Stem definition | Drug id | CAS RN |
---|---|---|
local anaesthetics | 1097 | 36637-18-0 |
None
Property | Value | Reference |
---|---|---|
MRTD (Maximum Recommended Therapeutic Daily Dose) | 24.13 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 0 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Date | Agency | Company | Orphan |
---|---|---|---|
Aug. 30, 1976 | FDA |
None
None
None
None
Source | Code | Description |
---|---|---|
ATC | N01BB07 | NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Amides |
ATC | N01BB57 | NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Amides |
CHEBI has role | CHEBI:36333 | local anesthetics |
MeSH PA | D000777 | Anesthetics |
MeSH PA | D000779 | Anesthetics, Local |
MeSH PA | D002491 | Central Nervous System Agents |
MeSH PA | D002492 | Central Nervous System Depressants |
MeSH PA | D018373 | Peripheral Nervous System Agents |
MeSH PA | D018689 | Sensory System Agents |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Sinus tachycardia | contraindication | 11092001 | |
Myocardial infarction | contraindication | 22298006 | DOID:5844 |
Parkinsonism | contraindication | 32798002 | |
Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
Conduction disorder of the heart | contraindication | 44808001 | |
Cerebral arteriosclerosis | contraindication | 65312002 | |
Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
Cardiogenic shock | contraindication | 89138009 | |
Bleeding | contraindication | 131148009 | |
Angina pectoris | contraindication | 194828000 | |
Primary dilated cardiomyopathy | contraindication | 195021004 | |
Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
Disorder of coronary artery | contraindication | 414024009 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 13.24 | acidic |
pKa2 | 7.84 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Sodium channel protein type 5 subunit alpha | Ion channel | BLOCKER | WOMBAT-PK | CHEMBL | |||||
Sodium channel protein type 2 subunit alpha | Ion channel | BLOCKER | UNKNOWN | CHEMBL | |||||
Sodium channel protein type 4 subunit alpha | Ion channel | BLOCKER | WOMBAT-PK | CHEMBL | |||||
Potassium channel subfamily K member 3 | Ion channel | IC50 | 4.41 | CHEMBL | |||||
Sodium channel protein type 2 subunit alpha | Ion channel | BLOCKER | IC50 | 6 | IUPHAR |
ID | Source |
---|---|
4019752 | VUID |
N0000147843 | NUI |
D04095 | KEGG_DRUG |
36637-19-1 | SECONDARY_CAS_RN |
4018912 | VANDF |
4019752 | VANDF |
C0015120 | UMLSCUI |
CHEBI:4904 | CHEBI |
CHEMBL492 | ChEMBL_ID |
DB08987 | DRUGBANK_ID |
D005041 | MESH_DESCRIPTOR_UI |
37497 | PUBCHEM_CID |
2621 | IUPHAR_LIGAND_ID |
3419 | INN_ID |
I6CQM0F31V | UNII |
227221 | RXNORM |
4705 | MMSL |
d01400 | MMSL |
001339 | NDDF |
005119 | NDDF |
370282009 | SNOMEDCT_US |
4043008 | SNOMEDCT_US |
88485001 | SNOMEDCT_US |
CHEMBL1200597 | ChEMBL_ID |
None