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| Clinical data | |
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| Drug class | Trace amine-associated receptor 1 (TAAR1)agonist |
| Identifiers | |
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| Chemical and physical data | |
| Formula | C16H15ClN4 |
| Molar mass | 298.77 g·mol−1 |
| 3D model (JSmol) | |
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LK00764 is atrace amine-associated receptor 1 (TAAR1)agonist that is being investigated for the treatment ofschizophrenia and otherpsychiatric disorders.[1][2][3][4]
The drug is a highlypotentfull agonist of the human TAAR1 with anEC50Tooltip half-maximal effective concentration of 4.0 nM and anEmaxTooltip half-maximal effective concentration of 101%.[3] It is 30-fold more potent as a TAAR1 agonist thanulotaront (SEP-363856)in vitro.[3] The drug has been found to reverse thehyperlocomotion indopamine transporter (DAT)knockout mice and the hyperactivity induced by theNMDA receptor antagonistdizocilpine (MK-801) in rats, which are considered to beantipsychotic-like effects.[2][4] It also attenuatesstress-inducedhyperthermia in rats, which is thought to be ananxiolytic-like effect.[3] Hence, LK00764 appears to not only be an agonist of the human TAAR1, but also of the mouse and rat TAAR1, although this does not seem to have been assessedin vitro.[2][3][4]
LK00764 was first described in thescientific literature by 2018.[4] It is being developed by Accellena.[1] As of February 2025, the drug is in thepreclinical research stage of development.[1] LK00764 isstructurally distinct from other known TAAR1 agonists but containsβ-phenethylamine-like structural features.[2][3]
This same laboratory discovered yet another TAAR1 agonist (LK00764), also chemically distinct from those currently known. LK00764 was shown to reduce hyperlocomotion in DAT knockout rats, as well as reduce MK-801-induce hyperactivity and spontaneous activity in rats [Citation94]. [...]
The rigidified biphenyl analogs 58—67 appeared to display a much better, full agonistic profile with respect to TAARI. Clearly, the linear p-biphenyl versions 58—65 were preferred over m-biphenyl counterparts 66—67. Simply based on the best potency displayed by compound 62 (LK00764) (its potency (EC5() 4 nM) being more than 30 times higher than that of Ulotaront (EC50 140 nM) [31], which received FDA Breakthrough Therapy Designation and is currently being investigated in Phase 3 clinical trials [9], it was nominated for further evaluation in rodent pharmacological tests sensitive to TAARI agonists [ and relevant to the development of novel antipsychotics.
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