Samiksha Jaiswal (Editor)

Alpha 1A adrenergic receptor

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Species
  
Entrez
  
148

Human
  
Ensembl
  
ENSG00000120907

Alpha-1A adrenergic receptor

Aliases
  
ADRA1A, ADRA1C, ADRA1L1, ALPHA1AAR, adrenoceptor alpha 1A

External IDs
  
MGI: 104773 HomoloGene: 68078 GeneCards: ADRA1A

The alpha-1A adrenergic receptor1A 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.

Contents

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.

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
  • Antagonists

  • Tamsulosin: for treatment of benign prostatic hyperplasia
  • Silodosin: for treatment of benign prostatic hyperplasia
  • Risperidone
  • WB-4101
  • Ziprasidone
  • 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

    Alpha-1A adrenergic receptor Wikipedia


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