Alpha-1a adrenergic receptor

Adrenoceptor alpha 1A
Identifiers
ADRA1A Gene
RNA expression pattern

The alpha-1A adrenergic receptor1A adrenoreceptor), also known as ADRA1A, formerly known as the alpha-1C adrenergic receptor,[1] is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it.[2]

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.[2]

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[3]
  • further partial agonistic imidazole compounds[4][5]
  • Desvenlafaxine, this is a reuptake inhibitor, but, in reality, it effects epinephrine positively, and therefore, simulates the effect of an agonist

Antagonists

See also

References

External links

Further reading


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