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Alpha-1A adrenergic receptor
Protein-coding gene in the species Homo sapiens From Wikipedia, the free encyclopedia
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The alpha-1A adrenergic receptor (α1A adrenoreceptor), also known as ADRA1A, formerly known also as the alpha-1C adrenergic receptor,[5] is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it.[6] There is no longer a subtype α1C receptor. At one time, there was a subtype known as α1C, but it was found to be identical to the previously discovered α1A receptor subtype. To avoid confusion, the naming convention was continued with the letter D.
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Receptor
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.
Gene
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]
Ligands
Agonists
- 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[7]
- further partial agonistic imidazole compounds[8][9]
- A-61603[10]
- Metaraminol
Antagonists
- Tamsulosin: for treatment of benign prostatic hyperplasia
- Silodosin: for treatment of benign prostatic hyperplasia
- Doxazosin: for treatment of benign prostatic hyperplasia and/or Hypertension
- Risperidone: used to treat schizophrenia and bipolar disorder
- WB-4101
- Ziprasidone
- Nicergoline
- Most tricyclic antidepressants
Role in neural circuits
α1A-adrenergic receptor subtypes increase inhibition at dendrodendritic synapses, suggesting a synaptic mechanism for noradrenergic modulation of olfactory driven behaviors.[11]
See also
References
External links
Further reading
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