List of adrenergic drugs

This is a list of adrenergic drugs. These are pharmaceutical drugs, naturally occurring compounds and other chemicals that influence the function of the neurotransmitter epinephrine (adrenaline).

Receptor ligands

α₁-adrenergic receptor ligands

Agonists

Antagonists

Many tricyclic antidepressants, tetracyclic antidepressants, antipsychotics, ergolines, and some piperazines like buspirone, trazodone, nefazodone, etoperidone, and mepiprazole antagonize α₁-adrenergic receptors as well, which contributes to their side effects such as orthostatic hypotension.

α₂-adrenergic receptor ligands

Agonists

Antagonists

Many atypical antipsychotics and azapirones like buspirone and gepirone (via metabolite pyrimidinylpiperazine) antagonize α₂-adrenergic receptors as well.

β-adrenergic receptor ligands

Agonists

Antagonists

Reuptake inhibitors

Norepinephrine transporter (NET) inhibitors

Selective norepinephrine reuptake inhibitors: Amedalin; Atomoxetine (tomoxetine); Ciclazindol; Daledalin; Esreboxetine; Lortalamine; Mazindol; Nisoxetine; Reboxetine; Talopram; Talsupram; Tandamine; Viloxazine

Norepinephrine-dopamine reuptake inhibitors: Amineptine; Bupropion (amfebutamone); Fencamine; Fencamfamine; Lefetamine; Levophacetoperane; LR-5182; Manifaxine; Methylphenidate; Nomifensine; O-2172; Radafaxine

Serotonin-norepinephrine reuptake inhibitors: Bicifadine; Desvenlafaxine; Duloxetine; Eclanamine; Levomilnacipran; Milnacipran; Sibutramine; Venlafaxine

Serotonin-norepinephrine-dopamine reuptake inhibitors: Brasofensine; Diclofensine; DOV-102,677; DOV-21,947; DOV-216,303; JNJ-7925476; JZ-IV-10; Methylnaphthidate; Naphyrone; NS-2359; PRC200-SS; SEP-225,289; SEP-227,162; Tesofensine

Tricyclic antidepressants: Amitriptyline; Butriptyline; Cianopramine; Clomipramine; Desipramine; Dosulepin; Doxepin; Imipramine; Lofepramine; melitracen; Nortriptyline; Protriptyline; Trimipramine

Tetracyclic antidepressants: Amoxapine; Maprotiline; Mianserin; Oxaprotiline; Setiptiline

Others: Cocaine; CP-39,332; EXP-561; Fezolamine; Ginkgo biloba; Indeloxazine; Nefazodone; Nefopam; Pridefrine; Tapentadol; Teniloxazine; Tramadol; Ziprasidone

Vesicular monoamine transporter (VMAT) inhibitors

Releasing agents

Morpholines: Fenbutrazate; Morazone; Phendimetrazine; Phenmetrazine

Oxazolines: Aminorex; Clominorex; Cyclazodone; Fenozolone; Fluminorex; 4-Methylaminorex; Pemoline; Thozalinone

Phenethylamines (also amphetamines, cathinones, phentermines, etc.)

2-OH-PEA

4-MA

4-MMA

Butylone

Dimethylamphetamine

Dimethylcathinone (dimethylpropion, metamfepramone)

DMA

Ethylamphetamine

Flephedrone

Hordenine

IAP

IMP

Lisdexamfetamine

MDA (tenamfetamine)

MDEA

Methamphetamine

Methylone

Ortetamine

pCA

Pentorex (phenpentermine)

Phenpromethamine

Phenylpropanolamine

Propylamphetamine

Pseudoephedrine

Selegiline (L-deprenyl)

Piperazines: Benzylpiperazine (BZP); 2,5-Dimethoxy-4-bromobenzylpiperazine (2C-B-BZP); Methylbenzylpiperazine (MBZP); Metachlorophenylpiperazine (mCPP); Methylenedioxybenzylpiperazine (MDBZP); Methoxyphenylpiperazine (MeOPP); Parafluorophenylpiperazine (pFPP)

