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5874-97-5

5874-97-5 structure
5874-97-5 structure
  • Name: Orciprenaline sulfate
  • Chemical Name: Metaproterenol Hemisulfate Salt
  • CAS Number: 5874-97-5
  • Molecular Formula: C11H17NO3.1/2H2O4S
  • Molecular Weight: 520.59400
  • Catalog: API Respiratory medication Asthma
  • Create Date: 2018-02-12 08:00:00
  • Modify Date: 2024-01-08 01:19:53
  • Metaproterenol hemisulfate (Orciprenaline hemisulfate) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity[1][2].
Name Metaproterenol Hemisulfate Salt
Synonyms Orciprenaline sulfate
Description Metaproterenol hemisulfate (Orciprenaline hemisulfate) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity[1][2].
Related Catalog
Target

IC50: 68 nM (β2-adrenergic receptor)[1]

In Vitro Metaproterenol (10 μM; 74 hours; THP-1 cells and bone marrow macrophages) treatment enhances β-arrestin2 and its interaction with IκBα in high glucose-induced THP-1 cells and bone marrow macrophages[1]. Metaproterenol (10 μM; 74 hours; THP-1 cells and bone marrow macrophages) treatment leads to downregulation of NF-κB in high glucose-induced THP-1 cells and bone marrow macrophages[1]. Western Blot Analysis[1] Cell Line: THP-1 cells and bone marrow macrophages Concentration: 10 μM Incubation Time: 74 hours Result: Enhanced β-arrestin2 and its interaction with IκBα. RT-PCR[1] Cell Line: THP-1 cells and bone marrow macrophages Concentration: 10 μM Incubation Time: 74 hours Result: Led to downregulation of NF-κB.
In Vivo Treatment of Zucker diabetic fatty rats with Metaproterenol for 12 weeks attenuates monocyte activation as well as pro-inflammatory and pro-fibrotic responses in the kidneys and heart. Thus, Metaproterenol might has protective effects against diabetic renal and cardiovascular complications[1].
References

[1]. Noh H, et al. Beta 2-adrenergic receptor agonists are novel regulators of macrophage activation in diabetic renal and cardiovascular complications. Kidney Int. 2017 Jul;92(1):101-113.

[2]. Ibrahim FA, et al. Highly sensitive spectrofluorimetric method for rapid determination of orciprenaline in biological fluids and pharmaceuticals. Luminescence. 2019 Feb;34(1):77-83.
Density 1.199g/cm3
Boiling Point 417.5ºC at 760mmHg
Melting Point 202-203°
Molecular Formula C11H17NO3.1/2H2O4S
Molecular Weight 520.59400
Flash Point 179.7ºC
Exact Mass 520.20900
PSA 228.42000
LogP 3.46820
Water Solubility Freely soluble in water, slightly soluble in ethanol (96 per cent), practically insoluble in methylene chloride.

CHEMICAL IDENTIFICATION

RTECS NUMBER :
DO2275000
CAS REGISTRY NUMBER :
5874-97-5
LAST UPDATED :
199606
DATA ITEMS CITED :
10
MOLECULAR FORMULA :
C22-H34-N2-O6.H2-O4-S
MOLECULAR WEIGHT :
520.66
WISWESSER LINE NOTATION :
QR DQ BYQ1MY1&1 2 WSQQ

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 :
5538 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>4 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 180,155,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraduodenal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2230 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 180,155,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
4800 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - effect, not otherwise specified Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,521,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
290 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - effect, not otherwise specified Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,521,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
114 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - effect, not otherwise specified Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,521,1961 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
500 mg/kg
SEX/DURATION :
female 6-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death
REFERENCE :
TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 38,15,1988
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
5 gm/kg
SEX/DURATION :
female 6-15 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 :
TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 38,15,1988
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
150 mg/kg
SEX/DURATION :
female 11-13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)
REFERENCE :
TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 38,15,1988 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3133 No. of Facilities: 1204 (estimated) No. of Industries: 1 No. of Occupations: 7 No. of Employees: 23118 (estimated) No. of Female Employees: 9688 (estimated)
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H332
Precautionary Statements P261
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xn
Risk Phrases 20
Safety Phrases 36
RIDADR NONH for all modes of transport
WGK Germany 2
RTECS DO2275000

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