DREADD agonist 21

56296-18-5

C17H18N4

DMSO : >= 78 mg/mL (280.22 mM)

Neuronal Signaling; GPCR/G Protein

DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist(EC₅₀=1.7 nM). IC50 & Target: EC50: 1.7 nM (hM3Dq)^[1]
Ki: 6 nM (H1 histamine receptor), 66 nM (5HT2A serotonin receptor 5HT2A), 170 nM (5HT2C serotonin receptor), 280 nM (alpha1A adrenergic receptor)^[1] In Vitro: DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC₅₀=1.7 nM) and does not activate human M3 receptor (hM3). In addition to being inactive at hM3, DREADD agonist 21, a potent full agonist of hM3Dq (EC₅₀=1.7 nM), 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 with K_i values of 66, 170, 280, and 6 nM, respectively^[1].