Manidipine hydrochloride

Modify Date: 2024-01-02 20:33:17

Manidipine hydrochloride structure	Common Name	Manidipine hydrochloride
	CAS Number	89226-75-5	Molecular Weight	683.62
	Density	N/A	Boiling Point	722ºC at 760 mmHg
	Molecular Formula	C₃₅H₄₀Cl₂N₄O₆	Melting Point	211 °C(dec.)
	MSDS	N/A	Flash Point	N/A

Use of Manidipine hydrochloride

Manidipine 2Hcl (CV-4093) is a dihydropyridine compound and a calcium channel blocker for Ca2+ current with IC50 of 2.6 nM. IC50 value: 2.6 nMTarget: calcium channelManidipine is described to block T-type Ca2+ channels specifically and is also described to have a high selectivity for the vasculature, presenting negligible cardiodepression as compared to other Ca2+ channel antagonists. Manidipine is also described to not significantly affect norepinephrine levels, suggesting a lack of sympathetic activation with this compound. Manidipine reduces pro-inflammatory cytokines secretion in human endothelial cells and macrophages. Manidipine, unlike other third-generation dihydropyridine derived drugs, blocks T-type calcium channels present in the efferent glomerular arterioles, reducing intraglomerular pressure and microalbuminuria.

Name	Manidipine Dihydrochloride
Synonym	More Synonyms

Description	Manidipine 2Hcl (CV-4093) is a dihydropyridine compound and a calcium channel blocker for Ca2+ current with IC50 of 2.6 nM. IC50 value: 2.6 nMTarget: calcium channelManidipine is described to block T-type Ca2+ channels specifically and is also described to have a high selectivity for the vasculature, presenting negligible cardiodepression as compared to other Ca2+ channel antagonists. Manidipine is also described to not significantly affect norepinephrine levels, suggesting a lack of sympathetic activation with this compound. Manidipine reduces pro-inflammatory cytokines secretion in human endothelial cells and macrophages. Manidipine, unlike other third-generation dihydropyridine derived drugs, blocks T-type calcium channels present in the efferent glomerular arterioles, reducing intraglomerular pressure and microalbuminuria.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel Research Areas >> Cardiovascular Disease
References	[1]. Buset Ríos N, Rodríguez Esparragón F, Fernández-Andrade Rodríguez C, et al. Vascular and metabolic properties of manidipine . Nefrologia. 2011;31(3):268-74. [2]. Costa S, Zimetti F, Pedrelli M, et al. Manidipine reduces pro-inflammatory cytokines secretion in human endothelial cells and macrophages. Pharmacol Res. 2010 Sep;62(3):265-70. [3]. Cavalieri L, Cremonesi G. Metabolic effects of manidipine. Am J Cardiovasc Drugs. 2009;9(3):163-76. doi: 10.2165/00129784-200909030-00004. [4]. Roca-Cusachs A, Triposkiadis F. Antihypertensive effect of manidipine. Drugs. 2005;65 Suppl 2:11-9. [5]. Nagaoka A. Pharmacologic characteristics of a new calcium antagonist, manidipine: beneficial effects on renal circulation and vascular changes. Am Heart J. 1993 Feb;125(2 Pt 2):560-5.

Description

Related Catalog

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

Research Areas >> Cardiovascular Disease

References

[1]. Buset Ríos N, Rodríguez Esparragón F, Fernández-Andrade Rodríguez C, et al. Vascular and metabolic properties of manidipine . Nefrologia. 2011;31(3):268-74.

[2]. Costa S, Zimetti F, Pedrelli M, et al. Manidipine reduces pro-inflammatory cytokines secretion in human endothelial cells and macrophages. Pharmacol Res. 2010 Sep;62(3):265-70.

[3]. Cavalieri L, Cremonesi G. Metabolic effects of manidipine. Am J Cardiovasc Drugs. 2009;9(3):163-76. doi: 10.2165/00129784-200909030-00004.

[4]. Roca-Cusachs A, Triposkiadis F. Antihypertensive effect of manidipine. Drugs. 2005;65 Suppl 2:11-9.

