High affinity and highly potent activator of hM3Dq and hM4Di DREADDs (Ki values are 1.8 nM and 8.7 nM for hM3Dq and hM4Di in vitro, respectively; EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in vitro, respectively). Selectively displaces [3H]clozapine from DREADDs in vivo, but not from other clozapine binding sites. Inhibits locomotor activity in mice expressing hM3Dq and hM4Di in D1-expressing neurons. Brain penetrant in mice, rats and non-human primates.
CAS Number: 2369979-67-7
Molecular Weight: 358.84
Chemical Name: 8-Chloro-11-(4-ethylpiperazin-1-yl)-1-fluoro-5H-dibenzo[b,e][1,4]diazepine InChI Key NZMZJNNWMSYDNX-UHFFFAOYSA-N Smiles CCN1CCN(C2=NC3=CC(Cl)=CC=C3NC4=CC=CC(F)=C24)CC1 References
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
- Bonaventura et al (2019) High-potency ligands for DREADD imaging and activation in rodents and monkeys. Nat.Commun. 10 4627 PMID: 31604917
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