Alpha-1A adrenergic receptor

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Adrenoceptor alpha 1A
Identifiers
Symbols ADRA1A ; ADRA1C; ADRA1L1; ALPHA1AAR
External IDs OMIM104221 MGI104773 HomoloGene68078 IUPHAR: α1A-adrenoceptor ChEMBL: 229 GeneCards: ADRA1A Gene
RNA expression pattern
PBB GE ADRA1A 211492 s at tn.png
PBB GE ADRA1A 211490 at tn.png
PBB GE ADRA1A 211491 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 148 11549
Ensembl ENSG00000120907 ENSMUSG00000045875
UniProt P35348 P97718
RefSeq (mRNA) NM_000680 NM_001271759
RefSeq (protein) NP_000671 NP_001258688
Location (UCSC) Chr 8:
26.61 – 26.72 Mb
Chr 14:
66.64 – 66.73 Mb
PubMed search [1] [2]

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]

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. 

External links[edit]

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

Further reading[edit]