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Spectinomycin
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Spectinomycin
CAS No. : 1695-77-8
MCE 站:Spectinomycin
产品活性:Spectinomycin 是一种广谱抗生素,可以抑制多种革兰氏阳性和革兰氏阴性细菌的生长。Spectinomycin 通过特异靶向细菌核糖体,干扰蛋白质合成。Spectinomycin 也是 td 内含子 RNA 的非竞争性抑制剂。
研究领域:Anti-infection
作用靶点:Antibiotic | Bacterial
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.
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.
Spectinomycin blocks the translocation of peptidyl-tRNAs from A-site to P-site by inhibiting the binding of elongation factor G to the ribosome.
Spectinomycin interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially makes it inactive.
Spectinomycin exhibits splicing inhibition and dependent on pH changes and Mg2+ concentration, indicating electrostatic interactions with the intron RNA.
In Vivo: Spectinomycin (20 mg/kg; i.m.; 20-100 mg/kg; 9 d) shows the safety in healthy chicks.
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.
Pharmacokinetics of Spectinomycin in Rat
Parameter | C0 (μg/mL) | AUC0-∞ (μgh/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 | / | / |
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