List of Adrenergic Drugs: History
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Subjects: Chemistry, Applied
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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).

  • epinephrine
  • neurotransmitter
  • adrenaline

1. Receptor ligands

1.1. α1-Adrenergic Receptor Ligands

Agonists

Etilefrine
  • Amidephrine
  • Anisodamine
  • Anisodine
  • Cirazoline
  • Dipivefrine
  • Dopamine
  • Ephedrine
  • Epinephrine (adrenaline)
  • Etilefrine
  • Ethylnorepinephrine
  • 5-Fluoronorepinephrine
  • 6-Fluoronorepinephrine
  • Indanidine
  • Levonordefrin
  • Metaraminol
  • Methoxamine
  • Methyldopa
  • Midodrine
  • Naphazoline
  • Norepinephrine (noradrenaline)
  • Octopamine
  • Oxymetazoline
  • Phenylephrine
  • Phenylpropanolamine
  • Pseudoephedrine
  • Synephrine
  • Tetrahydrozoline

Antagonists

  • Abanoquil
  • Adimolol
  • Ajmalicine
  • Alfuzosin
  • Amosulalol
  • Arotinolol
  • Atiprosin
  • Benoxathian
  • Buflomedil
  • Bunazosin
  • Carvedilol
  • CI-926
  • Corynanthine
  • Dapiprazole
  • DL-017
  • Domesticine
  • Doxazosin
  • Eugenodilol
  • Fenspiride
  • GYKI-12,743
  • GYKI-16,084
  • Indoramin
  • Ketanserin
  • L-765,314
  • Labetalol
  • Mephendioxan
  • Metazosin
  • Monatepil
  • Moxisylyte (thymoxamine)
  • Naftopidil
  • Nantenine
  • Neldazosin
  • Nicergoline
  • Niguldipine
  • Pelanserin
  • Phendioxan
  • Phenoxybenzamine
  • Phentolamine
  • Piperoxan
  • Prazosin
  • Quinazosin
  • Ritanserin
  • RS-97,078
  • SGB-1,534
  • Silodosin
  • SL-89.0591
  • Spiperone
  • Talipexole
  • Tamsulosin
  • Terazosin
  • Tibalosin
  • Tiodazosin
  • Tipentosin
  • Tolazoline
  • Trimazosin
  • Upidosin
  • Urapidil
  • Zolertine

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.

1.2. α2-Adrenergic Receptor Ligands

Agonists

  • Adrenoswitches (photoswitchable agonists)[1]
  • Amitraz
  • Apraclonidine
  • Brimonidine
  • Cannabivarin
  • Clonidine
  • Detomidine
  • Dexmedetomidine
  • Dihydroergotamine
  • Dipivefrine
  • Dopamine
  • Ephedrine
  • Ergotamine
  • Epinephrine (adrenaline)
  • Esproquin
  • Etilefrine
  • Ethylnorepinephrine
  • 6-Fluoronorepinephrine
  • Guanabenz
  • Guanfacine
  • Guanoxabenz
  • Levonordefrin
  • Lofexidine
  • Medetomidine
  • Methyldopa
  • Mivazerol
  • Naphazoline
  • 4-NEMD
  • (R)-3-Nitrobiphenyline
  • Norepinephrine (noradrenaline)
  • Phenylpropanolamine
  • Piperoxan
  • Pseudoephedrine
  • Rilmenidine
  • Romifidine
  • Talipexole
  • Tetrahydrozoline
  • Tizanidine
  • Tolonidine
  • Urapidil
  • Xylazine
  • Xylometazoline

