Spectinomycin

Modify Date: 2024-01-04 06:12:09

Spectinomycin structure	Common Name	Spectinomycin
	CAS Number	1695-77-8	Molecular Weight	332.35000
	Density	1.43 g/cm3	Boiling Point	583.1ºC at 760 mmHg
	Molecular Formula	C₁₄H₂₄N₂O₇	Melting Point	185ºC
	MSDS	USA	Flash Point	N/A

Use of Spectinomycin

Spectinomycin is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin is also a noncompetitive inhibitor of td intron RNA[1][2][3][4][5].

Name	spectinomycin
Synonym	More Synonyms

Description	Spectinomycin is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin is also a noncompetitive inhibitor of td intron RNA[1][2][3][4][5].
Related Catalog	Research Areas >> Infection Signaling Pathways >> Anti-infection >> Bacterial
Target	bacterial ribosomal subunit[5]
In Vitro	Spectinomycin selectively inhibits protein synthesis in cells and in extracts of Escherichia coli. Spectinomycin (50 μg/mL) inhibits Escherichia coli growth rapidly and reversibly, and suppresses amino acid incorporation immediately[1]. Spectinomycin (1 μg/mL or 3 μM) inhibits polypeptide synthesis directed either by endogenous messenger RNA or by MS-2 bacteriophage RNA, with maximum inhibition of 70-80% in extracts of Escherichia coli[1]. Spectinomycin blocks the translocation of peptidyl-tRNAs from A-site to P-site by inhibiting the binding of elongation factor G to the ribosome[2]. Spectinomycin interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially makes it inactive[2]. Spectinomycin exhibits splicing inhibition and dependent on pH changes and Mg2+ concentration, indicating electrostatic interactions with the intron RNA[3].
In Vivo	Spectinomycin (20 mg/kg; i.m.; 20-100 mg/kg; 9 d) shows the safety in healthy chicks[4]. Spectinomycin (10 mg/kg; i.v.; single dose) has the major elimination pathway by renal excretion, approximately 55% is excreted into the urine in unchanged form[5]. Pharmacokinetics of Spectinomycin in Rat[5] Parameter C0 (μg/mL) AUC0-∞ (μg•h/mL) Vd (L/kg) CL (L/h/kg) MRT (h) T1/2α (h) T1/2β (h) T1/2γ (h) fe CLrenal (L/h/kg) Eratio Non atrioventricular analysis 44.3 16.8 0.756 0.602 0.757 / / / 0.553 0.359 1.00 Three-compartment model 37.8 15.7 0.747 0.649 1.11 / 0.237 0.754 19.5 / / Animal Model: Arbor Acres plus broiler chicks (15-day-old)[4] Dosage: 20 mg/kg, 60 mg/kg, 100 mg/kg Administration: Intramuscular injection (chest muscles); 9 days Result: Showed biosecurity of 20 mg/kg by complete blood count, biochemical parameters, histopathological, clinical signs, body weight gain, and feed conversion ratio (FCR). Resulted minor toxicity of 60 mg/kg.
References	[1]. Davies J, et al. Inhibition of protein synthesis by spectinomycin. Science. 1965 Sep 3;149(3688):1096-8. [2]. Brink MF, et al. Spectinomycin interacts specifically with the residues G1064 and C1192 in 16S rRNA, thereby potentially freezing this molecule into an inactive conformation. Nucleic Acids Res. 1994 Feb 11;22(3):325-31. [3]. Park IK, et al. Spectinomycin inhibits the self-splicing of the group 1 intron RNA. Biochem Biophys Res Commun. 2000 Mar 16;269(2):574-9. [4]. Khan EA, et al. Safety evaluation study of lincomycin and spectinomycin hydrochloride intramuscular injection in chickens. Toxicol Rep. 2022 Jan 29;9:204-209. [5]. Madhura DB, et al. Pharmacokinetic profile of spectinomycin in rats. Pharmazie. 2013 Aug;68(8):675-6.

Density	1.43 g/cm3
Boiling Point	583.1ºC at 760 mmHg
Melting Point	185ºC
Molecular Formula	C₁₄H₂₄N₂O₇
Molecular Weight	332.35000
Exact Mass	332.15800
PSA	129.51000
Vapour Pressure	5.05E-16mmHg at 25°C

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UQ0332500

CHEMICAL NAME :: 4H-Pyrano(2,3-b)(1,4)benzodioxin-4-one, decahydro-4a,7,9-trihydroxy-2-methyl-6,8- bis(methylamino)-

CAS REGISTRY NUMBER :: 1695-77-8

LAST UPDATED :: 199706

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C14-H24-N2-O7

MOLECULAR WEIGHT :: 332.40

WISWESSER LINE NOTATION :: T C666 BO DO GV IOTJ E1 HQ KM1 LQ MM1 NQ

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 :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 111,265,1972

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5724 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 111,265,1972

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 20 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AACHAX Antimicrobial Agents and Chemotherapy (1961-70). (Ann Arbor, MI) 1961-70. For publisher information, see AMACCQ. Volume(issue)/page/year: -,507,1961

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 85FZAT "Index of Antibiotics from Actinomycetes," Umezawa, H. et al., eds., Tokyo, Univ. of Tokyo Press, 1967 Volume(issue)/page/year: -,105,1967

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AACHAX Antimicrobial Agents and Chemotherapy (1961-70). (Ann Arbor, MI) 1961-70. For publisher information, see AMACCQ. Volume(issue)/page/year: -,507,1961

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Behavioral - muscle weakness Behavioral - ataxia Gastrointestinal - nausea or vomiting

REFERENCE :: AACHAX Antimicrobial Agents and Chemotherapy (1961-70). (Ann Arbor, MI) 1961-70. For publisher information, see AMACCQ. Volume(issue)/page/year: -,507,1961

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AACHAX Antimicrobial Agents and Chemotherapy (1961-70). (Ann Arbor, MI) 1961-70. For publisher information, see AMACCQ. Volume(issue)/page/year: -,507,1961

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: >800 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia

REFERENCE :: AACHAX Antimicrobial Agents and Chemotherapy (1961-70). (Ann Arbor, MI) 1961-70. For publisher information, see AMACCQ. Volume(issue)/page/year: -,507,1961

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >40 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - other changes

REFERENCE :: AACHAX Antimicrobial Agents and Chemotherapy (1961-70). (Ann Arbor, MI) 1961-70. For publisher information, see AMACCQ. Volume(issue)/page/year: -,507,1961 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X7549 No. of Facilities: 14 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 432 (estimated) No. of Female Employees: 203 (estimated)