Others

2-Amino-1,2-dihydronaphthalene

2-Aminotetralin

2-Benzylpiperidine

4-Benzylpiperidine

Feprosidnine

5-Iodo-2-aminoindane (5-IAI)

Methylhexanamine

Phthalimidopropiophenone

Propylhexedrine

levopropylhexedrine

Enzyme inhibitors

Anabolism

Phenylalanine hydroxylase (PAH) inhibitors

3,4-Dihydroxystyrene

Tyrosine hydroxylase inhibitors

3-Iodotyrosine
Aquayamycin
Bulbocapnine
Metirosine
Oudenone

Aromatic L-amino acid decarboxylase (AAAD) inhibitors

Dopamine-beta-hydroxylase (DBH) inhibitors

Bupicomide
Disulfiram
Dopastin
Fusaric acid
Nepicastat
Phenopicolinic acid
Tropolone

Phenylethanolamine N-methyltransferase (PNMT) inhibitors

CGS-19281A
SKF-64139
SKF-7698

Catabolism

Monoamine oxidase (MAO) inhibitors

Nonselective: Benmoxin; Caroxazone; Echinopsidine; Furazolidone; Hydralazine; Indantadol; Iproclozide; Iproniazid; Isocarboxazid; Isoniazid; Linezolid; Mebanazine; Metfendrazine; Nialamide; Octamoxin; Paraxazone; Phenelzine; Pheniprazine; Phenoxypropazine; Pivalylbenzhydrazine; Procarbazine; Safrazine; Tranylcypromine

MAO-A selective

Befloxatone

Harmala alkaloids

harmine
harmaline
tetrahydroharmine
harman
norharman
etc.

MAO-B selective: D-Deprenyl; Selegiline (L-deprenyl); Ladostigil; Lazabemide; Milacemide; Mofegiline; Pargyline; Rasagiline; Safinamide

MAO-B inhibitors also influence norepinephrine/epinephrine levels since they inhibit the breakdown of their precursor dopamine.

Catechol-O-methyl transferase (COMT) inhibitors

Others

Precursors

L-Phenylalanine

L-Phenylalanine → L-tyrosine → L-DOPA (levodopa) → dopamine
L-DOPS (droxidopa)

Cofactors

Ferrous iron (Fe²⁺)
S-Adenosyl-L-methionine
Vitamin B₃
- niacin
- nicotinamide → NADPH
Vitamin B₆ (pyridoxine, pyridoxamine, pyridoxal → Pyridoxal phosphate)
Vitamin B₉ (folic acid → tetrahydrofolic acid)
Vitamin C
- ascorbic acid
Zinc (Zn²⁺)

Activity enhancers

Benzofuranylpropylaminopentane (BPAP)
Phenylpropylaminopentane (PPAP)

Release blockers

Toxins

Oxidopamine (6-hydroxydopamine)

References

↑ Prischich, Davia; Gomila, Alexandre M. J.; Milla-Navarro, Santiago; Sangüesa, Gemma; Diez-Alarcia, Rebeca; Preda, Beatrice; Matera, Carlo; Batlle, Montserrat; Ramírez, Laura; Giralt, Ernest; Hernando, Jordi; Guasch, Eduard; Meana, J. Javier; de la Villa, Pedro; Gorostiza, Pau (2020). "Adrenergic modulation with photochromic ligands". Angewandte Chemie International Edition. doi:10.1002/anie.202010553. hdl:2434/778579. ISSN 1433-7851.

