5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-1-fluoro-
- Product Name
- 5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-1-fluoro-
- CAS No.
- 2369979-67-7
- Chemical Name
- 5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-1-fluoro-
- Synonyms
- JHU37152, 10 mM in DMSO;8-Chloro-11-(4-ethylpiperazin-1-yl)-1-fluoro-5H-dibenzo[b,e][1,4]diazepine;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-;JHU37152,inhibit,hM3Dq,Clozapine,Inhibitor,DREADD,Muscarinic acetylcholine receptor,mAChR,hM4Di,JHU-37152
- CBNumber
- CB78236806
- Molecular Formula
- C19H20ClFN4
- Formula Weight
- 358.84
- MOL File
- 2369979-67-7.mol
5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-1-fluoro- Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P501Dispose of contents/container to..…
5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-1-fluoro- Chemical Properties,Usage,Production
Uses
JHU37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5nM and 0.5nM 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
5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-1-fluoro- Preparation Products And Raw materials
Raw materials
Preparation Products
5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-1-fluoro- Suppliers
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