| Identification | Back Directory | [Name]
5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-1-fluoro- | [CAS]
2369979-67-7 | [Synonyms]
8-chloro-11-(4-ethyl-1-piperazinyl)-1-fluoro-5H-Dibenzo[b,e][1,4]diazepine
5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-1-fluoro- | [Molecular Formula]
C19H20ClFN4 | [MDL Number]
MFCD34167518 | [MOL File]
2369979-67-7.mol | [Molecular Weight]
358.84 |
| Chemical Properties | Back Directory | [Boiling point ]
492.6±55.0 °C(Predicted) | [density ]
1.34±0.1 g/cm3(Predicted) | [storage temp. ]
Store at RT | [solubility ]
DMSO|35.88|100|ethanol|35.88|100| | [form ]
solid | [pka]
7.63±0.10(Predicted) | [color ]
Yellow |
| Hazard Information | Back Directory | [Uses]
JHU37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5?nM and 0.5?nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue[1]. | [in vivo]
JHU37152 (0.1 mg/kg; i.p.) exhibits high DREADD occupancy in mice and rats[1].
JHU37152 (0.01-1 mg/kg; i.p.) selectively inhibits locomotor activity in D1-hM3Dq and D1-hM4Di mice without any significant locomotor effects observed in WT mice[1]. | [IC 50]
mAChR3; mAChR4 | [storage]
Room temperature | [References]
[1] Bonaventura J, et, al. High-potency ligands for DREADD imaging and activation in rodents and monkeys. Nat Commun. 2019 Oct 11;10(1):4627. DOI:10.1038/s41467-019-12236-z |
|
|