Adrenergic receptor modulators

α₁

Agonists

Antagonists

α₂

Agonists

Antagonists

β

Agonists

Antagonists

See also: Receptor/signaling modulators
Dopaminergics
Serotonergics
Monoamine reuptake inhibitors
Monoamine releasing agents
Monoamine metabolism modulators
Monoamine neurotoxins

Monoamine reuptake inhibitors

Piperazines: DBL-583 GBR-12783 GBR-12935 GBR-13069 GBR-13098 Nefazodone Vanoxerine
Piperidines: 4-Fluoropethidine Benocyclidine (BTCP) Desoxypipradrol Dexmethylphenidate Difemetorex Ethylphenidate HDMP-28 Methylphenidate Pethidine (meperidine) Phencyclidine Pipradrol Serdexmethylphenidate Tenocyclidine
Pyrrolidines: Diphenylprolinol MDPV Naphyrone Prolintane Pyrovalerone
Tropanes: Altropane Benzatropine (benztropine) Brasofensine CFT Cocaine Dichloropane Difluoropine Etybenzatropine (ethybenztropine) FE-β-CPPIT FP-β-CPPIT Ioflupane (¹²³I) RTI-55 RTI-112 RTI-113 RTI-121 RTI-126 RTI-150 RTI-177 RTI-229 RTI-336 Tesofensine Troparil Tropoxane WF-11 WF-23 WF-31 WF-33
Others: Adrafinil Amifitadine Armodafinil Amfonelic acid Amineptine Ansofaxine BTQ BTS 74,398 Bupropion Chaenomeles speciosa Ciclazindol Dasotraline Desmethylsertraline Desmethylsibutramine (BTS-54354) Diclofensine Didesmethylsibutramine (BTS-54505) Dimethocaine Diphenylpyraline Dizocilpine (MK-801) DOV-102,677 DOV-216,303 Efavirenz Ephenidine Esketamine EXP-561 Fencamfamin Fezolamine Fluorenol GYKI-52895 Indatraline Ketamine Lefetamine Levophacetoperane Liafensine LR-5182 Manifaxine Mazindol Medifoxamine Mesocarb Metaphit MIN-117 (WF-516) Modafinil Nefopam Nomifensine NS-2359 O-2172 Oroxylin A Perafensine Pridefine Radafaxine Rimcazole Sertraline Sibutramine Solriamfetol Tametraline Tedatioxetine Tripelennamine Venlafaxine

Selective norepinephrine reuptake inhibitors: Amedalin Alseroxylon Ciclazindol Daledalin Edivoxetine Esreboxetine Lortalamine Mazindol Nisoxetine Reboxetine Talopram Talsupram Tandamine Teniloxazine Viloxazine
Norepinephrine–dopamine reuptake inhibitors: Amineptine Bupropion Fencamine Fencamfamin Hydroxybupropion Lefetamine Levophacetoperane LR-5182 Manifaxine Methylphenidate Nomifensine O-2172 Radafaxine Serdexmethylphenidate Solriamfetol
Serotonin–norepinephrine reuptake inhibitors: Atomoxetine (tomoxetine) CP-39,332 Desvenlafaxine Duloxetine Eclanamine Levomilnacipran McN5652 Milnacipran N-Methyl-PPPA Nafenodone PPPA Tofenacin Venlafaxine
Serotonin–norepinephrine–dopamine reuptake inhibitors: 3,3-Diphenylcyclobutanamine Amifitadine Ansofaxine Bicifadine Brasofensine Centanafadine Cocaine Dasotraline Desmethylsertraline Desmethylsibutramine (BTS-54354) Diclofensine Didesmethylsibutramine (BTS-54505) DOV-102677 DOV-216303 EXP-561 Fezolamine HDMP-28 Indatraline JNJ-7925476 JZ-IV-10 Liafensine Mazindol Naphyrone Nefazodone Nefopam NS-2359 Perafensine PRC200 Pridefine SEP-228431 SEP-228432 Sibutramine Tedatioxetine Tesofensine Tropanes (e.g., cocaine)
Tricyclic antidepressants: Amitriptyline Butriptyline Cianopramine Clomipramine Desipramine Dosulepin (dothiepin) Doxepin Imipramine Lofepramine Melitracen Nortriptyline Protriptyline Trimipramine
Tetracyclic antidepressants: Amoxapine Maprotiline Mianserin Oxaprotiline Setiptiline
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
(SRIs)

