JHU37152

• CAT Number: I029781
• CAS Number: 2369979-67-7
• Molecular Formula: C19H20ClFN4
• Molecular Weight: 358.84
• Purity: ≥95%
• Synonyms: 3-chloro-6-(4-ethylpiperazin-1-yl)-7-fluoro-11H-benzo[b][1,4]benzodiazepine
• InChI: InChI=1S/C19H20ClFN4/c1-2-24-8-10-25(11-9-24)19-18-14(21)4-3-5-16(18)22-15-7-6-13(20)12-17(15)23-19/h3-7,12,22H,2,8-11H2,1H3
• InChIKey: NZMZJNNWMSYDNX-UHFFFAOYSA-N
• SMILES: CCN1CCN(CC1)C2=NC3=C(C=CC(=C3)Cl)NC4=C2C(=CC=C4)F

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].
JHU37152 displays high DREADD affinity, with Kis of 1.8 nM and 8.7 nM for hM3Dq and hM4Di expressed in mouse brain sections[1].
JHU37152 (1-1000 nM) selectively displaces [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites[1].
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].

Reference

[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.
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