Nitrendipine

Modify Date: 2024-01-02 12:41:20

Nitrendipine structure	Common Name	Nitrendipine
	CAS Number	39562-70-4	Molecular Weight	360.361
	Density	1.2±0.1 g/cm3	Boiling Point	488.9±45.0 °C at 760 mmHg
	Molecular Formula	C₁₈H₂₀N₂O₆	Melting Point	1580C
	MSDS	Chinese USA	Flash Point	249.5±28.7 °C
	Symbol	GHS07	Signal Word	Warning

Use of Nitrendipine

Nitrendipine is a calcium channel blocker with marked vasodilator action.Target: Calcium ChannelNitrendipine is a dihydropyridine calcium channel blocker. It is used in the treatment of primary hypertension to decrease blood pressure. Nitrendipine blocked Ca2+ currents very potently, with half-block by subnanomolar concentrations. The concentration dependence of block had the form expected for 1:1 binding, with an apparent dissociation constant (Kd) of 0.36 nM. In contrast, when cells were held at hyperpolarized potentials, nitrendipine blocked Ca2+ currents much less potently (Kd approximately equal to 700 nM) [1, 2]. Nitrendipine, a potent analogue of nifedipine, binds in a reversible and saturable manner to partially purified guinea-pig heart membranes [3]. [3H]nitrendipine binding in smooth muscle is to a site which mediates the pharmacologic response [4].

Name	nitrendipine
Synonym	More Synonyms

Description	Nitrendipine is a calcium channel blocker with marked vasodilator action.Target: Calcium ChannelNitrendipine is a dihydropyridine calcium channel blocker. It is used in the treatment of primary hypertension to decrease blood pressure. Nitrendipine blocked Ca2+ currents very potently, with half-block by subnanomolar concentrations. The concentration dependence of block had the form expected for 1:1 binding, with an apparent dissociation constant (Kd) of 0.36 nM. In contrast, when cells were held at hyperpolarized potentials, nitrendipine blocked Ca2+ currents much less potently (Kd approximately equal to 700 nM) [1, 2]. Nitrendipine, a potent analogue of nifedipine, binds in a reversible and saturable manner to partially purified guinea-pig heart membranes [3]. [3H]nitrendipine binding in smooth muscle is to a site which mediates the pharmacologic response [4].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel Research Areas >> Cardiovascular Disease
References	[1]. Bean, B.P., Nitrendipine block of cardiac calcium channels: high-affinity binding to the inactivated state. Proc Natl Acad Sci U S A, 1984. 81(20): p. 6388-92. [2]. Peterson, B.Z., T.N. Tanada, and W.A. Catterall, Molecular determinants of high affinity dihydropyridine binding in L-type calcium channels. J Biol Chem, 1996. 271(10): p. 5293-6. [3]. Bellemann, P., et al., [3H]-Nitrendipine, a potent calcium antagonist, binds with high affinity to cardiac membranes. Arzneimittelforschung, 1981. 31(12): p. 2064-7. [4]. Bolger, G.T., et al., Characterization of binding of the Ca++ channel antagonist, [3H]nitrendipine, to guinea-pig ileal smooth muscle. J Pharmacol Exp Ther, 1983. 225(2): p. 291-309.

Description

Related Catalog

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

Research Areas >> Cardiovascular Disease

References

[1]. Bean, B.P., Nitrendipine block of cardiac calcium channels: high-affinity binding to the inactivated state. Proc Natl Acad Sci U S A, 1984. 81(20): p. 6388-92.

[2]. Peterson, B.Z., T.N. Tanada, and W.A. Catterall, Molecular determinants of high affinity dihydropyridine binding in L-type calcium channels. J Biol Chem, 1996. 271(10): p. 5293-6.

[3]. Bellemann, P., et al., [3H]-Nitrendipine, a potent calcium antagonist, binds with high affinity to cardiac membranes. Arzneimittelforschung, 1981. 31(12): p. 2064-7.

[4]. Bolger, G.T., et al., Characterization of binding of the Ca++ channel antagonist, [3H]nitrendipine, to guinea-pig ileal smooth muscle. J Pharmacol Exp Ther, 1983. 225(2): p. 291-309.

Density	1.2±0.1 g/cm3
Boiling Point	488.9±45.0 °C at 760 mmHg
Melting Point	1580C
Molecular Formula	C₁₈H₂₀N₂O₆
Molecular Weight	360.361
Flash Point	249.5±28.7 °C
Exact Mass	360.132141
PSA	110.45000
LogP	3.50
Vapour Pressure	0.0±1.2 mmHg at 25°C
Index of Refraction	1.554
Storage condition	Store at RT
Water Solubility	methanol: 15 mg/mL

CHEMICAL IDENTIFICATION

RTECS NUMBER :: US5653000

CHEMICAL NAME :: 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, ethyl methyl ester

CAS REGISTRY NUMBER :: 39562-70-4

LAST UPDATED :: 199612

DATA ITEMS CITED :: 17

MOLECULAR FORMULA :: C18-H20-N2-O6

MOLECULAR WEIGHT :: 360.40

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 15370 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes Blood - changes in spleen

