Triamterene

Modify Date: 2025-08-21 09:49:43

Triamterene structure	Common Name	Triamterene
	CAS Number	396-01-0	Molecular Weight	253.26300
	Density	1.502 g/cm3	Boiling Point	573.4ºC at 760 mmHg
	Molecular Formula	C₁₂H₁₁N₇	Melting Point	316°C
	MSDS	Chinese USA	Flash Point	11 °C
	Symbol	GHS07	Signal Word	Warning

Use of Triamterene

Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic.Target: Sodium ChannelTriamterene blocked rENaC in a voltage-dependent manner, and was 100-fold less potent than amiloride at pH 7.5. At -90 mV and -40 mV, the IC50 values were 5 microM and 10 microM, respectively. The blockage by triamterene, which is a weak base with a pKa of 6.2, was dependent on the extracellular pH. The IC50 was 1 microM at pH 6.5 and only 17 microM at pH 8.5 [1]. Triamterene (TA) is partly eliminated by a first-pass-effect. The main metabolite of TA is OH-TA-ester, which is pharmacologically active [2].

Name	2,4,7-Triamino-6-Phenylpteridine
Synonym	More Synonyms

Description	Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic.Target: Sodium ChannelTriamterene blocked rENaC in a voltage-dependent manner, and was 100-fold less potent than amiloride at pH 7.5. At -90 mV and -40 mV, the IC50 values were 5 microM and 10 microM, respectively. The blockage by triamterene, which is a weak base with a pKa of 6.2, was dependent on the extracellular pH. The IC50 was 1 microM at pH 6.5 and only 17 microM at pH 8.5 [1]. Triamterene (TA) is partly eliminated by a first-pass-effect. The main metabolite of TA is OH-TA-ester, which is pharmacologically active [2].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel Research Areas >> Metabolic Disease
References	[1]. Busch, A.E., et al., Blockade of epithelial Na+ channels by triamterenes - underlying mechanisms and molecular basis. Pflugers Arch, 1996. 432(5): p. 760-6. [2]. Gilfrich, H.J., et al., Pharmacokinetics of triamterene after i.v. administration to man: determination of bioavailability. Eur J Clin Pharmacol, 1983. 25(2): p. 237-41.

Description

Related Catalog

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel

Research Areas >> Metabolic Disease

References

[1]. Busch, A.E., et al., Blockade of epithelial Na+ channels by triamterenes - underlying mechanisms and molecular basis. Pflugers Arch, 1996. 432(5): p. 760-6.

[2]. Gilfrich, H.J., et al., Pharmacokinetics of triamterene after i.v. administration to man: determination of bioavailability. Eur J Clin Pharmacol, 1983. 25(2): p. 237-41.

Density	1.502 g/cm3
Boiling Point	573.4ºC at 760 mmHg
Melting Point	316°C
Molecular Formula	C₁₂H₁₁N₇
Molecular Weight	253.26300
Flash Point	11 °C
Exact Mass	253.10800
PSA	129.62000
LogP	2.57700
InChIKey	FNYLWPVRPXGIIP-UHFFFAOYSA-N
SMILES	Nc1nc(N)c2nc(-c3ccccc3)c(N)nc2n1
Storage condition	2-8°C
Water Solubility	<0.1 G/100 ML AT 20 ºC

Triamterene MSDS(Chinese)

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UO3470000

CHEMICAL NAME :: Pteridine, 2,4,7-triamino-6-phenyl-

CAS REGISTRY NUMBER :: 396-01-0

BEILSTEIN REFERENCE NO. :: 0266723

LAST UPDATED :: 199612

DATA ITEMS CITED :: 21

MOLECULAR FORMULA :: C12-H11-N7

MOLECULAR WEIGHT :: 253.30

WISWESSER LINE NOTATION :: T66 BN DN GN JNJ CZ EZ HR& IZ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 42 mg/kg/3W-I

TOXIC EFFECTS :: Liver - hepatitis (hepatocellular necrosis), zonal Nutritional and Gross Metabolic - body temperature increase

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 285 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 249 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 620 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 25077 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 157 mg/kg/3W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2700 mg/m3/15D-C

TOXIC EFFECTS :: Endocrine - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 6370 mg/m3/13W-C

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8190 mg/kg/13W-C

TOXIC EFFECTS :: Endocrine - other changes Blood - changes in leukocyte (WBC) count Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 21840 mg/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Liver - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 34944 mg/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Liver - tumors

MUTATION DATA

TYPE OF TEST :: Sister chromatid exchange

TEST SYSTEM :: Rodent - hamster Lung

DOSE/DURATION :: 12600 ug/L

REFERENCE :: SNSHBT Senshokutai. Chromosome. (Sensyokutai Gakkai, Kaokusai Kirisutokyo Daigaku, Mitaka, Tokyo-to, Japan) No.1- 1946- Adopted new numbering in 1976. Volume(issue)/page/year: (20),574,1980 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5679 No. of Facilities: 60 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 587 (estimated) No. of Female Employees: 310 (estimated)

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302-H315-H319-H335
Precautionary Statements	P301 + P312 + P330-P305 + P351 + P338
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Faceshields;Gloves
Hazard Codes	Xn:Harmful;
Risk Phrases	R22;R36/37/38
Safety Phrases	S26-S36/37/39-S45-S33-S24-S16-S7
RIDADR	2811
WGK Germany	3
RTECS	UO3470000
Packaging Group	III
Hazard Class	6.1(b)
HS Code	2933990090

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

[Clinical strategies for prevention of drug-induced urinary calculi].

Clin. Calcium 21(10) , 1457-63, (2011)

Drug-induced urinary calculi, although they account for only 1-2% of urinary calculi, deserve consideration because most of them are preventable. In the drug-containing calculi resulting from the crys...

Bioavailability study of triamterene and xipamide using urinary pharmacokinetic data following single oral dose of each drug or their combination.

J. Pharm. Biomed. Anal. 61 , 78-85, (2012)

An efficient chromatographic method for the simultaneous determination of triamterene (TRI) and xipamide (XIP) in urine samples, based on high performance liquid chromatography with photodiode array d...

Spectrophotometric and spectrodensitometric determination of triamterene and xipamide in pure form and in pharmaceutical formulation.

Drug Test. Anal. 2(3) , 113-21, (2010)

Sensitive and validated UV-spectrophotometric, chemometric and TLC-densitometric methods were developed for determination of triamterene (TRM) and xipamide (XIP) in their binary mixture, formulated fo...

Triamterene

MFCD00006708

6-Phenylpteridine-2,4,7-triamine

2,4,7-Triamino-6-phenylpteridine,6-Phenyl-2,4,7-pteridinetriamine

EINECS 206-904-3

2,4,7-Triamino-6-phenylpteridine 6-Phenyl-2,4,7-pteridinetriamine

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Triamterene

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