List of adrenergic drugs

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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).

Contents

1 Receptor ligands
2 Reuptake inhibitors
- 2.1 Norepinephrine transporter (NET) inhibitors
- 2.2 Vesicular monoamine transporter (VMAT) inhibitors
3 Releasing agents
4 Enzyme inhibitors
- 4.1 Anabolism
- 4.2 Catabolism
  - 4.2.1 Monoamine oxidase (MAO) inhibitors
  - 4.2.2 Catechol-O-methyl transferase (COMT) inhibitors
5 Others
6 References

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.)

Dimethylamphetamine

Dimethylcathinone (dimethylpropion, metamfepramone)

Ethylamphetamine

Lisdexamfetamine

MDA (tenamfetamine)

Methamphetamine

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

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

Methylhexanamine

Phthalimidopropiophenone

Propylhexedrine

levopropylhexedrine

Enzyme inhibitors

Anabolism

Phenylalanine hydroxylase (PAH) inhibitors

3,4-Dihydroxystyrene

Tyrosine hydroxylase inhibitors

Aromatic L-amino acid decarboxylase (AAAD) inhibitors

Dopamine-beta-hydroxylase (DBH) inhibitors

Phenylethanolamine N-methyltransferase (PNMT) inhibitors

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

Harmala alkaloids

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

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Receptor ligands

Agonists: 6-FNE; Amidephrine; Anisodine; Buspirone; Cirazoline; Corbadrine; Dipivefrine; Dopamine; Ephedrine; Epinephrine; Etilefrine; Ethylnorepinephrine; Indanidine; Metaraminol; Methoxamine; Methyldopa; Midodrine; Naphazoline; Norepinephrine; Octopamine (drug); Oxymetazoline; Phenylephrine; Phenylpropanolamine; Pseudoephedrine; Synephrine; Tetrahydrozoline; Tiamenidine; Xylometazoline

Antagonists: Abanoquil; Adimolol; Ajmalicine; Alfuzosin; Amosulalol; Anisodamine; Arotinolol; Atiprosin; Atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine, risperidone); Benoxathian; Buflomedil; Bunazosin; Carvedilol; Corynanthine; Dapiprazole; Domesticine; Doxazosin; Ergolines (e.g., ergotamine, dihydroergotamine, lisuride, terguride); Etoperidone; Eugenodilol; Fenspiride; Hydroxyzine; Indoramin; Ketanserin; L-765,314; Labetalol; mCPP; Mepiprazole; Metazosin; Monatepil; Moxisylyte; Naftopidil; Nantenine; Nefazodone; Neldazosin; Niaprazine; Nicergoline; Niguldipine; Pardoprunox; Pelanserin; Phendioxan; Phenoxybenzamine; Phentolamine; Piperoxan; Prazosin; Quinazosin; Ritanserin; Silodosin; Spiperone; Talipexole; Tamsulosin; Terazosin; Tiodazosin; Tolazoline; Trazodone; Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin); Tricyclic antidepressants (e.g., amitriptyline, clomipramine, doxepin, imipramine, trimipramine); Trimazosin; Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine); Urapidil; WB-4101; Zolertine

Agonists: (R)-3-Nitrobiphenyline; 4-NEMD; 6-FNE; Amitraz; Apraclonidine; Brimonidine; Cannabivarin; Clonidine; Corbadrine; Detomidine; Dexmedetomidine; Dihydroergotamine; Dipivefrine; Dopamine; Ephedrine; Ergotamine; Epinephrine; Etilefrine; Ethylnorepinephrine; Guanabenz; Guanfacine; Guanoxabenz; Lofexidine; Medetomidine; Methamphetamine; Methyldopa; Mivazerol; Naphazoline; Norepinephrine; Oxymetazoline; Phenylpropanolamine; Piperoxan; Pseudoephedrine; Rilmenidine; Romifidine; Talipexole; Tetrahydrozoline; Tiamenidine; Tizanidine; Tolonidine; Urapidil; Xylazine; Xylometazoline

Antagonists: 1-PP; Adimolol; Aptazapine; Atipamezole; Atypical antipsychotics (e.g., asenapine, clozapine, lurasidone, paliperidone, quetiapine, risperidone, zotepine); Azapirones (e.g., buspirone, tandospirone); BRL-44408; Buflomedil; Cirazoline; Efaroxan; Esmirtazapine; Fenmetozole; Fluparoxan; Idazoxan; mCPP; Mianserin; Mirtazapine; NAN-190; Olanzapine; Pardoprunox; Phentolamine; Phenoxybenzamine; Piperoxan; Piribedil; Rauwolscine; Rotigotine; SB-269970; Setiptiline; Spiroxatrine; Sunepitron; Tolazoline; Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine); Yohimbine

