Drug intelligence / Profile preview

JHU37160-dihydrochloride

Development stage
Unknown
Lead developer
National Institute of Mental Health
Modality
Small Molecules
Administration
Intraperitoneal (in Animal Studies), Not For Human Use
01

Overview

JHU37160-dihydrochloride is a **novel, highly potent, water-soluble small molecule agonist for Designer Receptors Exclusively Activated by Designer Drugs (DREADDs)**, specifically targeting human engineered muscarinic acetylcholine receptors hM3Dq and hM4Di. These DREADD systems are widely used in research to control neuronal activity in vivo and in vitro via chemogenetic modulation. - **Mechanism:** JHU37160 acts as a potent agonist at the DREADD variants hM3Dq and hM4Di, activating or inhibiting neuronal circuits depending on the expressed receptor. - **Application:** The compound is utilized in CNS research to manipulate activity in specific neuronal populations. It shows high brain penetrance, high affinity (Ki for hM3Dq: 1.9 nM, for hM4Di: 3.6 nM) and high in vivo DREADD occupancy and has been suggested as an improved alternative to clozapine-N-oxide[1][3][5][4][7]. - **Selectivity:** While potent, its selectivity is described as not entirely ideal; dosing must be optimized to minimize off-target effects[1][5]. - **Developer:** Sold under license from the NIH; patent pending 62/627,527[1][3]. - **Primary indication:** Experimental research; NOT for therapeutic or diagnostic use in humans or animals[1].

Brand names
JHU37160-dihydrochlorideJHU-37160-dihydrochlorideJHU 37160-dihydrochloride
Other names
8-chloro-11-(4-ethylpiperazin-1-yl)-4-fluoro-5H-dibenzo[b,e][1,4]diazepine dihydrochlorideJHU37160 (DREADD ligand)3-chloro-6-(4-ethylpiperazin-1-yl)-10-fluoro-11H-benzo[b][1,4]benzodiazepineJ60 dihydrochlorideJ-60 dihydrochlorideJ 60 dihydrochloride
02

Targets

hM4Di (Human muscarinic acetylcholine receptor M4 designer receptor exclusively activated by designer drugs)hM3Dq (Human muscarinic acetylcholine receptor M3 DREADD)

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