66 research outputs found

    ์น˜๊ณผ ์ž„ํ”Œ๋ž€ํŠธ ์‹๋ฆฝ์„ ์œ„ํ•œ ๋“œ๋ฆด๋ง์‹œ ๋ฐœ์ƒํ•˜๋Š” ์—ด์˜ ์ง์ ‘ ์ธก์ •

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    ํ•™์œ„๋…ผ๋ฌธ (๋ฐ•์‚ฌ) -- ์„œ์šธ๋Œ€ํ•™๊ต ๋Œ€ํ•™์› : ์น˜์˜ํ•™๋Œ€ํ•™์› ์น˜์˜๊ณผํ•™๊ณผ, 2021. 2. ์•ˆ์ง„์ˆ˜.The aim of present study is to evaluate the heat production directly when performing osteotomy for implant placement. We made a comparison the values that were acquired through this study with the other from the former studies. A specially designed bur was manufactured and applied for the present study. A thermosensor was installed inside the drill which is made of stainless steel utilizing a 18-gauge needle and mercury containing slip ring. In addition, three thermocouples were placed into the artificial bone model with various depth of 10mm, 5mm, and 1mm. The location of the thermocouples inside the bone was as close as of 0.5mm from the lateral margin of the osteotomy site. The diameter of the drill was 3.4mm. Rotational speed of the drill was ranged from 500rpm to 2000 rpm. The experiment of drilling was repeated 10 times, and the average was analyzed. The temperature measured from the inside of the drill surged up very quick, and the temperature inside the bone achieved its highest peak when the measured temperature from the drill initiate to drop. The maximum inner temperature observed from the bone model was at the depth of 10mm. The trends of the temperature alteration shared similarity regardless of the drilling speed. Present study elucidates that there is significant discrepancy between the highest temperature measured from the drill and the temperature inside the bone, the value observed from the former is much higher than the latter.