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Alpha-1A adrenergic receptor

Protein-coding gene in the species Homo sapiens

Protein-coding gene in the species Homo sapiens

The alpha-1A adrenergic receptor (α1A adrenoreceptor), also known as ADRA1A, formerly known also as the alpha-1C adrenergic receptor, is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it. 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.

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.

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
  • further partial agonistic imidazole compounds
  • A-61603
  • 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
  • Aripiprazole
  • 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.

References

References

  1. Langer SZ. (1998). "Nomenclature and state of the art on alpha1-adrenoceptors". Eur. Urol..
  2. "Entrez Gene: ADRA1A adrenergic, alpha-1A-, receptor".
  3. (April 2009). "6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha(1A) adrenoceptor partial agonists". Bioorg. Med. Chem. Lett..
  4. (April 2009). "Potent and selective alpha(1A) adrenoceptor partial agonists-Novel imidazole frameworks". Bioorg. Med. Chem. Lett..
  5. (December 2008). "Novel 2-imidazoles as potent, selective and CNS penetrant alpha1A adrenoceptor partial agonists". Bioorg. Med. Chem. Lett..
  6. (1995). "A-61603, a potent alpha 1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype". J. Pharmacol. Exp. Ther..
  7. (2013). "α(1A)-Adrenergic regulation of inhibition in the olfactory bulb". J. Physiol..
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