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).

Epinephrine

Receptor ligands edit

α₁-adrenergic receptor ligands edit

Agonists edit

Antagonists edit

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 edit

Agonists edit

Antagonists edit

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

β-adrenergic receptor ligands edit

Agonists edit

Antagonists edit

Reuptake inhibitors edit

Norepinephrine transporter (NET) inhibitors edit

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 edit

Releasing agents edit

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 edit

Anabolism edit

Phenylalanine hydroxylase (PAH) inhibitors edit

3,4-Dihydroxystyrene

Tyrosine hydroxylase inhibitors edit

Aromatic L-amino acid decarboxylase (AAAD) inhibitors edit

Dopamine-beta-hydroxylase (DBH) inhibitors edit

Phenylethanolamine N-methyltransferase (PNMT) inhibitors edit

Catabolism edit

Monoamine oxidase (MAO) inhibitors edit

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 edit

Others edit

Precursors edit

L-Phenylalanine

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

Cofactors edit

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 edit

Benzofuranylpropylaminopentane (BPAP)
Phenylpropylaminopentane (PPAP)

Release blockers edit

Toxins edit

Oxidopamine (6-hydroxydopamine)

References edit

^ 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.

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