Adrenergic antagonist

An adrenergic antagonist is a pharmaceutical substance that acts to inhibit the action of catecholamines at the adrenergic receptors. It is thus a type of sympatholytic. Many important and commonly prescribed medications are adrenergic antagonists, including prazosin and propranolol. Like all pharmacological receptor antagonists, adrenergic antagonists only show an effect when the receptor's effector is present.

It has the opposite effect as adrenergic agonists.

More specifically, they can be divided into:

Structure–activity relationship

If the amine on the adrenergic agent has a substituent bigger than a tertiary butyl, then the compound becomes an adrenergic antagonist.^[1]

References

↑ Medicinal Chemistry of Adrenergics and Cholinergics

External links

Adrenergic antagonists at the US National Library of Medicine Medical Subject Headings (MeSH)

Sympatholytic (and closely related) antihypertensives (C02)

Sympatholytics
(antagonize α-adrenergic
vasoconstriction)

Central

α₂ agonist	Clonidine Guanabenz Guanfacine Methyldopa^# Tiamenidine^‡
Adrenergic release inhibitors	Bethanidine Bretylium Debrisoquine Guanadrel Guanazodine Guanethidine Guanoclor Guanazodine Guanoxabenz Guanoxan
Imidazoline receptor agonist	Moxonidine Rilmenidine Tolonidine
Ganglion-blocking/nicotinic antagonist	Hexamethonium^‡ Mecamylamine Pentolinium Trimethaphan

Peripheral

Indirect

MAOI	Pargyline^‡
Adrenergic uptake inhibitor	Bietaserpine Deserpidine Methoserpidine Rescinnamine Reserpine Syrosingopine
Tyrosine hydroxylase inhibitor	Metirosine

Direct

α₁ blockers	Prazosin Indoramin Trimazosin Doxazosin Urapidil
Non-selective α blocker	Phentolamine

Other antagonists

Serotonin antagonist	Ketanserin Lidanserin
Endothelin antagonist (for PH)	dual (Bosentan, Macitentan) selective (Ambrisentan, Sitaxentan)

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

Pharmacomodulation

Types

♦ Enzyme: Inducer
Inhibitor

♦ Ion channel: Opener
Blocker

♦ Miscellaneous: Precursor
Cofactor

Classes

Enzyme

see Enzyme inhibition

Ion channel

Receptor &
transporter

BA/M

Adrenergic	Adrenergic receptor agonist (α β (1 2)) Adrenergic receptor antagonist (α (1 2) β) Norepinephrine reuptake inhibitor (NRI)
Dopaminergic	Dopamine receptor agonist Dopamine receptor antagonist Dopamine reuptake inhibitor (DRI)
Histaminergic	Histamine receptor agonist Histamine receptor antagonist (H₁ H₂ H₃)
Serotonergic	Serotonin receptor agonist Serotonin Receptor Antagonist (5-HT₃) Serotonin reuptake inhibitor (SRI)

GABAergic	GABA receptor agonist GABA receptor antagonist GABA reuptake inhibitor (GRI)
Glutamatergic	Glutamate receptor agonist (AMPA) Glutamate receptor antagonist (NMDA) Glutamate reuptake inhibitor

Cholinergic

Cannabinoidergic

Cannabinoid receptor agonist
Cannabinoid receptor antagonist
Endocannabinoid enhancer (eCBE)
Endocannabinoid reuptake inhibitor (eCBRI)

Opioidergic

Other

Miscellaneous

Cofactor (see Enzyme cofactors)
Precursor (see Amino acids)

Adrenergic receptor modulators

α₁

Agonists: 6-FNE; Amidephrine; Anisodine; Buspirone; Cirazoline; Corbadrine; Desglymidodrine; Dexisometheptene; Dipivefrine; Dopamine; Droxidopa (L-DOPS); Ephedrine; Epinephrine; Etilefrine; Etilevodopa; Ethylnorepinephrine; Indanidine; Isometheptene; L-DOPA (levodopa); L-Phenylalanine; L-Tyrosine; Melevodopa; Metaraminol; Methoxamine; Methyldopa; Midodrine; Naphazoline; Norepinephrine; Octopamine (drug); Oxymetazoline; Phenylephrine; Phenylpropanolamine; Pseudoephedrine; Synephrine; Tetryzoline; Tiamenidine; XP21279; 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

α₂

Agonists: (R)-3-Nitrobiphenyline; 4-NEMD; 6-FNE; Amitraz; Apraclonidine; Brimonidine; Cannabivarin; Clonidine; Corbadrine; Detomidine; Dexmedetomidine; Dihydroergotamine; Dipivefrine; Dopamine; Droxidopa (L-DOPS); Etilevodopa; Ephedrine; Ergotamine; Epinephrine; Etilefrine; Ethylnorepinephrine; Guanabenz; Guanfacine; Guanoxabenz; L-DOPA (levodopa); L-Phenylalanine; L-Tyrosine; Lofexidine; Medetomidine; Melevodopa; Methyldopa; Mivazerol; Naphazoline; Norepinephrine; Oxymetazoline; Phenylpropanolamine; Piperoxan; Pseudoephedrine; Rezatomidine; Rilmenidine; Romifidine; Talipexole; Tetrahydrozoline; Tiamenidine; Tizanidine; Tolonidine; Urapidil; XP21279; 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; Droxidopa (L-DOPS); Ephedrine; Epinephrine; Etafedrine; Etilefrine; Etilevodopa; Ethylnorepinephrine; Fenoterol; Formoterol; Hexoprenaline; Higenamine; Indacaterol; Isoetarine; Isoprenaline; Isoxsuprine; L-DOPA (levodopa); L-Phenylalanine; L-Tyrosine; Levosalbutamol; Mabuterol; Melevodopa; 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; XP21279; 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

See also: Receptor/signaling modulators

Dopaminergics

Serotonergics

Monoamine reuptake inhibitors

Monoamine releasing agents

Monoamine metabolism modulators

Monoamine neurotoxins

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