Selective serotonin reuptake inhibitors: 6-Nitroquipazine Alaproclate Centpropazine Cericlamine Citalopram Dapoxetine Desmethylcitalopram Didesmethylcitalopram Escitalopram Femoxetine Fluoxetine Fluvoxamine Indalpine Ifoxetine Norfluoxetine Omiloxetine Panuramine Paroxetine PIM-35 Pirandamine RTI-353 Seproxetine Sertraline Zimelidine Selective serotonin reuptake inhibitors and serotonin receptor modulators: Etoperidone Litoxetine Lubazodone LY-393558 Quipazine SB-649915 TGBA01AD Trazodone Vilazodone Vortioxetine
Serotonin–norepinephrine reuptake inhibitors: Atomoxetine (tomoxetine) Bicifadine CP-39332 Desvenlafaxine Duloxetine Eclanamine Levomilnacipran McN5652 Milnacipran N-Methyl-PPPA PPPA Tofenacin Venlafaxine
Serotonin–norepinephrine–dopamine reuptake inhibitors: 3,3-Diphenylcyclobutanamine Amifitadine Ansofaxine Bicifadine Brasofensine Centanafadine Cocaine Dasotraline Desmethylsertraline Desmethylsibutramine (BTS-54354) Diclofensine Didesmethylsibutramine (BTS-54505) DOV-102677 DOV-216303 EXP-561 Fezolamine HDMP-28 Indatraline JNJ-7925476 JZ-IV-10 Liafensine Mazindol Naphyrone Nefazodone Nefopam NS-2359 Perafensine PRC200 Pridefine SEP-228431 SEP-228432 Sibutramine Tedatioxetine Tesofensine Tropanes (e.g., cocaine)
Tricyclic antidepressants: Amitriptyline Cianopramine Clomipramine Cyanodothiepin Desipramine Dosulepin (dothiepin) Doxepin Imipramine Lofepramine Nortriptyline Pipofezine Protriptyline
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

Amiodarone
Amphetamines (e.g., amphetamine, methamphetamine, MDMA)
APP
AZIK
Bietaserpine
Deserpidine
Deutetrabenazine
Dihydrotetrabenazine
Efavirenz
GBR-12935
GZ-793A
Ibogaine
Ketanserin
Lobeline
Methoxytetrabenazine
Reserpine
Rose bengal
Tetrabenazine
Valbenazine
Vanoxerine (GBR-12909)

Others

DAT enhancers: Luteolin

DAT modulators: Agonist-like: SoRI-9804
SoRI-20040; Antagonist-like: SoRI-20041

See also: Receptor/signaling modulators • Monoamine releasing agents • Adrenergics • Dopaminergics • Serotonergics • Monoamine metabolism modulators • Monoamine neurotoxins

Monoamine metabolism modulators

Non-specific

Substrates→Products: L-DOPA (levodopa)→Dopamine
5-HTP→Serotonin
L-Histidine→Histamine
Phenylalanine→Phenethylamine
L-Tyrosine→Tyramine
Tryptophan→Tryptamine

Inhibitors: Benserazide
Carbidopa
DFMD
Genistein
Methyldopa

Substrates→Products (with ALDH/ALR): Epinephrine (adrenaline)→DHMA Metanephrine→MHPG/VMA Norepinephrine (noradrenaline)→DHMA Normetanephrine→MHPG/VMA Dopamine→DOPAC 3-Methoxytyramine→HVA Serotonin→5-HIAA Inhibitors: Non-selective: Benmoxin Caroxazone Echinopsidine Furazolidone Guineesine Hydralazine Indantadol Iproclozide Iproniazid Isocarboxazid Isoniazid Linezolid Mebanazine Metfendrazine Nialamide Octamoxin Paraxazone Phenelzine Pheniprazine Phenoxypropazine Pivhydrazine Procarbazine Safrazine Tranylcypromine
Inhibitors: MAO-A-selective: Amiflamine Bazinaprine Befloxatone Brofaromine Cimoxatone Clorgiline CX157 (Tyrima) Eprobemide Esuprone Harmala alkaloids (e.g., harmine, harmaline, harman, norharman, tetrahydroharmine) Methylene blue Metralindole Minaprine Moclobemide Pirlindole Sercloremine Tetrindole Toloxatone
Inhibitors: MAO-B selective: Adarigiline Almoxatone D-Deprenyl Ethanol Ladostigil Lazabemide Milacemide Mofegiline Nicotine Pargyline^‡ Rasagiline Safinamide Selegiline (L-Deprenyl) Sembragiline

