Drug intelligence / Profile preview

LY235959

Development stage
Discontinued
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Intrathecal, Subcutaneous, Intracerebroventricular
01

Overview

**LY235959** is a small molecule competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, specifically blocking the glutamate site of the NMDA receptor. It is highly selective for NMDA over other ionotropic glutamate receptors and has been used in animal models to study pain, neuroprotection, hypothermia, morphine tolerance, and effects on cocaine self-administration[1][3][6][7]. LY235959 demonstrates much higher potency when administered centrally (intrathecal or intracerebroventricular) compared to systemic (subcutaneous) administration[1][3]. In preclinical studies, it prevents hyperalgesia and formalin-induced central sensitization, produces analgesic and neuroprotective effects, causes hypothermia, reduces the development of morphine tolerance, and can alter rewarding properties of cocaine. Development for clinical use (e.g., dementia) has been terminated[4]. The drug's developer is Eli Lilly[4].

Brand names
LY274614LY-274614LY 274614
Other names
(3S,4aR,6S,8aR)-6-(phosphonomethyl)decahydroisoquinoline-3-carboxylic acidDecahydro-6-(phosphonomethyl)-3-isoquinolinecarboxylic acid3-Isoquinolinecarboxylic acid, decahydro-6-(phosphonomethyl)-, (3S,4aR,6S,8aR)-3-Isoquinolinecarboxylicacid, decahydro-6-(phosphonomethyl)-, (3S,4aR,6S,8aR)-[3S-(3A,4AA,6B,8AA)]-decahydro-6-(phosphonomethyl)-3-isoquinolinecarboxylic acid[3S-(3α,4aα,6β,8aα)]-Decahydro-6-(phosphonomethyl)-3-isoquinolinecarboxylic acidUNII-AR2BHC0C6PUNII-AR-2BHC0C6PUNII-AR 2BHC0C6PCAS 137433-06-8CAS137433-06-8CAS-137433-06-8
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)

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