Adrenaline, (Nor-)

The classification of alpha and beta subtypes of the adrenergic receptor results from the diverse responses towards adrenergic stimulation. Epinephrine and norepinephrine are the primary adrenergic neurotransmitters. The receptors are part of the super family of metabotropic G-protein coupled receptors (GPCR-A17), and are often referred to as being responsible for the ‘flight or fight response’. Activation of the alpha subtype generally results in vasoconstriction, whereas activation of the beta  subtype leads to vasodilatation.  While beta blockers  are generally  known for their management of  cardiac arrhythmias, cardioprotection after myocardial infarction (heart attack), angina and hypertension (e.g. Axon 1159 (Celiprolol hydrochloride), and Axon 1518 (Timolol maleate))[1], in contrast, drugs interacting at the alpha adrenergic receptors are often used for a variety of medical disorders; e.g. for the treatment of hemorrhagic shock (Axon 1154, B-HT 933 dihydrochloride)[2], as an antidepressant, antidiabetic, or to prevent central neurodegenerative disorders (e.g. Axon 1155, Efaroxan hydrochloride)[3], or for the treatment of narcolepsy and sleep disorders (e.g. Axon 1296, Modafinil)[4].

(Nor-) Adrenergic receptor subtypes listed: Adrenoceptor α1Adrenoceptor α2Adrenoceptor β1Adrenoceptor β2Adrenoceptor β3

 


[1] G-Protein-coupled receptors: Better beta-blockers. J. Owens. Nature Reviews Drug Discovery 2005, 4, 371.
[2] Pressor effects of the alpha 2-adrenoceptor agonist B-HT 933 in anaesthetized and haemorrhagic rats: comparison with the haemodynamic effects of amidephrine. M. R. MacLean, M. Thomson, C. R. Hiley. Br J Pharmacol. 1989, 97, 419-432.
[3] Use of efaroxan and derivatives thereof for the treatment of Alzheimer's disease. F. Colpaert et al.US patent US4855385, 1989.
[4] Randomized trial of modafinil as a treatment for the excessive daytime somnolence in narcolepsy.  Becker PM, et al. Neurology 2000, 54, 1166-1175.

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Axon ID Name Description From price
3488 (±)-CGP-12177A β1/β2 adrenoceptor antagonist, β3 adrenoceptor agonist €120.00
1503 Asenapine maleate Atypical antipsychotic €70.00
1371 Atipamezole hydrochloride α2 adrenoceptor antagonist €95.00
1153 B-HT 920 dihydrochloride D2 agonist, α2 adrenoceptor agonist; 5-HT3 antagonist €75.00
1154 B-HT 933 dihydrochloride α2 adrenoceptor agonist €115.00
1337 B-HT 958 dihydrochloride D2 agonist; α2 adrenoceptor agonist €95.00
3458 Bisoprolol fumarate Potent and cardioselective β1 antagonist €50.00
2335 Brexpiprazole dihydrochloride Drug candidate with high affinity for 5-HT1A, 5-HT2A, D2L, α1B, and α2C-adrenergic receptors €135.00
1555 Brimonidine tartrate α2 adrenoceptor agonist €70.00
1157 Bromobuterol β2 agonist €85.00
3456 Carvedilol β- and α1 adrenoceptor antagonist €50.00
1159 Celiprolol hydrochloride β1 antagonist €135.00
3044 Clonidine hydrochloride α2 adrenoceptor agonist €60.00
1146 Clozapine Atypical antipsychotic €45.00
1087 Desmethyl-WAY 100635 trihydrochloride Building Block for labelled 5-HT1A antagonist €145.00
3065 Dexmedetomidine hydrochloride Selective α2 adrenoceptor agonist €75.00
3665 Droxidopa Brain-penetrant norepinephrine prodrug  Recently added €90.00
1155 Efaroxan hydrochloride α2 adrenoceptor antagonist €65.00
1148 GMC 1-169 Atypical antipsychotic €145.00
1150 GMC 2-83 Atypical antipsychotic €145.00
1149 GMC 61-39 Atypical antipsychotic Inquire
3383 Guanfacine hydrochloride Selective α2 adrenoceptor agonist €50.00
1493 Iloperidone Atypical antipsychotic €85.00
3066 Medetomidine hydrochloride Potent and selective α2 adrenoceptor agonist €70.00
1750 MIBG hemisulfate Radiopharmaceutical; Noradrenaline analogue €115.00
2414 Mirabegron Highly selective and orally active agonist of the human β3-adrenoceptor €120.00
1138 Mirtazapine 5-HT antidepressant €65.00
1296 Modafinil α1 adrenoceptor agonist €55.00
3643 Phenoxybenzamine hydrochloride Selective α1/α2-adrenoceptor antagonist; Calmodulin inhibitor  Recently added €50.00
3510 Phentolamine mesylate Orally active α1- and α2 adrenoceptor antagonist €50.00

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