Phenethylamines
(dopamine, epinephrine,
norepinephrine)

PAH	Substrates→Products: Phenylalanine→Tyrosine Inhibitors: 3,4-Dihydroxystyrene
TH	Substrates→Products: Tyrosine→L-DOPA (levodopa) Inhibitors: 2-Hydroxyestradiol 2-Hydroxyestrone 3-Iodotyrosine Aquayamycin Bulbocapnine Metirosine Oudenone
DBH	Substrates→Products: Dopamine→Norepinephrine (Noradrenaline) Inhibitors: Bupicomide Disulfiram Dopastin Fusaric acid Nepicastat Phenopicolinic acid Tropolone
PNMT	Substrates→Products: Norepinephrine (noradrenaline)→Epinephrine (adrenaline) Inhibitors: CGS-19281A SKF-64139 SKF-7698
COMT	Substrates→Products: Dopamine→3-Methoxytyramine DOPAC→Homovanillic acid Norepinephrine→Normetanephrine Epinephrine→Metanephrine DOPEG→MOPEG DOMA→VMA 2-Hydroxyestradiol→2-Methoxyestradiol 2-Hydroxyestrone→2-Methoxyestrone 4-Hydroxyestradiol→4-Methoxyestradiol 4-Hydroxyestrone→4-Methoxyestrone Inhibitors: 2-Hydroxyestradiol 2-Hydroxyestrone Entacapone Neluxicapone Nitecapone Opicapone Quinalizarin Tolcapone

Tryptamines
(serotonin, melatonin)

TPH	Substrates→Products: Tryptophan→5-HTP Inhibitors: AGN-2979 Fenclonine (PCPA) Telotristat ethyl
AANAT	Substrates→Products: Serotonin→N-Acetylserotonin
ASMT	Substrates→Products: N-Acetylserotonin→Melatonin

Histamine

HDC	Substrates→Products: L-Histidine→Histamine Inhibitors: Catechin Alpha-Fluoromethylhistidine Histidine methyl ester Meciadanol Naringenin Tritoqualine
HNMT	Substrates→Products: Histamine→N-Methylhistamine Inhibitors: Amodiaquine Diphenhydramine Harmaline Metoprine Quinacrine SKF-91488 Tacrine
DAO	Substrates→Products: Histamine→Imidazole acetic acid Inhibitors: Pimagedine (aminoguanidine)

See also: Receptor/signaling modulators • Adrenergics • Dopaminergics • Melatonergics • Serotonergics • Monoamine reuptake inhibitors • Monoamine releasing agents • Monoamine neurotoxins

Monoamine neurotoxins
Adrenergic	DSP-4 Oxidopamine (6-OHDA)
Dopaminergic	Fenpropathrin Methamphetamine MPP⁺ MPTP Norsalsolinol Oxidopamine (6-OHDA) Rotenone
Serotonergic	3-CA 4-CAB 5,7-DHT α-Me-DA (3,4-DHA) αET αMT DCA MDA (tenamfetamine) MDMA (midomafetamine) PBA PCA PIA
See also: Receptor/signaling modulators • Adrenergics • Dopaminergics • Melatonergics • Serotonergics • Monoamine reuptake inhibitors • Monoamine releasing agents • Monoamine metabolism modulators

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