Isoxsuprine hydrochloride

Modify Date: 2024-01-03 12:30:01

Isoxsuprine hydrochloride Structure
Isoxsuprine hydrochloride structure
Common Name Isoxsuprine hydrochloride
CAS Number 579-56-6 Molecular Weight 337.84100
Density 1.146g/cm3 Boiling Point 484.2ºC at 760mmHg
Molecular Formula C18H24ClNO3 Melting Point 203-204°
MSDS Chinese USA Flash Point 246.6ºC
Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning

 Use of Isoxsuprine hydrochloride


Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.

 Names

Name isoxsuprine hydrochloride
Synonym More Synonyms

 Isoxsuprine hydrochloride Biological Activity

Description Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.
Related Catalog
Target

Ki: 13.65 μΜ (myometrial beta-adrenergic receptor), 3.48 μΜ (placcntal beta-adrenergic receptor)[1] NMDA receptor[3]

In Vitro Results show that Isoxsuprine hydrochloride inhibits circular chemorepellent induced defect (CCID) formation dose dependently (5 to 60 μM) and also inhibits 12(S)-HETE synthesis. Furthermore, Isoxsuprine hydrochloride is the only drug inhibiting the induction of all three mobility markers (MLC2, MYPT and paxillin)[2].
In Vivo Total infarct volume in vehicle-treated animals is 279±25 mm3 compare to 137±18 mm3 in Isoxsuprine hydrochloride-treated animals[3].
Cell Assay MCF-7ALOX12 cells are seeded in 3.5-cm dishes and grown in 2.5 mL complete MEM medium without selection pressure. The next day, the medium is changed to serum-free medium and cells are kept at 37°C for 24 h. Then, cells are treated with 10 μM arachidonic acid and simultaneously with different concentrations of Isoxsuprine hydrochloride for 4 h when the supernatants are aspirated, centrifuged at 2000, r.p.m. at 4°C for 5 min, collected in cryo-tubes, flash frozen and stored at -80 °C until analysis[2].
Animal Admin Male spontaneously hypertensive rats (SHR) weighing 290 to 300 g are used in this study. At reperfusion, animals receive 0.5 mL of vehicle (0.6% DMSO in normal saline) or 1 mg/kg Isoxsuprine hydrochloride by intravenous (IV) injection through the lateral tail vein. All animals receive 3 mL of subcutaneous saline after surgery to prevent dehydration. After 24 hours reperfusion, animals are sacrificed, brains are sectioned into 4 mm-thick quadrants, and infarcted tissue is identified by 2,3,5-triphenyltetrazolium chloride (TTC) staining. Edema-corrected infarct volume is calculated by subtracting the area of non-infarcted tissue in the ipsilateral hemisphere from the total volume of the contralateral hemisphere. Infarct volume is quantified using Image J software[3].
References

[1]. Falkay G, et al. Affinity of tocolytic agents on human placental and myometrial beta-adrenergic receptors. J Perinat Med. 1986;14(2):109-13.

[2]. Kretschy N, et al. In vitro inhibition of breast cancer spheroid-induced lymphendothelial defects resembling intravasation into the lymphatic vasculature by acetohexamide, isoxsuprine, nifedipin and proadifen. Br J Cancer. 2013 Feb 19;108(3):570-8.

[3]. Hill JW, et al. Identification of isoxsuprine hydrochloride as a neuroprotectant in ischemic stroke through cell-based high-throughput screening. PLoS One. 2014 May 7;9(5):e96761.

 Chemical & Physical Properties

Density 1.146g/cm3
Boiling Point 484.2ºC at 760mmHg
Melting Point 203-204°
Molecular Formula C18H24ClNO3
Molecular Weight 337.84100
Flash Point 246.6ºC
Exact Mass 337.14400
PSA 61.72000
LogP 4.06410
Storage condition 2-8°C

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
DO8225000
CHEMICAL NAME :
Benzyl alcohol, p-hydroxy-alpha-(1-((1-methyl-2-phenoxyethyl)amino)et hyl)-, hydrochloride
CAS REGISTRY NUMBER :
579-56-6
LAST UPDATED :
199601
DATA ITEMS CITED :
12
MOLECULAR FORMULA :
C18-H23-N-O3.Cl-H
MOLECULAR WEIGHT :
337.88
WISWESSER LINE NOTATION :
QR DYQY1&MY1&1OR &GH

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 :
1750 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 :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
164 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 :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1100 mg/kg
TOXIC EFFECTS :
Behavioral - excitement Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,579,1959
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
185 mg/kg
TOXIC EFFECTS :
Behavioral - excitement Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,579,1959
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1500 mg/kg
TOXIC EFFECTS :
Behavioral - excitement Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,579,1959
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
61 mg/kg
TOXIC EFFECTS :
Behavioral - excitement Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,579,1959
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>1200 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,579,1959
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
143 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: 1,579,1959
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
57 mg/kg
TOXIC EFFECTS :
Behavioral - ataxia Cardiac - change in rate Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,579,1959 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
9300 mg/kg/31D-I
TOXIC EFFECTS :
Cardiac - other changes Cardiac - changes in heart weight Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 19,1334,1985 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
4400 ug/kg/3H
SEX/DURATION :
female 21 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - hepatobiliary system Reproductive - Specific Developmental Abnormalities - endocrine system
REFERENCE :
JPEMAO Journal of Perinatal Medicine. (Walter de Gruyter, Inc., 200 Saw Mill River Rd., Hawthorne, NY 10532) V.1- 1973- Volume(issue)/page/year: 9,293,1981 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5237 No. of Facilities: 74 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 2349 (estimated) No. of Female Employees: 1218 (estimated)

 Safety Information

Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning
Hazard Statements H302-H410
Precautionary Statements P301 + P312 + P330
Hazard Codes Xn: Harmful;
Risk Phrases R22
Safety Phrases 36
RIDADR UN 3077 9 / PGIII
WGK Germany 3
RTECS DO8225000

 Synonyms

Dilavase
suprilent
vasoplex
Vadosilan
Vasotran
Divadilan
EINECS 209-443-6
Isoxsuprin-hydrochlorid
vasodilan
isoxsuprine*HCl
chlorhydrate d'isoxsuprine
Navilox
MFCD00058069
Duvadilan
isolait
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