cilostazol (Ref: OPC-13013) ** cilostazolum ** cilostazole ** Translations

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GENERAL INFORMATION

Description: A novel drug being explored for veterinary applications

Introduction: -

Examples of species treated: Dogs

General status:

Veterinary substance type	Antiplatelet agent, Antithrombotic agent, Medicinal drug
Substance group	Quinolone
Substance origin	-
Mode of action	A selective inhibitor of 3-type phosphodiesterase (PDE3) with therapeutic focus on increasing cAMP
Molecular targets	cGMP-inhibited 3',5'-cyclic phosphodiesterase A, antagonist
CAS RN	73963-72-1
EC number	-
CIPAC number	-
US EPA chemical code	-
ATCvet Code	QB01AC23
Therapeutic Class	Blood and blood forming organs: Antithrombotic agents
Controlled Drug?	No
Regulation 37/2010 MRL Classification	No data
Chemical formula	C20H27N5O2
SMILES	n1(c(nnn1)CCCCOc1cc2c(cc1)NC(=O)CC2)C1CCCCC1
International Chemical Identifier (InChI)	InChI=1S/C20H27N5O2/c26-20-12-9-15-14-17(10-11-18(15)21-20)27-13-5-4-8-19-22-23-24-25(19)16-6-2-1-3-7-16/h10-11,14,16H,1-9,12-13H2,(H,21,26)
Structure diagram/image available?	Yes
Molecular mass (g mol-1)	369.46
IUPAC Name	6-[4-(1-cyclohexyl-1H-1,2,3,4-tetrazol-5-yl)butoxy]-1,2,3,4-tetrahydroquinolin-2-one
CAS Name	6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-,4-dihydro-2(1H)-quinolinone
Other status information	-
Physical state	White crystalline powder
Related substances & organisms	-

Formulations:

Property	Product	Manufacturer	Authorisation Route	UK Legal Class
Example products using this active	None identified	None identified	No UK authorisation for use with animals	Not applicable
Formulation and application details	-

ENVIRONMENTAL FATE

Property		Value	Source/Quality Score/Other Information	Interpretation
Solubility - In water at 20oC (mg l-1)		-	-	-
Solubility - In organic solvents at 20oC (mg l-1)		-	-	-
Melting Point (oC)		160	V3	-
Boiling Point (oC)		-	-	-
Degradation point (oC)		-	-	-
Flashpoint (oC)		-	-	-
Octanol-water partition coefficient at pH 7, 20oC	P	2.00 X 1002	Calculated	-
	Log P	2.3	F4	Low
Bulk density (g ml-1)/Specific gravity		-	-	-
Dissociation constant (pKa) at 25oC		-	-	-
		Note:
Vapour pressure at 25oC (mPa)		-	-	-
Henry's law constant at 25oC (Pa m3 mol-1)		-	-	-
Henry's law constant at 20oC (dimensionless)		-	-	-
GUS leaching potential index		-	-	-
Maximum UV-vis absorption L mol-1 cm-1		-	-	-
Surface tension (mN m-1)		-	-	-
Refractive Index		-	-	-

Degradation:

Property		Value	Source/Quality Score/Other Information	Interpretation
Soil degradation (days) (aerobic)	DT50 (typical)	-	-	-
	DT50 (lab at 20oC)	-	-	-
	DT50 (field)	-	-	-
	DT90 (lab at 20oC)	-	-	-
	DT90 (field)	-	-	-
	Note:	-
Manure DT50 (days)		-	-	-
Aqueous photolysis DT50 (days) at pH 7	Value	-	-	-
	Note	-
Aqueous hydrolysis DT50 (days) at 20oC and pH 7	Value	-	-	-
	Note	-
Water-Sediment DT50 (days)		-	-	-
Water phase only DT50 (days)		-	-	-

Soil adsorption and mobility:

Property		Value	Source/Quality Score/Other Information	Interpretation
Linear	Kd	-	-	-
	Koc	-
	Notes and range	-
Freundlich	Kf	-	-	-
	Kfoc	-
	1/n	-
	Notes and range	-
pH sensitivity		-

Other known metabolites:

Metabolite name and reference	Aliases	Formation Medium / Rate	Estimated Maximum Occurrence Fraction	Metabolising Enzymes
(6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)- butoxy]-2(1H-quinolinone) (Ref: OPC-13015) Note: Pharmacologically active	DHC; 3,4-dehydrocilostazol	Rat (Urine)	~0.02% administered dose	Cytochrome P450 3A
3,4-dihydro-6-[4-(1-(trans-4-hydroxycyclohexyl-1H-tetrazol-5-yl)butoxy]-2(1H-quinolinone) (Ref: OPC-13213) Note: Pharmacologically active	HC; 4'-trans-hydroxycilostazol	Rat (Urine)	~0.3% administered dose	Cytochrome P450 3A
3,4-dihydro-6-[4-[1-(cis-4-hydroxycyclohexyl)-1H-tetrazol-5-yl)butoxy]-2(1H)-quinolinone)]. (Ref: OPC-13217) Note: Pharmacologically active	-	Rat (Liver)	-	Cytochrome P450 2C8 Cytochrome P450 2C19 Cytochrome P450 3A4 Cytochrome P450 3A5
(Ref: OPC-13269)	-	-	-	-
[6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-4-hydroxy-2(1H)-quinolinone] (Ref: OPC-13326) Note: Pharmacologically active	-	Rat (Liver)	-	Cytochrome P450 3A4 Cytochrome P450 1B1 Cytochrome P450 35A
(Ref: OPC-13366)	-	-	-	-
(Ref: OPC-13388)	-	-	-	-

