Alpha-1A adrenergic receptor: Difference between revisions
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* 6-(5-fluoro-2-pyrimidin-5-yl-phenyl)-6,7-dihydro-5H-pyrrolo[1,2-a]imidazole: EC<sub>50</sub> = 1nM, E<sub>max</sub> = 65%; good selectivity over α1B, α1D and α2A subtypes<ref name="pmid19414260">{{cite journal |author=Roberts LR, Fish PV, Ian Storer R, Whitlock GA |title=6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha(1A) adrenoceptor partial agonists |journal=Bioorg. Med. Chem. Lett. |volume= 19|issue= 11|pages= 3113–7|date=April 2009 |pmid=19414260 |doi=10.1016/j.bmcl.2009.03.166 |url=}}</ref> |
* 6-(5-fluoro-2-pyrimidin-5-yl-phenyl)-6,7-dihydro-5H-pyrrolo[1,2-a]imidazole: EC<sub>50</sub> = 1nM, E<sub>max</sub> = 65%; good selectivity over α1B, α1D and α2A subtypes<ref name="pmid19414260">{{cite journal |author=Roberts LR, Fish PV, Ian Storer R, Whitlock GA |title=6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha(1A) adrenoceptor partial agonists |journal=Bioorg. Med. Chem. Lett. |volume= 19|issue= 11|pages= 3113–7|date=April 2009 |pmid=19414260 |doi=10.1016/j.bmcl.2009.03.166 |url=}}</ref> |
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* further partial agonistic imidazole compounds<ref name="pmid19394220">{{cite journal |author=Whitlock GA, Brennan PE, Roberts LR, Stobie A |title=Potent and selective alpha(1A) adrenoceptor partial agonists-Novel imidazole frameworks |journal=Bioorg. Med. Chem. Lett. |volume= 19|issue= 11|pages= 3118–21|date=April 2009 |pmid=19394220 |doi=10.1016/j.bmcl.2009.03.162 |url=}}</ref><ref name="pmid18980842">{{cite journal |author=Roberts LR, Bryans J, Conlon K, McMurray G, Stobie A, Whitlock GA |title=Novel 2-imidazoles as potent, selective and CNS penetrant alpha1A adrenoceptor partial agonists |journal=Bioorg. Med. Chem. Lett. |volume=18 |issue=24 |pages=6437–40 |date=December 2008 |pmid=18980842 |doi=10.1016/j.bmcl.2008.10.066 |url=}}</ref> |
* further partial agonistic imidazole compounds<ref name="pmid19394220">{{cite journal |author=Whitlock GA, Brennan PE, Roberts LR, Stobie A |title=Potent and selective alpha(1A) adrenoceptor partial agonists-Novel imidazole frameworks |journal=Bioorg. Med. Chem. Lett. |volume= 19|issue= 11|pages= 3118–21|date=April 2009 |pmid=19394220 |doi=10.1016/j.bmcl.2009.03.162 |url=}}</ref><ref name="pmid18980842">{{cite journal |author=Roberts LR, Bryans J, Conlon K, McMurray G, Stobie A, Whitlock GA |title=Novel 2-imidazoles as potent, selective and CNS penetrant alpha1A adrenoceptor partial agonists |journal=Bioorg. Med. Chem. Lett. |volume=18 |issue=24 |pages=6437–40 |date=December 2008 |pmid=18980842 |doi=10.1016/j.bmcl.2008.10.066 |url=}}</ref> |
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* [[Desvenlafaxine]], this is a reuptake inhibitor, but, in reality, it effects epinephrine positively, and therefore, simulates the effect of an [[agonist]] |
* [[Desvenlafaxine]], this is a reuptake inhibitor, but, in reality, it effects epinephrine positively, and therefore, simulates the effect of an [[agonist]]{{Citation needed|Date=March 2014}} |
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===Antagonists=== |
===Antagonists=== |
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Revision as of 04:06, 14 March 2014
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]
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[citation needed]
Antagonists
- Tamsulosin: for treatment of benign prostatic hyperplasia
- Silodosin: for treatment of benign prostatic hyperplasia
See also
References
- ^ 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.
- ^ Cite error: The named reference
entrezwas invoked but never defined (see the help page). - ^ 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.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ 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.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ 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.
{{cite journal}}: CS1 maint: multiple names: authors list (link)
External links
- "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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