Table 8

Inhibitory potency of the noncompetitive antagonist, SCH-202676, on the orthosteric binding of different Class I GPCRs

ReceptorRadioligandIC50
μm
δ-Opioid[3H]Diprenorphine0.3
κ-Opioid[3H]Diprenorphine1.7
μ-Opioid[3H]Diprenorphine1.8
M1muscarinic[3H]N-methylscopolamine0.4
M2muscarinic[3H]N-methylscopolamine0.4
α2A-Adrenergic[3H]Yohimbine0.5
β1-Adrenergic[125I]Iodocyanopindolol1.2
D1 dopamine[3H]SCH-233900.1
D2dopamine[3H]Methylspiperone0.1
  • Adapted from Fawzi et al., 2001.