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: 148
RNA expression pattern
PBB GE ADRA1A 211490 at tn.png

PBB GE ADRA1A 211491 at tn.png

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

NM_001271759
NM_001271760
NM_001271761
NM_013461

RefSeq (protein)

NP_000671.2
NP_150645.2
NP_150646.3
NP_150647.2

NP_001258689.1
NP_038489.2

Location (UCSC) Chr 8: 26.75 – 26.87 Mb Chr 14: 66.64 – 66.73 Mb
PubMed search [1] [2]
Wikidata
View/Edit Human View/Edit Mouse

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[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.[2]

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[3]
  • further partial agonistic imidazole compounds[4][5]
  • A-61603[6]

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.[7]

See also[edit]

References[edit]

  1. ^ 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. 
  2. ^ a b "Entrez Gene: ADRA1A adrenergic, alpha-1A-, receptor". 
  3. ^ 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. 
  4. ^ 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. 
  5. ^ 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. 
  6. ^ 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. 
  7. ^ 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 3624843. PMID 23266935. 

External links[edit]

  • 1A-adrenoceptor". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 

Further reading[edit]