The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.
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Uhlen S, Porter AC, Neubig RR
The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.
J Pharmacol Exp Ther. 1994 Dec;271(3):1558-65.
- PubMed ID
- 7996470 [ View in PubMed]
- Abstract
We have determined the binding affinities of the novel alpha-2 adrenoceptor antagonist radioligand [3H]-MK912 for the cloned human alpha-2A, alpha-2B and alpha-2C adrenoceptors. The KD-values were 1.25 nM, 1.36 nM and 0.086 nM for the alpha-2A, alpha-2B and alpha-2C subtypes, respectively. Thus, the selectivity of [3H]-MK912 for the human alpha-2C adrenoceptor vs. the human alpha-2A and alpha-2B adrenoceptors is 14-fold and 16-fold, respectively. The alpha-2C selectivity, and the very high affinity of [3H]-MK912 for the alpha-2C adrenoceptor subtype (KD = 86 pM) makes this radioligand a promising tool for studying the role of alpha-2C adrenoceptors in the human. A selection of antagonists useful for differentiating between the human alpha-2A, alpha-2B and alpha-2C adrenoceptor subtypes is discussed.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Guanfacine Alpha-2A adrenergic receptor Ki (nM) 50.3 N/A N/A Details Guanfacine Alpha-2B adrenergic receptor Ki (nM) 1020 N/A N/A Details Oxymetazoline Alpha-2A adrenergic receptor Ki (nM) 9.68 N/A N/A Details Oxymetazoline Alpha-2B adrenergic receptor Ki (nM) 2980 N/A N/A Details Oxymetazoline Alpha-2C adrenergic receptor Ki (nM) 185 N/A N/A Details Prazosin Alpha-2A adrenergic receptor Ki (nM) 2250 N/A N/A Details Prazosin Alpha-2B adrenergic receptor Ki (nM) 116 N/A N/A Details Yohimbine Alpha-2A adrenergic receptor Ki (nM) 3.76 N/A N/A Details Yohimbine Alpha-2A adrenergic receptor Ki (nM) 3.71 N/A N/A Details Yohimbine Alpha-2B adrenergic receptor Ki (nM) 4.59 N/A N/A Details Yohimbine Alpha-2B adrenergic receptor Ki (nM) 13.6 N/A N/A Details Yohimbine Alpha-2C adrenergic receptor Ki (nM) 0.78 N/A N/A Details Yohimbine Alpha-2C adrenergic receptor Ki (nM) 3.02 N/A N/A Details