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 36,121,1988

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 205 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes Blood - changes in spleen

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 36,121,1988

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5166 mg/kg

TOXIC EFFECTS :: Gastrointestinal - other changes Blood - changes in spleen Skin and Appendages - hair

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 36,121,1988

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 12600 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: 52EDA6 "Nitrendipine, Based on Presentations at International Workshop on Nitrendipine, 1st, New York, 1982," Scriabine, A., et al., eds., Baltimore, Urban & Schwarzenberg, 1984 Volume(issue)/page/year: -,25,1984

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2540 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - rigidity (including catalepsy) Lungs, Thorax, or Respiration - cyanosis

REFERENCE :: 52EDA6 "Nitrendipine, Based on Presentations at International Workshop on Nitrendipine, 1st, New York, 1982," Scriabine, A., et al., eds., Baltimore, Urban & Schwarzenberg, 1984 Volume(issue)/page/year: -,25,1984

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 303 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes Blood - changes in spleen

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 36,121,1988

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7613 mg/kg

TOXIC EFFECTS :: Gastrointestinal - other changes Blood - changes in spleen Skin and Appendages - hair

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 36,121,1988

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 34500 ug/kg

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

REFERENCE :: FRPSAX Farmaco, Edizione Scientifica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 42,697,1987

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >100 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting

REFERENCE :: 52EDA6 "Nitrendipine, Based on Presentations at International Workshop on Nitrendipine, 1st, New York, 1982," Scriabine, A., et al., eds., Baltimore, Urban & Schwarzenberg, 1984 Volume(issue)/page/year: -,25,1984

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >2500 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: 52EDA6 "Nitrendipine, Based on Presentations at International Workshop on Nitrendipine, 1st, New York, 1982," Scriabine, A., et al., eds., Baltimore, Urban & Schwarzenberg, 1984 Volume(issue)/page/year: -,25,1984

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 2500 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - rigidity (including catalepsy) Lungs, Thorax, or Respiration - cyanosis

REFERENCE :: 52EDA6 "Nitrendipine, Based on Presentations at International Workshop on Nitrendipine, 1st, New York, 1982," Scriabine, A., et al., eds., Baltimore, Urban & Schwarzenberg, 1984 Volume(issue)/page/year: -,25,1984

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 2500 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: 52EDA6 "Nitrendipine, Based on Presentations at International Workshop on Nitrendipine, 1st, New York, 1982," Scriabine, A., et al., eds., Baltimore, Urban & Schwarzenberg, 1984 Volume(issue)/page/year: -,25,1984 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 107 gm/kg/2Y-C

TOXIC EFFECTS :: Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: 52EDA6 "Nitrendipine, Based on Presentations at International Workshop on Nitrendipine, 1st, New York, 1982," Scriabine, A., et al., eds., Baltimore, Urban & Schwarzenberg, 1984 Volume(issue)/page/year: -,25,1984 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1720 mg/kg

SEX/DURATION :: female 17-22 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 36,133,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 11000 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 36,145,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1100 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 36,145,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 330 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - live birth index (measured after birth)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 36,145,1988

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H312 + H332
Precautionary Statements	P261-P280
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes	Xn:Harmful
Risk Phrases	R20/21/22
Safety Phrases	S36
RIDADR	NONH for all modes of transport
WGK Germany	1
RTECS	US5653000
HS Code	2933399090

Precursor 9
CAS#:70076-42-5 ethyl 3-oxo-5-(... CAS#:21731-17-9 Methyl (Z)-3-am... CAS#:74-88-4 methyl iodide CAS#:39562-16-8 Ethyl 2-(3-nitr...
CAS#:81777-30-2 1,1,1-Triphenyl... CAS#:141-97-9 Ethyl acetoacetate CAS#:99-61-6 3-Nitrobenzaldehyde CAS#:14205-39-1 Methyl 3-aminoc...
CAS#:105-45-3 Methyl acetoacetate
DownStream 6
CAS#:64603-72-1 5-methoxycarbon... CAS#:74936-72-4 UNII:5DU0E310OI CAS#:64603-74-3 methyl 2-methyl... CAS#:80890-07-9 (+)-Nitrendipine
CAS#:80873-62-7 (-)-Nitrendipine CAS#:89267-41-4 Dehydronitrendipine

HS Code	2933399090
Summary	2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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3-Ethyl-5-methyl-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate

Nitrendipine

MFCD00082255

1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid ethyl methyl ester

Ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylate

Bylotensin

ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate

Ethyl methyl 1,4-dihydro-2,6-dimethyl-4-(meta-nitrophenyl)-3,5-pyridinedicarboxylate

UNII:9B627AW319

3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, ethyl methyl ester

EINECS 254-513-1

Deiten

Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: Nitrendipine
Price: ￥1058.0/1g ￥598.0/500mg ￥128.0/100mg
Purity: 95.0%
Stocking Period: 1 Day
Contact: Liu jia

DC Chemicals Limited
China
Product Name: Nitrendipine
Price: $300.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Nitrendipine
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

Henan Tianfu Chemical Co., Ltd.
China
Product Name: nitrendipine
Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
Purity: 99.0%
Stocking Period: Inquiry
Contact: Anson

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