Preferred Name |
pregabalin |
|
Synonyms |
PD-144723 |
|
Definitions |
A 3-isobutyl derivative of gamma-amino butyric acid (GABA) with anti-convulsant, anti-epileptic, anxiolytic, and analgesic activities. Although the exact mechanism of action is unknown, pregabalin selectively binds to alpha2delta (A2D) subunits of presynaptic voltage-dependent calcium channels (VDCCs) located in the central nervous system (CNS). Binding of pregabalin to VDCC A2D subunits prevents calcium influx and the subsequent calcium-dependent release of various neurotransmitters, including glutamate, norepinephrine, serotonin, dopamine, and substance P, from the presynaptic nerve terminals of hyperexcited neurons; synaptic transmission is inhibited and neuronal excitability is diminished. Pregabalin does not bind directly to GABA-A or GABA-B receptors and does not alter GABA uptake or degradation. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C64625" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C64625" NCI Thesaurus) |
|
ID |
http://purl.bioontology.org/ontology/PDQ/CDR0000518288 |
|
altLabel |
PD-144723 Lyrica CI-1008 3-Isobutyl GABA 3-(aminomethyl)-5-methyl-hexanoic acid |
|
cui |
C1570232 C0657912 C1955823 C0388352 |
|
DATE FIRST PUBLISHED |
2006-11-03 |
|
Date last modified |
2008-04-18 |
|
definition |
A 3-isobutyl derivative of gamma-amino butyric acid (GABA) with anti-convulsant, anti-epileptic, anxiolytic, and analgesic activities. Although the exact mechanism of action is unknown, pregabalin selectively binds to alpha2delta (A2D) subunits of presynaptic voltage-dependent calcium channels (VDCCs) located in the central nervous system (CNS). Binding of pregabalin to VDCC A2D subunits prevents calcium influx and the subsequent calcium-dependent release of various neurotransmitters, including glutamate, norepinephrine, serotonin, dopamine, and substance P, from the presynaptic nerve terminals of hyperexcited neurons; synaptic transmission is inhibited and neuronal excitability is diminished. Pregabalin does not bind directly to GABA-A or GABA-B receptors and does not alter GABA uptake or degradation. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C64625" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C64625" NCI Thesaurus) |
|
LT |
TRD |
|
NCI ID |
C64625 |
|
notation |
CDR0000518288 |
|
ORIG STY |
Drug/agent |
|
prefLabel |
pregabalin |
|
tui |
T109 T116 T121 |