S-MTC
目录号 : GC31243
S-MTC是一种选择性的I型一氧化氮合酶(NOS)抑制剂。
Cas No.:156719-41-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
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Cell experiment: | Mixed cortical glial and neuronal cultured cells are prepared from E15 to E18 embryos obtained from Spargue-Dawley rats. On day 7 after plating, the culture medium is removed and replaced with freshly prepared culture medium in the presence of either Aβ1-42 (1, 5, 10, or 20 μM), Aβ42-1, or peroxynitrite (100 or 200 μM) with or without either NG-nitro-L-arginine (L-NOARG,10 or 100 μM), S-MTC (10 or 100 μM), N-iminoethyl-L-lysine (10 or 100 μM), N-(3-(aminomethyl)benzyl)acetamidine (1400W,1 or 5 μM), 2-(4-carboxyphenyl)-4, 4, 5, 5-tetramethylimidazoline-1-oxyl-3-oxide (carboxy-PTIO,10 or 100 μM), or 6-hydorxy-2,5,7,8-tetramethylchroman-2-carboxylic acid (10 or 100 μM) alone or in combination. The cultured cells are then incubated for 20 h. For the time-course studies, the cultured cells are pre-treated with the described culture medium containing Aβ1-42 (10 μM). Either L-NIL (100 μM), L-NOARG (100 μM), 1400W (5 μM), S-MTC (100 μM), carboxy-PTIO (100 μM) or Trolox (100 μM) are administered at 1, 4, and 8 h later. Assessments are carried out 20 h after Aβ1-42 administration. The viability of cultured cells is evaluated by using MTT and neutral red colorimetric assays. MTT reduction and NR uptake are quantified at 570 and 540 nm, respectively, by using a micro-plate reader[1]. |
Animal experiment: | mice[2]Male NIH Swiss mice, weighing 18-22 g, are used. S-MTC (1.0 μg/mouse) is administered i.c.v. (15-min pretreatment time). In one set of experiments (#1, #2, and #3), opioid antagonists and NOS-inhibitors are administered 15–30 min prior to the 60-min HBO2 treatment (180 min prior to antinociceptive testing). In another experiment (#4), opioid antagonist and NOS-inhibitor pretreatment is administered 60 min following cessation of the 60-min HBO2 treatment (15–30 min prior to antinociceptive testing). For i.p. or s.c. pretreatments, the volume of injection is 0.1 mL/10 g body weight with control animals receiving an i.p. or s.c. injection of vehicle (sterile saline) only. For i.c.v. pretreatments, the volume of microinjection is 5.0 μL per mouse with control animals receiving an i.c.v. microinjection of vehicle (sterile saline) only.Rats[3]Male, Sprague-Dawley rats (350-450 g) are used. On the day after catheterisation (day 1), animals (n=7) receive bolus i.v. injections (0.1 mL) of either saline (vehicle), and 0.3 and 3 mg/kg S-MTC (n=4), or 0.1, 1 and 10 mg/kg S-MTC (n=3). On day 3, the dose regimen is switched to ensure that each animal has received all the doses of S-MTC. On each day, drugs are given in ascending dose-order, and at least 60 min is allowed between doses. The intervening day (day 2) is allowed for wash-out of any drug effects. |
References: [1]. Law A, et al. Neuroprotective and neurorescuing effects of isoform-specific nitric oxide synthase inhibitors, nitric oxide scavenger, and antioxidant against beta-amyloid toxicity. Br J Pharmacol. 2001 Aug;133(7):1114-24. | |
S-MTC is a selective type I nitric oxide synthase (NOS) inhibitor.