๋ณธ ์—ฐ๊ตฌ์˜ ๋ชฉ์ ์€ ์ž„ํ”Œ๋ž€ํŠธ ์‹๋ฆฝ์„ ์œ„ํ•ด ๋“œ๋ฆด๋ง์„ ์‹œํ–‰ํ•  ๋•Œ ๋ฐœ์ƒํ•˜๋Š” ์—ด์„ ์ง์ ‘์ ์œผ๋กœ ์ธก์ •ํ•˜๋Š” ๊ฒƒ์ด๋‹ค. ์‹คํ—˜์„ ํ†ตํ•ด ์ธก์ •๋œ ์˜จ๋„๋Š” ์น˜์กฐ๊ณจ ๋‚ด์—์„œ ์ธก์ •๋˜์—ˆ๋˜ ๋ฐฉ์‹์œผ๋กœ ์ด์ „์— ์ˆ˜ํ–‰๋˜์—ˆ๋˜ ์—ฐ๊ตฌ์—์„œ์˜ ์˜จ๋„์™€ ๋น„๊ต ํ•˜์˜€๋‹ค. ๋“œ๋ฆด์˜ ์˜จ๋„๋ณ€ํ™”๋Š” 18๊ฒŒ์ด์ง€ needle๊ณผ ์ˆ˜์€์„ ํฌํ•จํ•˜๋Š” slip ring์„ ์‚ฌ์šฉํ•˜์—ฌ ์Šคํ…Œ์ธ๋ฆฌ์Šค ์Šคํ‹ธ ๋“œ๋ฆด์˜ ๋‚ด๋ถ€์— ์—ด-์„ผ์„œ๋ฅผ ์‚ฝ์ž…ํ•˜๋Š” ๋ฐฉ์‹์œผ๋กœ ์ธก์ •ํ•˜์˜€๋‹ค. ๊ทธ๋ฆฌ๊ณ  ์„ธ๊ฐœ์˜ ์ถ”๊ฐ€์ ์ธ ์—ด-์„ผ์„œ๋ฅผ ์น˜์กฐ๊ณจ ๋ชจ๋ธ ์— ์‚ฝ์ž…์‹œ์ผฐ๊ณ  ๊ฐ๊ฐ 10 mm, 5 mm, 1 mm ๋“ฑ์˜ ๋‹ค๋ฅธ ๋‘๊ป˜๋กœ ์น˜์กฐ๊ณจ ๋ชจ ๋ธ์— ์œ„์น˜์‹œํ‚ค๋„๋ก ํ•˜์˜€๋‹ค. ์—ด-์„ผ์„œ๋“ค์€ ๋“œ๋ฆด ์ง๊ฒฝ 3.4 mm๋กœ ์น˜์กฐ๊ณจ ๋ชจ๋ธ์— ํ˜•์„ฑ๋œ ๊ตฌ๋ฉ๊ณผ ์ˆ˜ํ‰์ ์œผ๋กœ 0.5 mm ๋–จ์–ด์ ธ ์œ„์น˜ํ•˜๋„๋ก ํ•˜์˜€๋‹ค. 30 ๋“œ๋ฆด์˜ ํšŒ์ „ ์†๋„๋Š” 500 rpm 1200 rpm, 2000 rpm ๋“ฑ์œผ๋กœ ๋‹ค์–‘ํ•˜๊ฒŒ ํšŒ ์ „์‹œํ‚ค๋„๋ก ํ•˜์˜€๋‹ค. ๊ฐ๊ฐ์˜ ๋“œ๋ฆด๋ง ์‹œ์ˆ ์€ 10 ํšŒ์”ฉ ๋ฐ˜๋ณตํ•˜์—ฌ ๊ทธ ํ‰๊ท ์„ ๊ณ„์‚ฐํ•˜์˜€๋‹ค. ๋“œ๋ฆด์—์„œ ์ธก์ •๋œ ์˜จ๋„๋Š” ๋“œ๋ฆด๋ง ์‹œ์ž‘ ํ›„ ๊ธ‰์ž‘์Šค๋Ÿฝ๊ฒŒ ์ฆ๊ฐ€ํ•˜ ์˜€๊ณ  ๋“œ๋ฆด์˜ ์˜จ๋„๊ฐ€ ๊ฐ์†Œํ•˜๊ธฐ ์‹œ์ž‘ํ•œ ํ›„์— ์น˜์กฐ๊ณจ ๋ชจํ˜•์— ์‚ฝ์ž…๋œ ์—ด์„ผ์„œ ์—์„œ ์ธก์ •๋œ ์˜จ๋„๊ฐ€ ์ตœ๋Œ€์น˜์— ๋„๋‹ฌํ•˜์˜€๋‹ค. ๊นŠ์ด์— ๋”ฐ๋ฅธ ์˜จ๋„๋ณ€ํ™”๋ฅผ ๋ณด๋ฉด ๊นŠ์ด 10 mm์—์„œ ์น˜์กฐ๊ณจ ๋ชจ๋ธ์—์„œ ์ธก์ •๋œ ์ˆ˜์น˜ ์ค‘์—์„œ ์ตœ๋Œ€์น˜๋ฅผ ๋ณด์˜€๋‹ค. ์น˜์กฐ๊ณจ ๋ชจ๋ธ์—์„œ์˜ ๋“œ๋ฆด๋ง ์‹œ ์˜จ๋„ ๋ณ€ํ™”์˜ ์ถ”์„ธ๋ฅผ ๋ณด๋ฉด ๋‹ค์–‘ํ•œ ๋“œ๋ฆด ํšŒ ์ „์ˆ˜์—๋„ ์—ด๋ณ€ํ™”์˜ ํŒจํ„ด์€ ์ฆ๊ฐ€ํ–ˆ๋‹ค๊ฐ€ ์ตœ๋Œ€์น˜์— ๋‹ค๋‹ค๋ฅด๊ณ  ์„œ์„œํžˆ ๊ฐ์†Œํ•˜ ๋Š” ํ˜•ํƒœ๋กœ ์œ ์‚ฌํ•œ ์–‘์ƒ์„ ๋ณด์˜€๋‹ค. ์‹ค์ œ ์ด๋ฒˆ ์—ฐ๊ตฌ์—์„œ ์ธก์ •๋œ ๋“œ๋ฆด๊ณผ ์น˜ ์กฐ๊ณจ ๋ชจ๋ธ ๊ณ„๋ฉด์—์„œ์˜ ์ตœ๋Œ€ ์˜จ๋„๋Š” ๊ณจ ๋‚ด๋ถ€์—์„œ ์ธก์ •์„ ์‹œํ–‰ํ•œ ์ด์ „ ์—ฐ ๊ตฌ๋“ค์—์„œ ๋ณด๊ณ ๋œ ์ธก์ • ์ˆ˜์น˜๋“ค ๋ณด๋‹ค ์œ ์˜ํ•˜๊ฒŒ ๋†’๊ฒŒ ์ธก์ •๋˜์—ˆ๋‹ค.1. Introduction 1 2. Material and Methods 4 2.1. Themosensor located in bone for the heat evaluation 4 2.2. Themosensor located in contact with the proximal end of the drill for the heat evaluation 4 2.3. Rotating themosensor in complete-contact with the drill for the improved heat evaluation 5 2.4. Equipment set up 7 2.5. Statistical Analysis 8 3. Results 10 4. Dicussion 16 5. Conclusion 22 6. References 23 7. Korean Abstract 29Docto

    Hinman Syndrome: Long Term Follow up of 14 Cases

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    Purpose Hinman syndrome is the most severe form of nonneurogenic neurogenic bladder causing damage of the upper urinary tract. Fourteen patients with Hinman syndrome followed at our institution were evaluated for their clinical characteristics and prognosis. Here we report the findings of this series of patients for this poorly understood syndrome. Materials and Methods The medical records of 14 patients, 8 boys and 6 girls, diagnosed with Hinman syndrome from March 1993 to June 2006 were reviewed. The mean duration of follow up was 69 months. The ultrasonography, 99m Tc-dimercaptosuccinic acid renal scan (DMSA), voiding cystourethrogram (VCUG), and urodynamic study (UDS) results were retrospectively analyzed and efficacy of each treatment method was evaluated based on the medical records on follow up. Results Hydronephrosis of grade III or greater on ultrasonography and renal scarring of both kidneys on the DMSA renal scan were observed in 12 and 14 patients, respectively. Severe bladder trabeculation and high grade VUR (IV, V) were observed on the VCUG in 14 and 8 patients, respectively. Decreased bladder compliance on the UDS was noted in 13 and detrussor-sphincter dyssynergia (DSD) was observed in eight. Medical treatment was not effective in all 14 cases and six patients who underwent botulinum injection of the bladder were unresponsive to that treatment as well. In spite of conservative treatments such as clean intermittent catheterization (CIC), seven patients eventually underwent bladder augmentations after a mean period of thirty-seven months from diagnosis because of concern about the loss of bladder capacity and renal function. One patient who did not perform CIC progressed to end-stage renal disease and had to be transferred to pediatric nephrology for dialysis. Conclusions Patients diagnosed with the Hinman syndrome were treated similar to patients with neurogenic bladder. However, from the long-termfollow up data at our outpatient clinic, many patients eventually had bladder augmentation to prevent further loss of bladder capacity and renal function. Therefore, urologists must not hesitate in performing such treatment when necessary.ope

    Association between CCR5 Promoter Polymorphisms and Hepatitis B Virus Infection

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    Background/Aims: Immunogenetic factors may play a role in determining the susceptibility of an individual to viral infection. CCR5 promoter polymorphisms are known to be associated with HIV infection. However, there has been no report on the association between CCR5 promoter polymorphism and HBV infection. Therefore, we investigated the relationship between the CCR5 promoter polymorphism and HBV infection. Methods: A total of 377 patients were classified into two groups according to their HBV infection status: โ‘  the spontaneous clearance group (SC); HBsAg (-), anti-HBc (+), anti-HBs (+) โ‘ก the chronic HBsAg (+) carrier group (CC); HBsAg (+), anti-HBc (+), anti-HBs (-). CCR5 polymorphisms were detected by employing matrix-assisted laser desorption/ionization time of flight mass spectrometry (MALDI-TOF MS)-based SNP scoring assay, termed Restriction Fragment Mass Polymorphism (RFMP), which exploits the differences in molecular masses between the common allele and rare allele bases of interest. Results: We found that the genotype frequencies of CCR5 A59029G significantly differed between the SC group (n=138) and CC group (n=239) (P<0.05). The CCR5 59029A allelic genotype was associated with an increased risks of chronic infection rather than spontaneous clearance (P=0.002), and the presence of the CCR5 59029G allele was significantly associated with the spontaneous clearance of HBV (P=0.001). Strong linkage disequilibrium between the CCR5-59029 and the CCR5-59353 polymorphic variants was identified. None of the 377 subjects had the CCR5-32 bp deletion mutation. Conclusions: The CCR5 promoter polymorphisms at position 59029 might play a role in the clearance of HBV infection. This primary experimental evidence needs further studies to clarify the clinical usefulness of CCR5 promoter polymorphisms as a target for the screening or treatment of HBV infection.ope

    Recombinant interferon-Beta-1alpha plus ribavirin for the treatment of chronic HCV infection: a prospective, randomized, comparative pilot study

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    BACKGROUND/AIMS: Interferon beta (IFN-beta) has been shown to have antiviral activity, and thus could be useful in treating viral infections. Therefore, we compared the efficacy and safety of recombinant IFN-beta (IFN-beta-1a) plus oral ribavirin versus interferon alpha (IFN-alpha) plus ribavirin therapy for the treatment of chronic hepatitis C (HCV). METHODS: Twenty treatment-naรฏve patients were randomized into two equal-sized treatment groups. Both IFN-beta-1a (44 microg) and IFN-alpha (3 MIU) were given subcutaneously three times a week, while ribavirin was given orally at 1,000-1,200 mg/day. Patients were treated for 24 weeks and followed for an additional 24 weeks. RESULTS: After 24 weeks of treatment, six (60%) and four patients (40%) in the IFN-beta-1a group and IFN-alpha groups, respectively, achieved viral clearance. The sustained virological response (SVR) at the end of the observation period was similar in both groups (40%). However, the baseline viral load was significantly higher (p=0.034) in the IFN-beta-1a group than in the IFN-alpha group, and there were more HCV genotype 1 patients in the IFN-beta-1a group (eight versus seven). The IFN-beta-1a group was associated with similar adverse events in terms of frequency and severity. CONCLUSIONS: The SVR rate and safety profile were similar for the combination of IFN-beta-1a and ribavirin and that of IFN-alpha and ribavirinope

    Perirenal Fat Invasion(pT3a) in Renal Cell Carcinoma Less Than 4cm in Size(cT1a): Analysis of the Prognostic and Pathological Implications

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    Purpose: To investigate the incidence and histopathological factors of perirenal fat invasion (pT3a) in cT1a renal cell carcinomas. The implication for postoperative perirenal fat invasion, as a prognostic factor in patients with tumors less than 4cm tumor in size is also discussed. Materials and Methods: Of 503 patients who underwent an operation for a renal cell carcinoma at our institution, between June 1995 and April 2004, we retrospectively reviewed the records of 176 with T1a renal cell carcinomas. We evaluated the pathological grade, cell type, tumor size, location and incidence of perirenal fat invasion using the Fisher's exact test. The overall survival was estimated using the Kaplan-Meier method and log-rank test, and the prognostic factors influencing the survival were estimated using the Cox proportional hazard regression model. Results: In this study, a radical nephrectomy was performed in 128 men and 48 women, with a mean age of 54.6 years, ranging from 23 to 77. The mean follow-up was 31.3 months, ranging from 6 to 106 months. The average size of the renal cell carcinomas was 3.0cm, ranging from 1 to 4cm. The incidence of perirenal fat invasion in the T1a renal cell carcinomas was 5.7% (n=10). The nuclear grade (p<0.001) was a statistically significant factor in the incidence of postoperative perirenal fat invasion. Conclusions: In the patients with a renal cell carcinoma less than 4cm in size (cT1a), those in the postoperative perirenal fat invasion group had a significantly poorer prognosis. The tumor size and Fuhrman nuclear grade were implicated in the incidence of perirenal fat invasion in the T1a renal cell carcinomas. Therefore, in the case of nephron sparing surgery, more precise preoperative staging of the primary tumor is required.ope

    Ovarian Cystadenofibroma in a Patient with Familial Adenomatous Polyposis

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    Familial adenomatous polyposis (FAP) is a hereditary disease characterized by the appearance of numerous polyps in the large bowel with a high potential for malignant transformation unless untreated. A variety of extracolonic manifestations were reported such as osteoma, epidermoid cyst, desmoid tumor, gastroduodenal polyps, small bowel tumor, congenital hypertrophy of the retinal pigment epithelium, hepatobiliary tumor, thyroid tumor, and tumor of 12 the central nervous system. However, the ovarian involvement of FAP as an extracolonic manifestation was very rare and there have been only few reports. We experienced a rare case of ovarian cystadenofibroma in a patient with FAP as an extracolonic manifestation. We also found colon cancer with multiple hepatic metastasis initially manifested as intestinal obstruction in the same patient. Surgical treatment and subsequent chemotherapy for colon cancer and intraoperative radiofrequency ablation of hepatic metastasis were 15 performed.ope

    TRPV1 ๊ธธํ•ญ์ œ ๊ตฌ์กฐํ™œ์„ฑ ์—ฐ๊ตฌ : 2-(4-Methansulfonylaminophenyl) Propanamide ๊ณ„ ๋ฐ 6-5 Fused Heterocyclic Urea/Propanamide ๊ณ„ ์œ ๋„์ฒด ์—ฐ๊ตฌ

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    TRPV1(Transient Receptor Potential Vanilloid 1)์€ ํ†ต๊ฐ ์ž๊ทน์˜ ๋ถ„์ž ๋งค๊ฐœ์ฒด๋กœ์จ ๋ฌด ์ˆ˜์ดˆ ํ†ต๊ฐ ๊ฐ๊ฐ ์‹ ๊ฒฝ ์„ฌ์œ ์ธ C-fiber ์™€ small A-delta fiber ์— ๋ฐœํ˜„ํ•˜๋Š” ์ˆ˜์šฉ์ฒด์ด๋‹ค. TRPV1์€ ๋‹ค์–‘ํ•œ ์™ธ์ธ์„ฑ ์ธ์ž(vanilloid such as Capsaicin and Resiniferatoxin, 42โ„ƒ ์ด์ƒ์˜ ์—ด ๋“ฑ)์™€ ๋‚ด์ธ์„ฑ ์ธ์ž(๋‚ฎ์€ pH, anandamide, arachidonic acid ๋Œ€์‚ฌ์ฒด, bradykinin, ATP, NGF์™€ ๊ฐ™์€ pro-nociceptive ๋Œ€์‚ฌ์ฒด ๋“ฑ)์˜ ๋ฌผ๋ฆฌ์ , ํ™”ํ•™์  ์ž๊ทน์— ์˜ํ•ด ํ™œ์„ฑํ™” ๋˜๋Š” ๋น„์„ ํƒ์ ์ธ ์–‘์ด์˜จ ์ฑ„๋„์ด๋‹ค. ํŠนํžˆ ๋†’์€ Ca2+ ์˜ ํˆฌ๊ณผ๋ฅผ ํ•˜์—ฌ ์ด์˜จ ์ฑ„๋„์ด ํ™œ์„ฑํ™” ๋˜๊ณ , ์ด ํ™œ์„ฑํ™”๋Š” ์„ธํฌ ๋‚ด์— Ca2+ ์˜ ์–‘์ด ์ฆ๊ฐ€๋˜๋ฉฐ ์ผ์ฐจ ๊ฐ๊ฐ ์‹ ๊ฒฝ(primary sensory neurons)์˜ ํฅ๋ถ„์„ ์•ผ๊ธฐ ์‹œ์ผœ ๊ฒฐ๊ตญ ํ†ต์ฆ์„ ์ธ์ง€ํ•˜๊ฒŒ ๋œ๋‹ค. TRPV1 ์ˆ˜์šฉ์ฒด๋Š” ์—ฌ๋Ÿฌ ์กฐ์ง์˜ ์‹ ๊ฒฝ ์„ฌ์œ ์— ์กด์žฌํ•˜๋Š”๋ฐ DRG neuron ์— ๊ฐ€์žฅ ๋งŽ์ด ๋ถ„ํฌํ•˜๋ฉฐ ์ฒ™์ˆ˜์—์„œ๋„ ๋ฐœ๊ฒฌ๋˜๊ณ  ์‹œ์ƒํ•˜๋ถ€, ํ•ด๋งˆ, ํ‘์ƒ‰์งˆ ๋“ฑ ๋‡Œ์—์„œ๋„ ๋งŽ์ด ๋ถ„ํฌ๋˜์–ด ์žˆ์œผ๋ฉฐ ์‹ ์žฅ, ๋ฐฉ๊ด‘ ๋“ฑ์—์„œ๋„ ๋ฐœ๊ฒฌ๋œ๋‹ค. TRPV1 ์ˆ˜์šฉ์ฒด๋Š” ๋‹ค์–‘ํ•œ ํ†ต์ฆ์˜ ํ†ตํ•ฉ์ž๋กœ์จ ๋ฟ๋งŒ ์•„๋‹ˆ๋ผ ํ†ต์ฆ์˜ ์ „๋‹ฌ๊ณผ modulation ์˜ ์—ญํ• ์ด ์•Œ๋ ค์ง€๊ณ  ์žˆ์œผ๋ฉฐ, ์ด ์ž‘์šฉ์„ ๊ธธํ•ญํ•˜๋Š” ๊ธฐ์ „์˜ ํ™”ํ•ฉ๋ฌผ๋“ค์ด ์ง„ํ†ต์ œ๋กœ ๊ฐœ๋ฐœ๋˜๋Š” ์—ฐ๊ตฌ๊ฐ€ ํ™œ๋ฐœํžˆ ์ง„ํ–‰๋˜๊ณ  ์žˆ๋‹ค. ๋” ๋‚˜์•„๊ฐ€ ์„ ํƒ์ ์œผ๋กœ ์ค‘์ถ”์‹ ๊ฒฝ๊ณ„์˜ ํ˜ˆ์•ก ๋‡Œ๊ด€๋ฌธ(Blood Brain Barrier)์— ํ†ต๊ณผ๊ฐ€ ๊ฐ€๋Šฅํ•œ TRPV1 ์ˆ˜์šฉ์ฒด ๊ธธํ•ญ์ œ์˜ ๊ฐœ๋ฐœ์€ ์ƒˆ๋กœ์šด ํ†ต์ฆํ•™์  ์น˜๋ฃŒ๋กœ ๊ธฐ๋Œ€๋˜๊ณ  ์žˆ๋‹ค. ๋ณธ ์—ฐ๊ตฌ์‹ค์€ 2-(4-Methansulfonylaminophenyl) Propanamide ๊ณ„์—ด์˜ ์œ ๋„์ฒด๋“ค์„ ํ•ฉ์„ฑํ•˜์—ฌ TRPV1 ๊ธธํ•ญํšจ๊ณผ๋ฅผ ๊ฐ–๋Š”, ์ง„ํ†ต์ œ๋กœ์จ ๊ฐ€๋Šฅ์„ฑ ์žˆ๋Š” ์•ฝ๋ฌผ์„ ์ฐพ๋Š” ์—ฐ๊ตฌ๋ฅผ ์ˆ˜ํ–‰ํ•˜์˜€๋‹ค. ๊ทธ๋ฆฌ๊ณ  ๋‹ค๊ตญ์  ์ œ์•ฝํšŒ์‚ฌ์ธ ์•„๋ณดํŠธ (Abbott Inc.) ์‚ฌ์—์„œ ๋„์ถœํ•œ ํ™”ํ•ฉ๋ฌผ ABT-102 ์˜ A-region ์ธ indazole ์˜ ๊ตฌ์กฐ๋ณ€ํ™˜์„ ํ•˜์—ฌ ์ƒˆ๋กœ์šด A-region ์„ ์„ค๊ณ„ ํ•˜์˜€๋‹ค. ์ด ์„ค๊ณ„๋ฅผ ๊ธฐ์ดˆ๋กœ ๋ณธ ์—ฐ๊ตฌ์‹ค์€ A-region ์— ๋‹ค์–‘ํ•œ 6-5 Fused Heterocyclic ํ™”ํ•ฉ๋ฌผ์„ (indole, benzimidazole, benzotriazole, benzoxazole, benzothiazole) ํ•ฉ์„ฑํ•˜์˜€๊ณ , ๊ตฌ์กฐ-ํ™œ์„ฑ ๊ด€๊ณ„๋ฅผ ์—ฐ๊ตฌํ•˜์˜€๋‹ค. ํŠนํžˆ 6๊ฐœ์˜ ํ™”ํ•ฉ๋ฌผ์ด 2 nM ์ดํ•˜์˜ ๊ฐ•๋ ฅํ•œ TRPV1 antagonism ์„ ๋‚˜ํƒ€๋‚ด์—ˆ๊ณ , ์ง„ํ†ต์ œ๋กœ์จ ๊ฐ€๋Šฅ์„ฑ ์žˆ๋Š” ์•ฝ๋ฌผ ํ›„๋ณด ๋ฌผ์งˆ์„ ๋ณธ ์—ฐ๊ตฌ๋ฅผ ํ†ตํ•ด ๋ฐœ๊ฒฌํ•˜์˜€๋‹ค.The transient receptor potential cation channel subfamily V member 1 (TRPV1), also known as the capsaicin receptor and the vanilloid receptor 1, is a protein that, in human, is encoded by the TRPV1 gene. TRPV1 is primarily expressed on, small myelinated and unmyelinated medium size, sensory neurons in dorsal root and trigeminal ganglia, where sensory neurons cluster. TRPV1 is a non-selective cation channel that may be activated by a wide variety of exogenous and endogenous physical and chemical