Antagonists

  • Adimolol
  • Aptazapine
  • Atipamezole
  • BRL-44408
  • Buflomedil
  • Cirazoline
  • Efaroxan
  • Esmirtazapine
  • Fenmetozole
  • Fluparoxan
  • GYKI-12,743
  • GYKI-16,084
  • Idazoxan
  • Mianserin
  • Mirtazapine
  • MK-912
  • NAN-190
  • Olanzapine
  • Phentolamine
  • Phenoxybenzamine
  • Piperoxan
  • Piribedil
  • Pyrimidinylpiperazine
  • Rauwolscine
  • Rotigotine
  • SB-269,970
  • Setiptiline
  • Spiroxatrine
  • Sunepitron
  • Tolazoline
  • Yohimbine

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

1.3. β-Adrenergic Receptor Ligands

Agonists

Salbutamol
  • Abediterol
  • Amibegron
  • Arbutamine
  • Arformoterol
  • Arotinolol
  • Bambuterol
  • Befunolol
  • Bitolterol
  • Bromoacetylalprenololmenthane (BAAM)
  • Broxaterol
  • Buphenine
  • Carbuterol
  • Cimaterol
  • Clenbuterol
  • Denopamine
  • Deterenol
  • Dipivefrine
  • Dobutamine
  • Dopamine
  • Dopexamine
  • Ephedrine
  • Epinephrine (adrenaline)
  • Etafedrine
  • Etilefrine
  • Ethylnorepinephrine
  • Fenoterol
  • 2-Fluoronorepinephrine
  • 5-Fluoronorepinephrine
  • Formoterol
  • Hexoprenaline
  • Higenamine
  • Indacaterol
  • Isoetarine
  • Isoprenaline (isoproterenol)
  • N-Isopropyloctopamine
  • Isoxsuprine
  • Labetalol
  • Levonordefrin
  • Levosalbutamol
  • Mabuterol
  • Methoxyphenamine
  • Methyldopa
  • Norepinephrine (noradrenaline)
  • Orciprenaline
  • Oxyfedrine
  • Phenylpropanolamine
  • Pirbuterol
  • Prenalterol
  • Ractopamine
  • Procaterol
  • Pseudoephedrine
  • Quinterenol
  • Reproterol
  • Rimiterol
  • Ritodrine
  • Salbutamol (albuterol)
  • Salmeterol
  • Solabegron
  • Terbutaline
  • Tretoquinol
  • Tulobuterol
  • 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
  • Esmolol
  • Eugenodilol
  • Exaprolol
  • Falintolol
  • Flestolol
  • Flusoxolol
  • Hydroxycarteolol
  • Hydroxytertatolol
  • ICI-118,551
  • Idropranolol
  • Indenolol
  • Indopanolol
  • Iodocyanopindolol
  • Iprocrolol
  • Isoxaprolol
  • Isamoltane
  • Labetalol
  • Landiolol
  • Levobetaxolol
  • Levobunolol
  • Levocicloprolol
  • Levomoprolol
  • Medroxalol
  • Mepindolol
  • Metalol
  • Metipranolol
  • Metoprolol
  • Moprolol
  • Nadolol
  • Nadoxolol
  • Nafetolol
  • Nebivolol
  • Neraminol
  • Nifenalol
  • Nipradilol
  • Oberadilol
  • Oxprenolol
  • Pacrinolol
  • Pafenolol
  • Pamatolol
  • Pargolol
  • Parodilol
  • Penbutolol
  • Penirolol
  • PhQA-33
  • Pindolol
  • Pirepolol
  • Practolol
  • Primidolol
  • Procinolol
  • Pronethalol
  • Propafenone
  • Propranolol
  • Ridazolol
  • Ronactolol
  • Soquinolol
  • Sotalol
  • Spirendolol
  • SR 59230A
  • Sulfinalol
  • TA-2005
  • Talinolol
  • Tazolol
  • Teoprolol
  • Tertatolol
  • Tienoxolol
  • Tilisolol
  • Timolol
  • Tiprenolol
  • Tolamolol
  • Toliprolol
  • Tribendilol
  • Trigevolol
  • Xibenolol
  • Xipranolol

