| Bioactivity | JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue[1]. | ||||||||||||
| Target | EC50: 18.5 nM (hM3Dq DREADD); 0.2 nM (hM4Di DREADD) | ||||||||||||
| Invitro | JHU37160 displays high DREADD affinity, with Kis of 1.9 nM and 3.6 nM for hM3Dq and hM4Di expressed in mouse brain sections[1].JHU37160 (1-1000 nM) selectively displaces [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites[1]. | ||||||||||||
| In Vivo | JHU37160 (0.1 mg/kg; i.p.) exhibits high DREADD occupancy in mice and rats[1].JHU37160 (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]. | ||||||||||||
| Name | JHU37160 | ||||||||||||
| CAS | 2369979-68-8 | ||||||||||||
| Formula | C19H20ClFN4 | ||||||||||||
| Molar Mass | 358.84 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |