DREADD Agonist 21

Modify Date: 2024-01-06 17:25:54

DREADD Agonist 21 Structure
DREADD Agonist 21 structure
Common Name DREADD Agonist 21
CAS Number 56296-18-5 Molecular Weight 278.352
Density 1.3±0.1 g/cm3 Boiling Point 470.1±55.0 °C at 760 mmHg
Molecular Formula C17H18N4 Melting Point N/A
MSDS N/A Flash Point 238.1±31.5 °C

 Use of DREADD Agonist 21


DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist(EC50=1.7 nM).

 Names

Name 11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Synonym More Synonyms

 DREADD Agonist 21 Biological Activity

Description DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist(EC50=1.7 nM).
Related Catalog
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.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 470.1±55.0 °C at 760 mmHg
Molecular Formula C17H18N4
Molecular Weight 278.352
Flash Point 238.1±31.5 °C
Exact Mass 278.153137
LogP 0.98
Vapour Pressure 0.0±1.2 mmHg at 25°C
Index of Refraction 1.699
Storage condition 2-8℃

 Synonyms

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