ECOTOXICOLOGY

Property		Value	Source/Quality Score/Other Information	Interpretation
Bio-concentration factor	BCF	-	-	-
	CT50 (days)	-		-
Bioaccumulation potential		-	Calculated	Low
Mammals - Acute oral LD50 (mg kg-1)		> 5000	V3 Rat	Low
Mammals - Short term dietary NOEL	(mg kg-1)	-	-	-
	(ppm diet)	-		-
Birds - Acute LD50 (mg kg-1)		-	-	-
Birds - Short term dietary (LC50/LD50)		-	-	-
Fish - Acute 96 hour LC50 (mg l-1)		-	-	-
Fish - Chronic 21 day NOEC (mg l-1)		-	-	-
Aquatic invertebrates - Acute 48 hour EC50 (mg l-1)		-	-	-
Aquatic invertebrates - Chronic 21 day NOEC (mg l-1)		-	-	-
Aquatic crustaceans - Acute 96 hour LC50 (mg l-1)		-	-	-
Sediment dwelling organisms - Acute 96 hour LC50 (mg l-1)		-	-	-
Sediment dwelling organisms - Chronic 28 day NOEC, static, water (mg l-1)		-	-	-
Sediment dwelling organisms - Chronic 28 day NOEC, sediment (mg kg-1)		-	-	-
Aquatic plants - Acute 7 day EC50, biomass (mg l-1)		-	-	-
Algae - Acute 72 hour EC50, growth (mg l-1)		-	-	-
Algae - Chronic 96 hour NOEC, growth (mg l-1)		-	-	-
Honeybees - Acute 48 hour LD50 (µg bee-1)		-	-	-
Earthworms - Acute 14 day LC50 (mg kg-1)		-	-	-
Earthworms - Chronic 14 day NOEC, reproduction (mg kg-1)		-	-	-
Other soil macro-organisms - e.g. Collembola	LR50product ha EC50product ha NOECproduct ha % Effect	-	-	-
Other arthropod (1)	LR50 g ha-1	-	-	-
	% Effect	-	-	-
Other arthropod (2)	LR50 g ha-1	-	-	-
	% Effect	-	-	-
Soil micro-organisms		-	-	-
Mesocosm study data	NOEAEC mg l-1	-	-	-
	NOEAEC mg l-1	-	-	-

HUMAN HEALTH AND PROTECTION

General:

Property		Value	Source/Quality Score/Other Information	Interpretation
Mammals - Acute oral LD50 (mg kg-1)		> 5000	V3 Rat	Low
Mammals - Dermal LD50 (mg kg-1 body weight)		-	-	-
Mammals - Inhalation LC50 (mg l-1)		-	-	-
Other Mammal toxicity endpoints		Intraperitoneal LD50 > 2000 mg kg-1	V3 Rat	-
		Intramuscular LD50 > 1000 mg kg-1	V3 Rat	-
ADI - Acceptable Daily Intake (mg kg-1bw day-1)		-	-	-
ARfD - Acute Reference Dose (mg kg-1bw day-1)		-	-	-
AOEL - Acceptable Operator Exposure Level - Systemic (mg kg-1bw day-1)		-	-	-
Dermal penetration studies (%)		-	-	-
Dangerous Substances Directive 76/464		-	-	-
Exposure Limits		-	-	-
Exposure Routes	Public	-
	Occupational	-
Elimination route and rate		Fully metabolised which are largely excreted in the urine with <20% being eliminated in the faeces	F4	-

Health issues:

Carcinogen	Mutagen	Endocrine disrupter	Reproduction / development effects	Acetyl cholinesterase inhibitor	Neurotoxicant	Respiratory tract irritant	Skin irritant	Eye irritant
		-		-
General human health issues		[May cause headaches and gastrointestinal problems], [May cause hypertension]

: Yes, known to cause a problem
: No, known not to cause a problem
: Possibly, status not identified
- : No data

Handling issues:

Property		Value	Source/Quality Score/Other Information	Interpretation
General		{No information available]
EC Risk Classification		-
EC Safety Classification		-
WHO Classification		None - not a ppp	-	-
US EPA Classification (formulation)		-	-	-
UN Number		-
Waste disposal & packaging		-

TRANSLATIONS