thiocolchicoside 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
	4731	602-41-5

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

thiocolchicoside
thiocholshikoside
coltramyl
muscoril

used in combination with glafenine and meprobamate to tranquilize patients undergoing hysterosalpingography; structure

Molecular weight: 563.62
Formula: C27H33NO10S
CLOGP: -0.89
LIPINSKI: 2
HAC: 11
HDO: 5
TPSA: 164.01
ALOGS: -3.21
ROTB: 7

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2B,BRAF,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAPK10,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PRKDC,TEK,TGFBR1,ZAP70	23
kinase-selectivity-class	AXL,MAP2K6,PDK1	3
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

None

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cholestasis	63.61	45.02	22	1134	36277	90591014
Hepatocellular injury	56.39	45.02	19	1137	28939	90598352
Vitamin B12 deficiency	46.16	45.02	12	1144	7474	90619817

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Poisoning deliberate	59.70	38.40	19	1281	10115	42609920
Panic attack	46.20	38.40	16	1284	11029	42609006
Accidental poisoning	39.92	38.40	9	1291	1287	42618748

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Poisoning deliberate	51.03	36.18	20	2471	26311	110560497
Angioedema	47.90	36.18	29	2462	98471	110488337
Hepatocellular injury	47.33	36.18	23	2468	50619	110536189
Palatal oedema	45.71	36.18	10	2481	1690	110585118
Erythema	44.65	36.18	43	2448	291404	110295404
Melaena	43.43	36.18	24	2467	68733	110518075
Cholestasis	42.07	36.18	23	2468	64495	110522313
Pancreas infection	37.92	36.18	7	2484	502	110586306
Accidental poisoning	36.79	36.18	9	2482	2478	110584330

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	M03BX05	MUSCULO-SKELETAL SYSTEM MUSCLE RELAXANTS MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS Other centrally acting agents
ATC	M03BX55	MUSCULO-SKELETAL SYSTEM MUSCLE RELAXANTS MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS Other centrally acting agents

Related Drugs by ATC class:

M03BX Other centrally acting agents 9 drugs

baclofen cyclobenzaprine eperisone fenyramidol mephenesin pridinol tetrazepam tizanidine tolperisone

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Spasticity	indication	221360009

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.22	acidic
pKa2	12.23	acidic
pKa3	12.92	acidic
pKa4	13.44	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
GABA-A receptor alpha-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRG2_HUMAN GBRB2_HUMAN	NEGATIVE MODULATOR	IC50	6.70		SCIENTIFIC LITERATURE
GABA A receptor alpha-2/beta-2/gamma-2	Ion channel	P18507 P47869 P47870	GBRG2_HUMAN GBRA2_HUMAN GBRB2_HUMAN	NEGATIVE MODULATOR	IC50	6.89		SCIENTIFIC LITERATURE
GABA A receptor alpha-1/beta-1/gamma-2	Ion channel	P14867 P18505 P18507	GBRA1_HUMAN GBRB1_HUMAN GBRG2_HUMAN	NEGATIVE MODULATOR	IC50	6.82		SCIENTIFIC LITERATURE
GABA-A receptor; anion channel	Ion channel		GBRP_RAT GBRB1_RAT GBRD_RAT GBRG2_RAT GBRA5_RAT GBRA3_RAT GBRG1_RAT GBRA2_RAT GBRA4_RAT GBRG3_RAT GBRA6_RAT GBRA1_RAT GBRB3_RAT GBRB2_RAT Q91ZM7_RAT GBRE_RAT		IC50	5.72		CHEMBL

External reference:

ID	Source
D07276	KEGG_DRUG
CHEBI:94557	CHEBI
CHEMBL213907	ChEMBL_ID
C004280	MESH_SUPPLEMENTAL_RECORD_UI
DB11582	DRUGBANK_ID
T1X8S697GT	UNII
38085	RXNORM
005350	NDDF
1173015002	SNOMEDCT_US
735241007	SNOMEDCT_US
C0076456	UMLSCUI
671	INN_ID
9915886	PUBCHEM_CID
T1X8S697GT	INXIGHT DRUGS

Pharmaceutical products:

None