56296-18-5

56296-18-5 structure

Name: DREADD Agonist 21
Chemical Name: 11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
CAS Number: 56296-18-5
Molecular Formula: C₁₇H₁₈N₄
Molecular Weight: 278.352
Catalog: Signaling Pathways GPCR/G Protein mAChR
Create Date: 2018-06-07 01:54:53
Modify Date: 2024-01-06 17:25:54
DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist(EC50=1.7 nM).

Name	11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Synonyms	11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine 5H-Dibenzo[b,e][1,4]diazepine, 11-(1-piperazinyl)- DREADD Agonist 21

Description	DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist(EC50=1.7 nM).
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mAChR Signaling Pathways >> Neuronal Signaling >> mAChR Research Areas >> Neurological Disease
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 (α1A 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 α1A. DREADD agonist 21 shows high binding affinities to 5HT2A and 5HT2C serotonin receptor, α1A adrenergic receptor, and H1 histamine receptor with Ki values of 66, 170, 280, and 6 nM, respectively[1].
References	[1]. Chen X, et al. The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs. ACS Chem Neurosci. 2015 Mar 18;6(3):476-84.