Alpha-1a adrenergic receptor
|Adrenoceptor alpha 1A|
|RNA expression pattern|
The alpha-1A adrenergic receptor (α1A adrenoreceptor), also known as ADRA1A, formerly known as the alpha-1C adrenergic receptor, is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it.
There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G-proteins. Different subtypes show different patterns of activation. The majority of alpha-1 receptors are directed toward the function of epinephrine, a hormone that has to do with the fight-or-flight response.
This gene encodes the alpha-1A-adrenergic receptor. Alternative splicing of this gene generates four transcript variants, which encode four different isoforms with distinct C-termini but having similar ligand binding properties.
- 6-(5-fluoro-2-pyrimidin-5-yl-phenyl)-6,7-dihydro-5H-pyrrolo[1,2-a]imidazole: EC50 = 1nM, Emax = 65%; good selectivity over α1B, α1D and α2A subtypes
- further partial agonistic imidazole compounds
- Desvenlafaxine, this is a reuptake inhibitor, but, in reality, it effects epinephrine positively, and therefore, simulates the effect of an agonist
- Tamsulosin: for treatment of benign prostatic hyperplasia
- Silodosin: for treatment of benign prostatic hyperplasia
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