Description
In addition to being inactive at hM3, DREADD agonist 21, a potent full agonist of hM3Dq (EC50: 1.7nM), is only 3.5-fold selective for hM3Dq over H1, 40-fold selective over 5HT2A, 100-fold selective over 5HT2C, and 165-fold selective over alpha1A. DREADD agonist 21 shows high binding affinities to 5HT2A and 5HT2C serotonin receptor, alpha1A adrenergic receptor, and H1 histamine receptor (Kis: 66, 170, 280, and 6nM) [1]. DREADD agonist 21 potently activates hM1Dq, hM3Dq, and hM4Di. DREADD agonist 21 binds to hM1, hM4, hM1Dq, and hM4Di receptors (pKis: 5.97, 5.44, 7.20, and 6.75). DREADD agonist 21 potently activates hM3Dq in Chinese hamster ovary (CHO) cells transfected cells in vitro with a pEC50 of 8.48+/-0.05. DREADD agonist 21 is a highly selective and potent agonist for muscarinic DREADDs (pEC50 for hM1Dq=6.54 and that for hM4Di=7.77 in pERK assays) [2]