S-MTC (10 or 100 μM) reduces cellular NO release in the absence of Aβ1-42. At 100 μM, S-MTC decreases cell viability. S-MTC (100 μM) significantly lowers nitrite production (11.2±1.1 μM) when compared to control (no NOS inhibitor exposure; 19.6±1.2 μM). Nitrite productions after Aβ1-42 and L-NOARG (100 μM) or Aβ1-42 and S-MTC (100 μM) treatments are significantly lower than Aβ1-42 alone (33.5±2.0 and 34.5±1.6 μM, respectively). S-MTC (100 μM) is able to significantly reduce nitrite production (25.2±1.1 μM) as compared to Aβ1-42 treatment alone (38.3±2.7 μM), when administered after Aβ1-42 at the 1 h time point. S-MTC (100 μM) concentration decreases both MTT (87±1% of control) and NR (80±1% of control, respectively) levels. The co-administration of S-MTC (100 μM) and Aβ1-42 significantly reverses the effects of Aβ1-42 alone (72±2% vs 61±2% of control)[1].
S-MTC (S-methyl-L-thiocitrulline) is a selective neuronal NOS-inhibitor. Following pretreatment with S-MTC (i.c.v.), the HBO2-induced antinociception is significantly antagonized. In Experiment #2, different groups of mice are pretreated with naltrexone hydrochloride (NTX) (3.0 mg/kg, i.p.), L-NAME (1.0 μg/mouse, i.c.v.), S-MTC (1.0 μg/mouse, i.c.v.) or N5-(1-iminoethyl)-L-ornithine (L-NIO) (3.0 mg/kg, s.c.) 15-30 min prior to HBO2 treatment. The antinociceptive effect assessed 90 min after HBO2 treatment is completely abolished by NTX and L-NAME, antagonized by two-thirds by S-MTC and largely unaffected by L-NIO (F=25.57, p
[1]. Law A, et al. Neuroprotective and neurorescuing effects of isoform-specific nitric oxide synthase inhibitors, nitric oxide scavenger, and antioxidant against beta-amyloid toxicity. Br J Pharmacol. 2001 Aug;133(7):1114-24. [2]. Zelinski LM, et al. A prolonged nitric oxide-dependent, opioid-mediated antinociceptive effect of hyperbaric oxygenin mice. J Pain. 2009 Feb;10(2):167-72. [3]. Wakefield ID, et al. Comparative regional haemodynamic effects of the nitric oxide synthase inhibitors, S-methyl-L-thiocitrulline and L-NAME, in conscious rats. Br J Pharmacol. 2003 Jul;139(6):1235-43.
| Cas No. | 156719-41-4 | SDF | |
| Canonical SMILES | N[C@@H](CCCNC(SC)=N)C(O)=O | ||
| 分子式 | C7H15N3O2S | 分子量 | 205.28 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.8714 mL | 24.357 mL | 48.714 mL |
| 5 mM | 0.9743 mL | 4.8714 mL | 9.7428 mL |
| 10 mM | 0.4871 mL | 2.4357 mL | 4.8714 mL |
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动物平均体重 | g | |
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Cytologic diagnosis of medullary thyroid carcinoma in the Asia-Pacific region
Background: The accurate preoperative identification of medullary thyroid carcinoma (MTC) is challenging due to the rarity of tumor and variable cytologic appearance. The Asian experience with diagnosing MTC by fine-needle aspiration (FNA) was scarcely reported.
Methods: Cases of MTC with available FNA slides were enrolled from 13 hospitals representing 8 Asia-Pacific countries. Clinicopathological information, including sample preparation technique, staining method, original cytologic diagnosis and review diagnosis were collected.
Results: Of a total of 145 MTC cases retrospectively recruited, 99 (68.3%) were initially interpreted as MTC/suspicious for MTC (S-MTC). The distribution of original FNA diagnostic categories was not associated with the staining method or sample preparation technique. The staining methods used were Papanicolaou, hematoxylin-eosin and Romanowsky stains. Liquid-based cytology (LBC) was used only in three countries. After reviewing all cases, the diagnostic rate of MTC/S-MTC increased to 91.7% (133/145). Cases with initially unrecognized MTC had either marked pleomorphism or cytology mimicking papillary carcinoma or follicular neoplasm. Although LBC provided certain benefits, there was no significant difference in diagnostic accuracy between conventional smear and LBC. Immunocytochemistry was available in 38 cases (26.2%), all of which were correctly recognized as MTC.
