Delving into the Latest Updates on IHCH-7113 with Synapse

Overview

Basic Info

Drug Type

Chemical drugs

Synonyms

Target

5-HT2A receptor

Mechanism

5-HT2A receptor modulators(Serotonin 2a (5-HT2a) receptor modulators)

Therapeutic Areas

Other Diseases

Active Indication

Psychotic Disorders

Inactive Indication-

Originator Organization

Center for Excellence and Innovation in Molecular Cell Science, Chinese Academy of Sciences

Active Organization

Center for Excellence and Innovation in Molecular Cell Science, Chinese Academy of Sciences

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Drugs that target the human serotonin 2A receptor (5-HT 2A R) are used to treat neuropsychiatric diseases; however, many have hallucinogenic effects, hampering their use. Here, we present structures of 5-HT 2A R complexed with the psychedelic drugs psilocin (the active metabolite of psilocybin) and d -lysergic acid diethylamide (LSD), as well as the endogenous neurotransmitter serotonin and the nonhallucinogenic psychedelic analog lisuride. Serotonin and psilocin display a second binding mode in addition to the canonical mode, which enabled the design of the psychedelic IHCH-7113 (a substructure of antipsychotic lumateperone) and several 5-HT 2A R β-arrestin–biased agonists that displayed antidepressant-like activity in mice but without hallucinogenic effects. The 5-HT 2A R complex structures presented herein and the resulting insights provide a solid foundation for the structure-based design of safe and effective nonhallucinogenic psychedelic analogs with therapeutic effects.

100 Deals associated with IHCH-7113

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