Agonists: Abediterol; Alifedrine; Amibegron; Arbutamine; Arformoterol; Arotinolol; BAAM; Bambuterol; Befunolol; Bitolterol; Broxaterol; Buphenine; Carbuterol; Carmoterol; Cimaterol; Clenbuterol; Corbadrine; Denopamine; Dipivefrine; Dobutamine; Dopamine; Dopexamine; Ephedrine; Epinephrine; Etafedrine; Etilefrine; Ethylnorepinephrine; Fenoterol; Formoterol; Hexoprenaline; Higenamine; Indacaterol; Isoetarine; Isoprenaline; Isoxsuprine; Levosalbutamol; Mabuterol; Methoxyphenamine; Methyldopa; Mirabegron; Norepinephrine; Orciprenaline; Oxyfedrine; PF-610355; Phenylpropanolamine; Pirbuterol; Prenalterol; Ractopamine; Procaterol; Pseudoephedrine; Reproterol; Rimiterol; Ritodrine; Salbutamol; Salmeterol; Solabegron; Terbutaline; Tretoquinol; Tulobuterol; Vilanterol; Xamoterol; Zilpaterol; Zinterol

Antagonists: Acebutolol; Adaprolol; Adimolol; Afurolol; Alprenolol; Alprenoxime; Amosulalol; Ancarolol; Arnolol; Arotinolol; Atenolol; Befunolol; Betaxolol; Bevantolol; Bisoprolol; Bopindolol; Bornaprolol; Brefonalol; Bucindolol; Bucumolol; Bufetolol; Bufuralol; Bunitrolol; Bunolol; Bupranolol; Butaxamine; Butidrine; Butofilolol; Capsinolol; Carazolol; Carpindolol; Carteolol; Carvedilol; Celiprolol; Cetamolol; Cicloprolol; Cinamolol; Cloranolol; Cyanopindolol; Dalbraminol; Dexpropranolol; Diacetolol; Dichloroisoprenaline; Dihydroalprenolol; Dilevalol; Diprafenone; Draquinolol; Ecastolol; Epanolol; Ericolol; Ersentilide; Esatenolol; Esprolol; Eugenodilol; Exaprolol; Falintolol; Flestolol; Flusoxolol; Hydroxycarteolol; Hydroxytertatolol; ICI-118,551; Idropranolol; Indenolol; Indopanolol; Iodocyanopindolol; Iprocrolol; Isoxaprolol; Isamoltane; Labetalol; Landiolol; Levobetaxolol; Levobunolol; Levomoprolol; Medroxalol; Mepindolol; Metipranolol; Metoprolol; Moprolol; Nadolol; Nadoxolol; Nebivolol; Nifenalol; Nipradilol; Oxprenolol; Pacrinolol; Pafenolol; Pamatolol; Pargolol; Penbutolol; Pindolol; Practolol; Primidolol; Procinolol; Pronethalol; Propafenone; Propranolol; Ridazolol; Ronactolol; Soquinolol; Sotalol; Spirendolol; SR 59230A; Sulfinalol; Talinolol; Tazolol; Tertatolol; Tienoxolol; Tilisolol; Timolol; Tiprenolol; Tolamolol; Toliprolol; Xibenolol; Xipranolol

Reuptake inhibitors

Selective norepinephrine reuptake inhibitors Amedalin Ciclazindol Daledalin Edivoxetine Esreboxetine Lortalamine Mazindol Nisoxetine Reboxetine Talopram Talsupram Tandamine Viloxazine
Norepinephrine-dopamine reuptake inhibitors Amineptine Bupropion Fencamine Fencamfamine Hydroxybupropion Lefetamine Levophacetoperane LR-5182 Manifaxine Methylphenidate Nomifensine O-2172 Radafaxine
Serotonin-norepinephrine reuptake inhibitors Atomoxetine (tomoxetine) Bicifadine BTS-54505 Desvenlafaxine Duloxetine Eclanamine Levomilnacipran McN-5652 Milnacipran N-Methyl-PPPA PPPA Sibutramine Venlafaxine WY-45233
Serotonin-norepinephrine-dopamine reuptake inhibitors (S)-Duloxetine 3,3-Diphenylcyclobutanamine Amifitadine Ansofaxine Bicifadine Brasofensine Centanafadine Cocaine Dasotraline Desmethylsertraline Diclofensine DOV-102677 DOV-216303 EXP-561 Fezolamine HDMP-28 Indatraline JNJ-7925476 JZ-IV-10 Liafensine Mazindol Naphyrone Nefazodone Nefopam NS-2359 Perafensine PRC200 SEP-228431 SEP-228432 Tedatioxetine Tesofensine
Tricyclic antidepressants Amitriptyline Butriptyline Cianopramine Clomipramine Desipramine Dosulepin Doxepin Imipramine Lofepramine Melitracen Nortriptyline Protriptyline Trimipramine
Tetracyclic antidepressants Amoxapine Maprotiline Mianserin Oxaprotiline Setiptiline
Others Antihistamines (e.g., brompheniramine, chlorphenamine, pheniramine, tripelennamine) Arylcyclohexylamines (e.g., ketamine, phencyclidine) CP-39,332 EXP-561 Fezolamine Ginkgo biloba Indeloxazine Loxapine Nefazodone Nefopam Opioids (e.g., methadone, pethidine (meperidine), tapentadol, tramadol, levorphanol) Pridefine Tedatioxetine Teniloxazine Tofenacin Tropanes (e.g., cocaine) Ziprasidone