Conclusion: Our report summarizes how MTC is handled in contemporary Asian thyroid FNA practice. Although the detection rate of MTC by cytology alone is less satisfactory, integration with ancillary tests could achieve an excellent performance. The recognition of constitutive cytomorphologic features is needed for each cytopreparatory method, which may result in a lower threshold to initiate further workup for MTC.
Polymorphisms of cell cycle control genes influence the development of sporadic medullary thyroid carcinoma
Background: The role of key cell cycle regulation genes such as, CDKN1B, CDKN2A, CDKN2B, and CDKN2C in sporadic medullary thyroid carcinoma (s-MTC) is still largely unknown.
Methods: In order to evaluate the influence of inherited polymorphisms of these genes on the pathogenesis of s-MTC, we used TaqMan SNP genotyping to examine 45 s-MTC patients carefully matched with 98 controls.
Results: A multivariate logistic regression analysis demonstrated that CDKN1B and CDKN2A genes were related to s-MTC susceptibility. The rs2066827*GT+GG CDKN1B genotype was more frequent in s-MTC patients (62.22%) than in controls (40.21%), increasing the susceptibility to s-MTC (OR=2.47; 95% CI=1.048-5.833; P=0.038). By contrast, the rs11515*CG+GG of CDKN2A gene was more frequent in the controls (32.65%) than in patients (15.56%), reducing the risk for s-MTC (OR=0.174; 95% CI=0.048-0.627; P=0.0075). A stepwise regression analysis indicated that two genotypes together could explain 11% of the total s-MTC risk. In addition, a relationship was found between disease progression and the presence of alterations in the CDKN1A (rs1801270), CDKN2C (rs12885), and CDKN2B (rs1063192) genes. WT rs1801270 CDKN1A patients presented extrathyroidal tumor extension more frequently (92%) than polymorphic CDKN1A rs1801270 patients (50%; P=0.0376). Patients with the WT CDKN2C gene (rs12885) presented larger tumors (2.9±1.8 cm) than polymorphic patients (1.5±0.7 cm; P=0.0324). On the other hand, patients with the polymorphic CDKN2B gene (rs1063192) presented distant metastases (36.3%; P=0.0261).
Conclusion: In summary, we demonstrated that CDKN1B and CDKN2A genes are associated with susceptibility, whereas the inherited genetic profile of CDKN1A, CDKN2B, and CDKN2C is associated with aggressive features of tumors. This study suggests that profiling cell cycle genes may help define the risk and characterize s-MTC aggressiveness.
Constitutive Cytomorphologic Features of Medullary Thyroid Carcinoma Using Different Staining Methods
(1) Background: Accurate preoperative identification of medullary thyroid carcinoma (MTC) is challenging due to a spectrum of cytomorphologic features. However, there is a scarcity of studies describing the cytomorphologic features as seen on fine-needle aspiration (FNA) smears prepared using different staining methods. (2) Methods: We performed a retrospective study on MTC cases with available FNA slides from 13 hospitals distributed across 8 Asia-Pacific countries. The differences in the constitutive cytomorphologic features of MTC with each cytopreparatory method were recorded. A comparative analysis of cytologic characteristics was carried out with appropriate statistical tests. (3) Results: Of a total of 167 MTC samples retrospectively recruited, 148 (88.6%) were interpreted as MTC/suspicious for MTC (S-MTC). The staining methods used were Papanicolaou, hematoxylin-eosin, and Romanowsky stains. Seven out of the eleven cytologic criteria can be readily recognized by all three cytopreparatory methods: high cellularity, cellular pleomorphism, plasmacytoid cells, round cells, dyshesive cells, salt-and-pepper chromatin, and binucleation or multinucleation. An accurate diagnosis was achieved in 125 (84.5%) of the 148 samples whose FNAs exhibited five or more atypical features. Conclusions: The present work is the first study on MTC to compare the morphological differences among the cytologic staining techniques. We investigated the constitutive features and the reliability of diagnostic parameters. A feasible scoring system based upon cytomorphologic data alone is proposed to achieve a high degree of diagnostic accuracy.