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.

8 Item(s)

per page
Axon ID Name Description From price
3456 Carvedilol β- and α1 adrenoceptor antagonist €50.00
1750 MIBG hemisulfate Radiopharmaceutical; Noradrenaline analogue €115.00
1296 Modafinil α1 adrenoceptor agonist €55.00
3510 Phentolamine mesylate Orally active α1- and α2 adrenoceptor antagonist €50.00
2040 Prazosin hydrochloride Peripherally acting α1 adrenoceptor antagonist €50.00
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

8 Item(s)

per page
Please wait...