Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C11H20NO5P |
| Molecular Weight | 277.254 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC[C@H](CP(O)(O)=O)C[C@]1([H])C[C@H](NC2)C(O)=O
InChI
InChIKey=STIRHCNEGQQBOY-QEYWKRMJSA-N
InChI=1S/C11H20NO5P/c13-11(14)10-4-9-3-7(6-18(15,16)17)1-2-8(9)5-12-10/h7-10,12H,1-6H2,(H,13,14)(H2,15,16,17)/t7-,8-,9+,10-/m0/s1
| Molecular Formula | C11H20NO5P |
| Molecular Weight | 277.254 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/16024734 | https://www.ncbi.nlm.nih.gov/pubmed/1404235
Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/16024734 | https://www.ncbi.nlm.nih.gov/pubmed/1404235
LY235959 is the active isomer of the 6-substituted decahydroisoquinoline-3-carboxylic acid, LY274614. Both LY274614 and LY235959 have demonstrated potent NMDA receptor antagonist activity both in vivo and in-vitro. LY235959 has been shown to attenuate and reverse morphine tolerance as well as, attenuate opioid withdrawal and block c-fos mRNA induction in limbic areas. The attenuation of morphine tolerance occurs through the interaction of LY235959 with the NMDA receptor and not by producing opiate receptor changes. LY235959 is able to block NMDA receptor-induced hyperalgesia, as well as formalin-induced inflammatory pain, in rats. These antinociceptive effects of LY235959 were obtained at doses that did not produce motor impairment. LY235959 does not block the hyperalgesia produced by kainic acid (a non-NMDA glutamate receptor agonist) providing evidence of its selectivity for the NMDA receptor.
CNS Activity
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Levodopa-induced dyskinesias improved by a glutamate antagonist in Parkinsonian monkeys. | 1996 May |
|
| Anticonvulsant efficacy of N-methyl-D-aspartate antagonists against convulsions induced by cocaine. | 1999 May |
|
| Continuous intracerebroventricular infusion of the competitive NMDA receptor antagonist, LY235959, facilitates escalation of cocaine self-administration and increases break point for cocaine in Sprague-Dawley rats. | 2007 Nov |
Patents
Sample Use Guides
Rats were treated i.t. with LY235959 at 0.001 or 0.003 nmol as a single dose.
Rats were treated s.c. with LY235959 at 20 mmol/kg as a single dose.
Route of Administration:
Other
AtT-20 cells were seeded in 24-well plates at initial densities of 5 x 10^4 cells per well and cultured in DMEM medium supplemented with 10% fetal calf serum for 5–7 days. On the day of the experiment, cells were washed twice and replaced with serum-free DMEM containing 0.2% BSA, 25 mM Hepes, and 100 kIU/ml aprotinin (pH 7.4, 37° C). LY235959 was made up in the experimental media at a concentration of 10x. Drug incubations were carried out in 0.5 ml of this solution for 45 min, and the supernatant collected for ACTH determination.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 08:33:13 UTC 2023
by
admin
on
Sat Dec 16 08:33:13 UTC 2023
|
| Record UNII |
AR2BHC0C6P
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
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Common Name | English | ||
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Systematic Name | English |
| Code System | Code | Type | Description | ||
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AR2BHC0C6P
Created by
admin on Sat Dec 16 08:33:13 UTC 2023 , Edited by admin on Sat Dec 16 08:33:13 UTC 2023
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LY-235959
Created by
admin on Sat Dec 16 08:33:13 UTC 2023 , Edited by admin on Sat Dec 16 08:33:13 UTC 2023
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137433-06-8
Created by
admin on Sat Dec 16 08:33:13 UTC 2023 , Edited by admin on Sat Dec 16 08:33:13 UTC 2023
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131938
Created by
admin on Sat Dec 16 08:33:13 UTC 2023 , Edited by admin on Sat Dec 16 08:33:13 UTC 2023
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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ACTIVE MOIETY |