Amiodarone
Amphetamines (e.g., amphetamine, methamphetamine, MDMA)
Bietaserpine
Deserpidine
Efavirenz
GBR-12935
Ibogaine
Ketanserin
Lobeline
Reserpine
Rose bengal
Tetrabenazine
Vanoxerine (GBR-12909)

Releasing agents

Morpholines Fenbutrazate Fenmetramide Morazone Morforex Phendimetrazine Phenmetrazine Pseudophenmetrazine
Oxazolines 4-MAR Aminorex Clominorex Cyclazodone Fenozolone Fluminorex Pemoline Thozalinone
Phenethylamines (also amphetamines, cathinones, etc) 2-OH-PEA 4-CAB 4-FA 4-FMA 4-MA 4-MMA Alfetamine Amfecloral Amfepentorex Amfepramone Amphetamine Dextroamphetamine Levoamphetamine Amphetaminil β-Me-PEA BDB Benzphetamine BOH Buphedrone Bupropion Butylone Cathine Cathinone Clobenzorex Clortermine Dimethylamphetamine DMA DMMA EBDB Ephedrine Ethcathinone Ethylone Etilamfetamine Famprofazone Fenethylline Fenproporex Flephedrone Fludorex Furfenorex Hordenine 4-Hydroxyamphetamine 5-APDI (IAP) 5-MAPDI (IMP) Iofetamine (123I) Lisdexamfetamine Lophophine MBDB MDA MDEA MDMA Metamfepramone MDMPEA MDOH MDPEA Mefenorex Mephedrone Mephentermine Methamphetamine Dextromethamphetamine Levomethamphetamine Methcathinone Methedrone Methylone Morforex Naphthylaminopropane Ortetamine pBA pCA Pentorex Phenethylamine Pholedrine Phenpromethamine Phentermine Phenylpropanolamine pIA Prenylamine Propylamphetamine Pseudoephedrine Selegiline (also D-Deprenyl) Tiflorex Tyramine Xylopropamine Zylofuramine
Piperazines 2C-B-BZP BZP MBZP mCPP MDBZP MeOPP pFPP
Others 2-ADN 2-AI 2-AT 2-BP 4-BP 5-IAI Clofenciclan Cyclopentamine Cypenamine Cyprodenate Feprosidnine Gilutensin Heptaminol Hexacyclonate Indanorex Isometheptene Methylhexanamine Octodrine Phthalimidopropiophenone Propylhexedrine (Levopropylhexedrine) Tuaminoheptane

Enzyme inhibitors

3,4-Dihydroxystyrene

Nonselective Benmoxin Caroxazone Echinopsidine Furazolidone Hydralazine Indantadol Iproclozide Iproniazid Isocarboxazid Isoniazid Linezolid Mebanazine Metfendrazine Nialamide Octamoxin Paraxazone Phenelzine Pheniprazine Phenoxypropazine Pivhydrazine Procarbazine Safrazine Tranylcypromine
MAO-A selective Amiflamine Bazinaprine Befloxatone Brofaromine Cimoxatone Clorgiline CX157 (Tyrima) Eprobemide Esuprone Harmala alkaloids Harmine Harmaline Tetrahydroharmine Harman Methylene blue Metralindole Minaprine Moclobemide Pirlindole Sercloremine Tetrindole Toloxatone
MAO-B selective Ladostigil Lazabemide Milacemide Mofegiline Pargyline Rasagiline Safinamide Selegiline (also D-Deprenyl)

Others

L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa) → Dopamine
L-DOPS (Droxidopa)

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⁺)

Others

Activity enhancers BPAP PPAP
Release blockers Bethanidine Bretylium Guanadrel Guanazodine Guanethidine Guanoxan

See also:: Dopaminergics; Melatonergics; Serotonergics; List of adrenergic drugs

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Alpha-adrenergic agonists

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