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111470-99-6

111470-99-6 structure
111470-99-6 structure
  • Name: Amlodipine besylate
  • Chemical Name: amlodipine benzenesulfonate
  • CAS Number: 111470-99-6
  • Molecular Formula: C26H31ClN2O8S
  • Molecular Weight: 567.051
  • Catalog: API Circulatory system medication Prevention and treatment of angina pectoris
  • Create Date: 2018-02-06 08:00:00
  • Modify Date: 2024-01-02 10:20:31
  • Amlodipine besylate is a long-acting calcium channel blocker.Target: Calcium ChannelAmlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the movement of calcium ions into vascular smooth muscle cells and cardiac muscle cells. Experimental data suggest amlodipine binds to both dihydropyridine and nondihydropyridine binding sites. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. Negative inotropic effects, or decreased heart muscle contractility, can be detected in vitro, but such effects have not been seen in intact animals at therapeutic doses. Serum calcium concentration is not affected by amlodipine. Within the physiologic pH range, amlodipine is an ionized compound (pKa = 8.6), and its interaction with the calcium channel receptor is characterized by a gradual rate of association and dissociation with the receptor binding site, resulting in a gradual onset of effect. Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure. From Wikipedia.
Name amlodipine benzenesulfonate
Synonyms Amlodin
Norvasc
3-Ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate benzenesulfonate (1:1)
3-Ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylate benzenesulfonate (1:1)
3,5-Pyridinedicarboxylic acid, 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-, 3-ethyl 5-methyl ester, benzenesulfonate (1:1)
Benzolsulfonsäure--3-ethyl-5-methyl-2-[(2-aminoethoxy)methyl]-4-(2-chlorphenyl)-6-methyl-1,4-dihydropyridin-3,5-dicarboxylat(1:1)
UNII:864V2Q084H
MFCD00887594
acide benzènesulfonique - 2-[(2-aminoéthoxy)méthyl]-4-(2-chlorophényl)-6-méthyl-1,4-dihydropyridine-3,5-dicarboxylate de 3-éthyle et de 5-méthyle (1:1)
3-ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate benzenesulfonate
3-Ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylate benzenesulfonate
Amlodipine Besilate
Amlodipine besylate
benzenesulfonic acid,3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
AMLODIPINE BENZENESULFONATE
3-Ethyl 5-Methyl (±)-2-[(2-Aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylate Monobenzenesulfonate
Description Amlodipine besylate is a long-acting calcium channel blocker.Target: Calcium ChannelAmlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the movement of calcium ions into vascular smooth muscle cells and cardiac muscle cells. Experimental data suggest amlodipine binds to both dihydropyridine and nondihydropyridine binding sites. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. Negative inotropic effects, or decreased heart muscle contractility, can be detected in vitro, but such effects have not been seen in intact animals at therapeutic doses. Serum calcium concentration is not affected by amlodipine. Within the physiologic pH range, amlodipine is an ionized compound (pKa = 8.6), and its interaction with the calcium channel receptor is characterized by a gradual rate of association and dissociation with the receptor binding site, resulting in a gradual onset of effect. Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure. From Wikipedia.
Related Catalog
References

[1]. http://en.wikipedia.org/wiki/Amlodipine
Density 1.227g/cm3
Boiling Point 527.2ºC at 760 mmHg
Melting Point 199-201°C
Molecular Formula C26H31ClN2O8S
Molecular Weight 567.051
Flash Point 272.6ºC
Exact Mass 566.148987
PSA 162.63000
LogP 5.30950
Vapour Pressure 3.34E-11mmHg at 25°C
Storage condition Store at RT
Water Solubility DMSO: 20 mg/mL

CHEMICAL IDENTIFICATION

RTECS NUMBER :
US7967700
CHEMICAL NAME :
3,5-Pyridinedicarboxylic acid, 2-((2-aminoethoxy)methyl)-4-(2-chlorophenyl)- 1,4-dihydro-6-methyl-, 3-ethyl-5-methyl ester, monobenzenesulfonate
CAS REGISTRY NUMBER :
111470-99-6
LAST UPDATED :
199806
DATA ITEMS CITED :
12
MOLECULAR FORMULA :
C20-H25-Cl-N2-O5.C6-H6-O3-S
MOLECULAR WEIGHT :
567.10