2. Reuptake Inhibitors

2.1. Norepinephrine Transporter (NET) Inhibitors

Reboxetine
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

2.2. Vesicular Monoamine Transporter (VMAT) Inhibitors

  • Ibogaine
  • Reserpine
  • Tetrabenazine
  • Bietaserpine

3. Releasing Agents

Aminorex
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-CAB
4-FA
4-FMA
4-MA
4-MMA
Alfetamine
Amfecloral
Amfepentorex
Amfepramone
Amphetamine
  • dextroamphetamine
  • levoamphetamine
Amphetaminil
β-Me-PEA
BDB
Benzphetamine
BOH
Buphedrone
Butylone
Cathine
Cathinone
Clobenzorex
Clortermine
D-Deprenyl
Dimethylamphetamine
Dimethylcathinone (dimethylpropion, metamfepramone)
DMA
DMMA
EBDB
Ephedrine
Ethcathinone
Ethylamphetamine
Ethylone
Famprofazone
Fenethylline
Fenproporex
Flephedrone
Fludorex
Furfenorex
Hordenine
IAP
IMP
Lisdexamfetamine
Lophophine
MBDB
MDA (tenamfetamine)
MDEA
MDMA
MDMPEA
MDOH
MDPEA
Mefenorex
Mephedrone
Mephentermine
Methamphetamine
  • dextromethamphetamine
  • levomethamphetamine
Methcathinone
Methedrone
Methylone
NAP
Ortetamine
Paredrine
pBA
pCA
Pentorex (phenpentermine)
Phenethylamine
Pholedrine
Phenpromethamine
Phentermine
Phenylpropanolamine
pIA
Prenylamine
Propylamphetamine
Pseudoephedrine
Selegiline (L-deprenyl)
Tiflorex
Tyramine
Xylopropamine
Zylofuramine
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-Aminoindane
2-Aminotetralin
2-Benzylpiperidine
4-Benzylpiperidine
Clofenciclan
Cyclopentamine
Cypenamine
Cyprodenate
Feprosidnine
Gilutensin
Heptaminol
Hexacyclonate
Indanorex
5-Iodo-2-aminoindane (5-IAI)
Isometheptene
Methylhexanamine
Octodrine
Phthalimidopropiophenone
Propylhexedrine
  • levopropylhexedrine
Tuaminoheptane

4. Enzyme Inhibitors

4.1. Anabolism

Phenylalanine hydroxylase (PAH) inhibitors

  • 3,4-Dihydroxystyrene

Tyrosine hydroxylase inhibitors

  • 3-Iodotyrosine
  • Aquayamycin
  • Bulbocapnine
  • Metirosine
  • Oudenone

Aromatic L-amino acid decarboxylase (AAAD) inhibitors

  • Benserazide
  • Carbidopa
  • Genistein
  • Methyldopa

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

4.2. Catabolism

Monoamine oxidase (MAO) inhibitors

Selegiline
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
Amiflamine
Bazinaprine
Befloxatone
Befol
Brofaromine
Cimoxatone
Clorgiline
Esuprone
Harmala alkaloids
  • harmine
  • harmaline
  • tetrahydroharmine
  • harman
  • norharman
  • etc.
Methylene Blue
Metralindole
Minaprine
Moclobemide
Pirlindole
Sercloremine
Tetrindole
Toloxatone
Tyrima
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

  • Entacapone
  • Tolcapone

5. Others

5.1. Precursors

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

5.2. 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+)

5.3. Activity Enhancers

  • Benzofuranylpropylaminopentane (BPAP)
  • Phenylpropylaminopentane (PPAP)

5.4. Release Blockers

  • Bethanidine
  • Bretylium
  • Guanadrel
  • Guanazodine
  • Guanclofine
  • Guanethidine
  • Guanoxan

5.5. Toxins

  • Oxidopamine (6-hydroxydopamine)

The content is sourced from: https://handwiki.org/wiki/Chemistry:List_of_adrenergic_drugs

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