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Alpha-1A adrenergic receptor

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Template:PBB The alpha-1A adrenergic receptor (α1A 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]

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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]

Antagonists

See also

References

  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. ^ Cite error: The named reference entrez was invoked but never defined (see the help page).
  3. ^ Roberts LR, Fish PV, Ian Storer R, Whitlock GA (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  4. ^ Whitlock GA, Brennan PE, Roberts LR, Stobie A (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  5. ^ Roberts LR, Bryans J, Conlon K, McMurray G, Stobie A, Whitlock GA (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  • "α1A-adrenoceptor". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. {{cite web}}: Cite has empty unknown parameter: |coauthors= (help)

Further reading

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