[5]. Nagaoka A. Pharmacologic characteristics of a new calcium antagonist, manidipine: beneficial effects on renal circulation and vascular changes. Am Heart J. 1993 Feb;125(2 Pt 2):560-5.

Boiling Point	722ºC at 760 mmHg
Melting Point	211 °C(dec.)
Molecular Formula	C₃₅H₄₀Cl₂N₄O₆
Molecular Weight	683.62
PSA	116.93000
LogP	6.48280

Manidipine hydrochloride MSDS(Chinese)

CHEMICAL IDENTIFICATION

RTECS NUMBER :: US7975300

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

CAS REGISTRY NUMBER :: 89226-75-5

LAST UPDATED :: 199210

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C35-H38-N4-O6.2Cl-H

MOLECULAR WEIGHT :: 683.69

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 :: 156 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 4),961,1989

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 49 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 4),961,1989

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 199 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 4),961,1989

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 171 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 4),961,1989

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 62 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 4),961,1989

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 340 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 4),961,1989 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2880 mg/kg

SEX/DURATION :: male 9 week(s) pre-mating female 2 week(s) pre-mating - 19 day(s) after conception

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

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 4),1101,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 136 mg/kg

SEX/DURATION :: female 15-22 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - stillbirth

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 4),1151,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 136 mg/kg

SEX/DURATION :: multigeneration

TOXIC EFFECTS :: Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 4),1151,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1300 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 4),1141,1989

Hazard Codes	Xi
HS Code	2942000000

Manidipine

CAS#:89226-50-6

Manidipine hydr...

CAS#:89226-75-5

Literature: WO2011/23954 A2, ; Page/Page column 18 ;

N-Benzhydrylpip...

CAS#:841-77-0

Manidipine hydr...

CAS#:89226-75-5

Literature: WO2011/23954 A2, ;

2-(4-benzhydryl...

CAS#:10527-64-7

Manidipine hydr...

CAS#:89226-75-5

Literature: Chemical and Pharmaceutical Bulletin, , vol. 33, # 9 p. 3787 - 3797

2-(4-benzhydryl...

CAS#:89226-49-3

Manidipine hydr...

CAS#:89226-75-5

Literature: Chemical and Pharmaceutical Bulletin, , vol. 33, # 9 p. 3787 - 3797

Methyl 2-(3-nit...

CAS#:39562-17-9

2-(4-diphenylme...

CAS#:90096-33-6

~14%

Manidipine hydr...

CAS#:89226-75-5

Literature: Meguro; Aizawa; Sohda; Kawamatsu; Nagaoka Chemical and Pharmaceutical Bulletin, 1985 , vol. 33, # 9 p. 3787 - 3797

3-Nitrobenzaldehyde

CAS#:99-61-6

Methyl acetoacetate

CAS#:105-45-3

2-(4-diphenylme...

CAS#:90096-33-6

~17%

Manidipine hydr...

CAS#:89226-75-5

Literature: Meguro; Aizawa; Sohda; Kawamatsu; Nagaoka Chemical and Pharmaceutical Bulletin, 1985 , vol. 33, # 9 p. 3787 - 3797

Precursor 7
CAS#:89226-50-6 Manidipine CAS#:841-77-0 N-Benzhydrylpip... CAS#:10527-64-7 2-(4-benzhydryl... CAS#:89226-49-3 2-(4-benzhydryl...
CAS#:39562-17-9 Methyl 2-(3-nit... CAS#:99-61-6 3-Nitrobenzaldehyde CAS#:105-45-3 Methyl acetoacetate
DownStream 1
CAS#:104305-93-3 Diphpetmednp

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%

3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 2-[4-(diphenylmethyl)-1-piperazinyl]ethyl methyl ester, hydrochloride (1:1)

Manidipine hydrochloride

2-[4-(Diphenylmethyl)piperazin-1-yl]ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate hydrochloride (1:1)

MFCD00896434

2-[4-(Diphenylmethyl)-1-piperazinyl]ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylate hydrochloride (1:1)

Manidipine 2HCl

Manidipine (dihydrochloride)

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