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Unreported
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
6 mg/kg/60D-I
TOXIC EFFECTS :
Sense Organs and Special Senses (Olfaction) - effect, not otherwise specified
REFERENCE :
LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 341,1102,1993
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
393 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Lungs, Thorax, or Respiration - respiratory depression Blood - other changes
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,177,1991
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
42 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,71,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
678 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,71,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
37 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,71,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
31 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,71,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
36 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,71,1995 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
910 mg/kg/13W-C
TOXIC EFFECTS :
Kidney, Ureter, Bladder - urine volume increased Kidney, Ureter, Bladder - other changes in urine composition
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,177,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
36400 mg/kg/52W-C
TOXIC EFFECTS :
Kidney, Ureter, Bladder - urine volume increased Kidney, Ureter, Bladder - other changes in urine composition Related to Chronic Data - death
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,177,1991 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
2300 mg/kg
SEX/DURATION :
male 71 day(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,167,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
275 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,167,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
260 mg/kg
SEX/DURATION :
female 17-21 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,167,1991
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Precautionary Statements P301 + P312 + P330
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Faceshields;Gloves
Hazard Codes Xn: Harmful;
Risk Phrases R22
Safety Phrases 26-36
RIDADR NONH for all modes of transport
WGK Germany 3
RTECS US7967700
HS Code 2933990090
88150-42-9 structure

88150-42-9

98-11-3 structure

98-11-3

~87%

111470-99-6 structure

111470-99-6

Literature: EOS ECZACIBASI OZGUN KIMYASAL URUNLER SANAYI VE TICARET A.S. Patent: WO2004/58711 A1, 2004 ; Location in patent: Page 16, 17 ;
246852-08-4 structure

246852-08-4

515-42-4 structure

515-42-4

~88%

111470-99-6 structure

111470-99-6

Literature: Adamed SP. Z O.O. Patent: EP993447 B1, 2005 ; Location in patent: Page/Page column 3 ;
246852-10-8 structure

246852-10-8

515-42-4 structure

515-42-4

~81%

111470-99-6 structure

111470-99-6

Literature: Adamed SP. Z O.O. Patent: EP993447 B1, 2005 ; Location in patent: Page/Page column 3 ;
88150-62-3 structure

88150-62-3

98-11-3 structure

98-11-3

~%

111470-99-6 structure

111470-99-6

Literature: WO2011/117876 A1, ; Page/Page column 11-12 ;
156366-27-7 structure

156366-27-7

98-11-3 structure

98-11-3

~%

331258-31-2 structure

331258-31-2

140171-66-0 structure

140171-66-0

Detail
Literature: WO2003/101965 A1, ; Page 18; 19; 23-25 ;
246852-11-9 structure

246852-11-9

515-42-4 structure

515-42-4

~88%

111470-99-6 structure

111470-99-6

Literature: Adamed SP. Z O.O. Patent: EP993447 B1, 2005 ; Location in patent: Page/Page column 3 ;
246852-13-1 structure

246852-13-1

515-42-4 structure

515-42-4

~81%

111470-99-6 structure

111470-99-6

Literature: Adamed SP. Z O.O. Patent: EP993447 B1, 2005 ; Location in patent: Page/Page column 4 ;
156366-27-7 structure

156366-27-7

98-11-3 structure

98-11-3

~%

111470-99-6 structure

111470-99-6

Literature: WO2007/131759 A1, ; Page/Page column 8-10 ;
246852-09-5 structure

246852-09-5

515-42-4 structure

515-42-4

~%

111470-99-6 structure

111470-99-6

Literature: EP993447 B1, ; Page/Page column 3 ;
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%

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title: CAS No. 111470-99-6 | Chemsrc address: https://www.chemsrc.com/en/baike/1084283.html

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