuptake inhibitors )
NET Tooltip Norepinephrine transporter (NRIs Tooltip Norepinephrine reuptake inhibitors )
Others: Antihistamines (e.g., brompheniramine , chlorphenamine , pheniramine , tripelennamine )
Antipsychotics (e.g., loxapine , ziprasidone )
Arylcyclohexylamines (e.g., ketamine , phencyclidine )
Dopexamine
Ephenidine
Ginkgo biloba
Indeloxazine
Nefazodone
Opioids (e.g., desmetramadol , methadone , pethidine (meperidine) , tapentadol , tramadol , levorphanol )
SERT Tooltip Serotonin transporter (SRIs Tooltip Serotonin reuptake inhibitors )
Others: A-80426
Amoxapine
Antihistamines (e.g., brompheniramine , chlorphenamine , dimenhydrinate , diphenhydramine , mepyramine (pyrilamine) , pheniramine , tripelennamine )
Antipsychotics (e.g., loxapine , ziprasidone )
Arylcyclohexylamines (e.g., 3-MeO-PCP , esketamine , ketamine , methoxetamine , phencyclidine )
Cyclobenzaprine
Delucemine
Dextromethorphan
Dextrorphan
Efavirenz
Hypidone
Medifoxamine
Mesembrine
Mifepristone
MIN-117 (WF-516)
N-Me-5-HT
Opioids (e.g., dextropropoxyphene , methadone , pethidine (meperidine) , levorphanol , tapentadol , tramadol )
Roxindole
VMATs Tooltip Vesicular monoamine transporters
Others
See also: Receptor/signaling modulators • Monoamine releasing agents • Adrenergics • Dopaminergics • Serotonergics • Monoamine metabolism modulators • Monoamine neurotoxins
R e t r i e v e d f r o m " https://en.wikipedia.org/w/index.php?title=Monoamine_reuptake_inhibitor&oldid=1191317162 "
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