Alpha-1A adrenergic receptor

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ADRA1A
Identifiers
Aliases ADRA1A, ADRA1C, ADRA1L1, ALPHA1AAR, adrenoceptor alpha 1A
External IDs MGI: 104773 HomoloGene: 68078 GeneCards: ADRA1A
Targeted by Drug
epinephrine, methoxamine, norepinephrine, oxymetazoline, phenylephrine, diazepam, alfuzosin, bmy-7378 free base, cabergoline, clozapine, cyproheptadine, doxazosin, indoramin, ketanserin, lisuride, mianserin, NAN 190, phentolamine, piribedil, risperidone, ritanserin, roxindole, silodosin, spiperone, spiroxatrine, tamsulosin, terazosin, terguride, WB-4101, prazosin[1]
RNA expression pattern
PBB GE ADRA1A 211490 at fs.png

PBB GE ADRA1A 211491 at fs.png

PBB GE ADRA1A 211492 s at fs.png
More reference expression data
Orthologs
Species Human Mouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_001271759
NM_001271760
NM_001271761
NM_013461

RefSeq (protein)
Location (UCSC) Chr 8: 26.75 – 26.87 Mb Chr 14: 66.64 – 66.73 Mb
PubMed search [2] [3]
Wikidata
View/Edit Human View/Edit Mouse

The alpha-1A adrenergic receptor1A adrenoreceptor), also known as ADRA1A, formerly known also as the alpha-1C adrenergic receptor,[4] is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it.[5] 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[edit]

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[edit]

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.[5]

Ligands[edit]

Agonists[edit]

  • 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[6]
  • further partial agonistic imidazole compounds[7][8]
  • A-61603[9]

Antagonists[edit]

Role in neural circuits[edit]

α1A-adrenergic receptor subtypes increase inhibition at dendrodendritic synapses, suggesting a synaptic mechanism for noradrenergic modulation of olfactory driven behaviors.[10]

See also[edit]

References[edit]

  1. ^ "Drugs that physically interact with Adrenoceptor alpha 1A view/edit references on wikidata". 
  2. ^ "Human PubMed Reference:". 
  3. ^ "Mouse PubMed Reference:". 
  4. ^ Langer SZ (1998). "Nomenclature and state of the art on alpha1-adrenoceptors". Eur. Urol. 33 Suppl 2: 2–6. doi:10.1159/000052227. PMID 9556189. 
  5. ^ a b "Entrez Gene: ADRA1A adrenergic, alpha-1A-, receptor". 
  6. ^ Roberts LR, Fish PV, Ian Storer R, Whitlock GA (April 2009). "6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha(1A) adrenoceptor partial agonists". Bioorg. Med. Chem. Lett. 19 (11): 3113–7. doi:10.1016/j.bmcl.2009.03.166. PMID 19414260. 
  7. ^ Whitlock GA, Brennan PE, Roberts LR, Stobie A (April 2009). "Potent and selective alpha(1A) adrenoceptor partial agonists-Novel imidazole frameworks". Bioorg. Med. Chem. Lett. 19 (11): 3118–21. doi:10.1016/j.bmcl.2009.03.162. PMID 19394220. 
  8. ^ Roberts LR, Bryans J, Conlon K, McMurray G, Stobie A, Whitlock GA (December 2008). "Novel 2-imidazoles as potent, selective and CNS penetrant alpha1A adrenoceptor partial agonists". Bioorg. Med. Chem. Lett. 18 (24): 6437–40. doi:10.1016/j.bmcl.2008.10.066. PMID 18980842. 
  9. ^ Knepper SM, Buckner SA, Brune ME, DeBernardis JF, Meyer MD, Hancock AA (1995). "A-61603, a potent alpha 1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype". J. Pharmacol. Exp. Ther. 274 (1): 97–103. PMID 7616455. 
  10. ^ Zimnik NC, Treadway T, Smith RS, Araneda RC (2013). "α(1A)-Adrenergic regulation of inhibition in the olfactory bulb". J. Physiol. (Lond.). 591 (Pt 7): 1631–43. doi:10.1113/jphysiol.2012.248591. PMC 3624843Freely accessible. PMID 23266935. 

External links[edit]

Further reading[edit]