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 α1, Adrenoceptor α2, Adrenoceptor β1, Adrenoceptor β2, Adrenoceptor 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.
Axon ID | Name | Description | From price | |
---|---|---|---|---|
1503 | Asenapine maleate | Atypical antipsychotic | €70.00 | |
2335 | Brexpiprazole dihydrochloride | Drug candidate with high affinity for 5-HT1A, 5-HT2A, D2L, α1B, and α2C-adrenergic receptors | €135.00 | |
3456 | Carvedilol | β- and α1 adrenoceptor antagonist | €50.00 | |
1146 | Clozapine | Atypical antipsychotic | €50.00 | |
1087 | Desmethyl-WAY 100635 trihydrochloride | Building Block for labelled 5-HT1A antagonist | €145.00 | |
1148 | GMC 1-169 | Atypical antipsychotic | €150.00 | |
1150 | GMC 2-83 | Atypical antipsychotic | €150.00 | |
1149 | GMC 61-39 | Atypical antipsychotic | Inquire | |
1493 | Iloperidone | Atypical antipsychotic | €85.00 | |
1750 | MIBG hemisulfate | Radiopharmaceutical; Noradrenaline analogue | €115.00 | |
1296 | Modafinil | α1 adrenoceptor agonist | €60.00 | |
3643 | Phenoxybenzamine hydrochloride | Selective α1/α2-adrenoceptor antagonist; Calmodulin inhibitor | €50.00 | |
3510 | Phentolamine mesylate | Orally active α1- and α2 adrenoceptor antagonist | €50.00 | |
2040 | Prazosin hydrochloride | Peripherally acting α1 adrenoceptor antagonist | €50.00 | |
1354 | Quetiapine fumarate | Atypical antipsychotic | €75.00 | |
3112 | Silodosin | Selective α1A adrenoceptor antagonist | €60.00 | |
2579 | TAK 259 | Selective and orally active α1D adrenoceptor antagonist | €95.00 | |
3512 | Terazosin hydrochloride | Selective, orally active α1 adrenoceptor antagonist | €60.00 | |
2193 | Thioridazine hydrochloride | DA and α1 adrenoceptor antagonist; MALT1 inhibitor | €50.00 | |
1086 | WAY 100635 hydrochloride | 5-HT1A antagonist | €125.00 | |
2424 | WAY 100635 maleate | 5-HT1A antagonist with D4 agonistic properties | €125.00 |