Adrenoceptor α1

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
1503 Asenapine maleate Atypical antipsychotic €75.00
2335 Brexpiprazole dihydrochloride Drug candidate with high affinity for 5-HT1A, 5-HT2A, D2L, α1B, and α2C-adrenergic receptors €135.00
1146 Clozapine Atypical antipsychotic €45.00
1151 GMC 1-116 Clozapine analogue €135.00
1148 GMC 1-169 Atypical antipsychotic €145.00
1150 GMC 2-83 Atypical antipsychotic €145.00
1149 GMC 61-39 Atypical antipsychotic Inquire
1493 Iloperidone Atypical antipsychotic €85.00
1750 MIBG Radiopharmaceutical; Noradrenaline analogue €115.00
1296 Modafinil α1 adrenoceptor agonist €55.00
2040 Prazosin hydrochloride Peripherally acting α1 adrenoceptor antagonist €50.00
1354 Quetiapine fumarate Atypical antipsychotic €75.00
2579 TAK 259 Selective and orally active α1D adrenoceptor antagonist €95.00
2193 Thioridazine hydrochloride DA and α1 adrenoceptor antagonist; MALT1 inhibitor €50.00
1086 WAY 100635 hydrochloride 5-HT1A antagonist €125.00

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