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
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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
DrugTargetPropertyMeasurementpHTemperature (°C)
GuanfacineAlpha-2A adrenergic receptorKi (nM)50.3N/AN/ADetails
GuanfacineAlpha-2B adrenergic receptorKi (nM)1020N/AN/ADetails
OxymetazolineAlpha-2A adrenergic receptorKi (nM)9.68N/AN/ADetails
OxymetazolineAlpha-2B adrenergic receptorKi (nM)2980N/AN/ADetails
OxymetazolineAlpha-2C adrenergic receptorKi (nM)185N/AN/ADetails
PrazosinAlpha-2A adrenergic receptorKi (nM)2250N/AN/ADetails
PrazosinAlpha-2B adrenergic receptorKi (nM)116N/AN/ADetails
YohimbineAlpha-2A adrenergic receptorKi (nM)3.76N/AN/ADetails
YohimbineAlpha-2A adrenergic receptorKi (nM)3.71N/AN/ADetails
YohimbineAlpha-2B adrenergic receptorKi (nM)4.59N/AN/ADetails
YohimbineAlpha-2B adrenergic receptorKi (nM)13.6N/AN/ADetails
YohimbineAlpha-2C adrenergic receptorKi (nM)0.78N/AN/ADetails
YohimbineAlpha-2C adrenergic receptorKi (nM)3.02N/AN/ADetails