stimuli. The best-known activators of TRPV1 are heat greater than 43 0C and capsaicin, the pungent compound in hot chili peppers and resiniferatoxin (RTX). The activiation of TRPV1 leads painful, burning sensation. Its endogenous activators include low pH (acidic conditions), the endocannabinoid anandamide, N-arachionyl dopamine. In addition TRPV1 activation can be potentiated by pro-nociceptive mediators such as bradykinin, ATP, NGF, and others. TRPV1 receptors are found mainly in the nociceptive neurons of the peripheral nervous system, but they have also been described in many other tissues, including the central nervous system. TRPV1 receptors are also found in muscles, joints, the urinary bladder and kidneys. The functional activity of TRPV1 has been demonstrated, within the central nervous system, in the spinal cord and specific sites in the brain including the hypothalamus, cerebellum, locus coeruleus, periaqueductal grey and cortex. Activation of TRPV1 sets off an influx of calcium and sodium, ions which in turn initiates a cascade of events that result in memebrane depolarization, neuronal firing and transduction of neural impulses. TRPV1 phosphorylates as a response to several algesic agents, resulting in a lower threshold of channel activation. Some substances such as bradykinin, nerve growth factor and protons have been reprted to sensitize the TRPV1 receptor. Activation of TRPV1 results in the release of pro-nociceptive peptides, which decreases when treated with TRPV1 antagonists. In general, most channel antagonists bind in the pore region, interacting with residues from all four monomers of the tetrameric channe. The siginificant role of this receptor plays as the transmission and modulation of pain (nociception), as well as the integration of diverse painful stimuli. For this reason, the discovery of small molecule antagonists of TRPV1 has been the subject of intense investigations among many pain research groups. Further more recently, it was demonstrated that the analgesic profile of TRPV1 antagonists can be siginificantly broadened if the receptor blockade occurs both in the peripheral and in the central nervous system. Therefore, development of selective TRPV1 receptor antagonists with good CNS penetration presents an important opportunity to treat a variety of pathological pain states. For finding promising analgesic with excellent antagonism, studies are performed not only by desigining and synthesizing TRPV1 receptor ligands which have 2-(4-methasulfonyaminophenyl) propanamide and 6-5 fused heterochcylic at A-region, urea/propanamide at B-region, but also by introducing various substituent based on rational method.Docto

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