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57470-78-7

57470-78-7 structure
57470-78-7 structure
  • Name: Celiprolol HCl
  • Chemical Name: Celiprolol Hydrochloride
  • CAS Number: 57470-78-7
  • Molecular Formula: C20H34ClN3O4
  • Molecular Weight: 415.955
  • Catalog: API Circulatory system medication Antiarrhythmic drug
  • Create Date: 2018-09-10 20:28:19
  • Modify Date: 2024-01-02 09:37:48
  • Celiprolol hydrochloride is a potent, selective and orally active antagonist of β1-andrenoceptor with partial β2 agonist activity, therefore it is a selective adrenoreceptor modulator (SAM). Celiprolol hydrochloride demonstrates antihypertensive and antianginal activity[1].
Name Celiprolol Hydrochloride
Synonyms MFCD00941500
3-{3-Acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl}-1,1-diethylurea hydrochloride (1:1)
Urea, N'-[3-acetyl-4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]phenyl]-N,N-diethyl-, hydrochloride (1:1)
(+)-3-(3-Acetyl-4-(3-(tert-butylamino)-2-hydroxypropoxy)phenyl)-1,1-diethylurea hydrochloride
Celiprolol Hydrochloride
UNII:G1M3398594
3-(3-Acetyl-4-{2-hydroxy-3-[(2-methyl-2-propanyl)amino]propoxy}phenyl)-1,1-diethylurea hydrochloride (1:1)
EINECS 260-752-2
Celiprolol HCl
3-[3-acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-1,1-diethylurea,hydrochloride
Description Celiprolol hydrochloride is a potent, selective and orally active antagonist of β1-andrenoceptor with partial β2 agonist activity, therefore it is a selective adrenoreceptor modulator (SAM). Celiprolol hydrochloride demonstrates antihypertensive and antianginal activity[1].
Related Catalog
Target

β1-andrenoceptor[1]
In Vivo Celiprolol (5 or 50 mg/kg; p.o. every day for 12 weeks) has a moderate antihypertensive action at the dose of 50 mg/kg, and significantly reduces media smooth muscle hypertrophy of the mesenteric artery in SHR[2]. Animal Model: Male spontaneously hypertensive rats (SHR) and age-matched Wistar-Kyoto (WKY) rats (8 weeks old)[2] Dosage: 5, 50 mg/kg Administration: P.o. every day (administered in drinking water) for 12 weeks Result: Attenuated the rise in blood pressure significantly at the dose of 50 mg/kg in SHR. Did not significantly affect absolute heart or body weights. Reduced the average medial thickness of the mesenteric artery in SHR.
References

[1]. Nawarskas JJ, et, al. Celiprolol: A Unique Selective Adrenoceptor Modulator. Cardiol Rev. Sep/Oct 2017; 25(5): 247-253.

[2]. Tolvanen JP, et, al. Effect of celiprolol therapy on arterial dilatation in experimental hypertension. Br J Pharmacol. 1996 Nov; 119(6): 1137-44.
Density 1.114g/cm3
Boiling Point 586.5ºC at 760 mmHg
Melting Point 197-200ºC (dec.)
Molecular Formula C20H34ClN3O4
Molecular Weight 415.955
Flash Point 308.5ºC
Exact Mass 415.223785
PSA 94.39000
LogP 4.09720
Storage condition Refrigerator

CHEMICAL IDENTIFICATION

RTECS NUMBER :
YR6560000
CHEMICAL NAME :
Urea, 3-(3-acetyl-4-(3-((1,1-dimethylethyl)amino)-2-hydroxy propoxy)phenyl)-1,1-d iethyl-, monohydrochloride
CAS REGISTRY NUMBER :
57470-78-7
LAST UPDATED :
199709
DATA ITEMS CITED :
9
MOLECULAR FORMULA :
C20-H33-N3-O4.Cl-H
MOLECULAR WEIGHT :
416.02

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
40 mg/kg/2W-I
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
APHRER Annals of Pharmacotherpy. (Harvey Whitney Books Co., POB 42696, Cincinnati, OH 45242) V. 26- 1992- Volume(issue)/page/year: 26,842,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2157 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
754 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
68300 ug/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 33,41,1983
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1362 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
310 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
42300 ug/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
512 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
100 mg/kg
TOXIC EFFECTS :
Behavioral - excitement Lungs, Thorax, or Respiration - dyspnea Gastrointestinal - nausea or vomiting
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 33,41,1983
56980-93-9 structure

56980-93-9

~80%

57470-78-7 structure

57470-78-7
Literature: Ji, Li; Qian, Chao; Chen, Xin-Zhi; Mao, Xiao-Yuan 2011 , vol. 35, # 11 p. 640 - 643,4
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57470-78-7 structure

57470-78-7
Literature: , vol. 35, # 11 p. 640 - 643,4
100-02-7 structure

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57470-78-7 structure

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Literature: Organic Process Research and Development, , vol. 5, # 2 p. 176 - 178
1450-76-6 structure

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Literature: Organic Process Research and Development, , vol. 5, # 2 p. 176 - 178
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57470-78-7 structure

57470-78-7
Literature: Organic Process Research and Development, , vol. 5, # 2 p. 176 - 178
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57470-78-7 structure

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57470-78-7 structure

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57470-78-7 structure

57470-78-7
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