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1.
Radiographics ; 43(5): e220096, 2023 05.
Artículo en Inglés | MEDLINE | ID: mdl-37022958

RESUMEN

New minimally invasive techniques that reduce morbidity while improving lower urinary tract symptoms (LUTS) due to benign prostatic hypertrophy (BPH) have become attractive alternatives for patients, in comparison to traditional techniques such as transurethral resection of the prostate (TURP) and simple prostatectomy. Pre- and postprocedural MRI is not routinely performed for LUTS due to BPH treatments. However, because of the combination of rapidly evolving treatments available for LUTS due to BPH and increasing demand for prebiopsy prostate MRI for detection of clinically significant prostate cancer (PCa), an understanding of procedural techniques and expected changes are important for accurate interpretation of prostate MRI performed after treatment of BPH. The authors discuss the imaging evaluation of LUTS due to BPH and emerging predictors of treatment success. The posttreatment appearance and underlying anatomic changes in the prostate after medical, surgical, and minimally invasive treatments including TURP, simple prostatectomy, laser enucleations and ablations, prostatic urethral lift, water vapor thermal therapy, and prostate artery embolization are detailed. Most procedures reduce prostate volume, notably in the periurethral prostatic tissue. Ablations create areas of necrosis and can distort the normal zonal anatomy between the transition zone and the peripheral zone, and prostate artery embolization creates infarcts in the transition zone. Mechanical prostatic urethral lift devices open the anterior channel at the bladder base but create susceptibility artifacts that can obscure and prevent detection of a lesion in the transition zone. Also discussed are the detection of clinically significant prostate cancer in the postprocedural prostate and imaging of BPH procedure complications such as urethral strictures, abscesses, and hematuria. ©RSNA, 2023 Quiz questions for this article are available in the supplemental material. See the invited commentary by Purysko in this issue.


Asunto(s)
Hiperplasia Prostática , Neoplasias de la Próstata , Resección Transuretral de la Próstata , Masculino , Humanos , Hiperplasia Prostática/diagnóstico por imagen , Hiperplasia Prostática/terapia , Resección Transuretral de la Próstata/métodos , Próstata/diagnóstico por imagen , Próstata/cirugía , Resultado del Tratamiento , Neoplasias de la Próstata/cirugía , Imagen por Resonancia Magnética
2.
Am J Kidney Dis ; 73(4): 552-565, 2019 04.
Artículo en Inglés | MEDLINE | ID: mdl-30777633

RESUMEN

Renal imaging has become a fundamental part of clinical care for patients with kidney disease. Imaging strategies for the kidney have been evolving during the past hundred years and have been even more rapidly changing during the past couple of decades due to the development of modern computed tomographic techniques, magnetic resonance imaging, and more sophisticated ultrasonographic techniques, such as contrast-enhanced ultrasonography. Applying the correct radiologic study for the clinical situation maximizes the diagnostic accuracy of the imaging, and a judicious choice between techniques helps limit radiation dose and potential adverse events. This Core Curriculum outlines the imaging modalities currently in use in radiology departments and is divided into 3 sections: (1) a review of the development of renal imaging and an outline of modalities available to the nephrologist, (2) imaging strategies for select clinical situations, and (3) a discussion of some potential adverse events from imaging, including effects of iodinated contrast on kidney function, risks of gadolinium-based contrast agents in kidney failure, and potential risks of imaging techniques that use ionizing radiation.


Asunto(s)
Riñón/diagnóstico por imagen , Imagen Multimodal/métodos , Obstrucción de la Arteria Renal/diagnóstico , Anciano , Angiografía por Tomografía Computarizada/métodos , Humanos , Angiografía por Resonancia Magnética/métodos , Masculino , Reproducibilidad de los Resultados , Ultrasonografía Doppler/métodos
4.
Can J Urol ; 20(5): 6933-7, 2013 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-24128832

RESUMEN

INTRODUCTION: Partial nephrectomy has a 3%-4% incidence of local treatment failure. This study is to present a series of percutaneous cryoablation for locally recurrent renal cell carcinoma after partial nephrectomy. MATERIALS AND METHODS: Five consecutive patients were referred to our quarternary center's multidisciplinary Small Renal Mass (SRM) Center for assessment after failure of partial nephrectomy. Tumor size and location was noted. CT-guided cryoablation was performed using an argon/helium-based system (Healthtronics, Austin, Texas, USA). Patients were admitted overnight for observation. Patients were followed with serial imaging, laboratory tests and examination at our SRM Center. Tumor size, location, and nephrometry scores were documented for each patient. RESULTS: Four tumors were endophytic and one was exophytic. The median tumor size was 2.2 cm (1.8 cm-4.0 cm). Nephrometry scores were 8a, 7x, 4p, 6x, 7p, and 6p prior to cryoablation. Median follow up after cryoablation was 32 months (20-39 months). One patient with a 4.0 cm endophytic tumor developed a second recurrence measuring 2.9 cm 13 months following ablation, which was managed successfully with repeat cryoablation with no evidence of disease after an additional 19 months of follow up. Two patients developed self-limited hematuria which was conservatively managed. There were no other complications, and all patients remained at their pretreatment performance status. CONCLUSIONS: Percutaneous cryoablation appears to be a safe and effective nephron-sparing modality for control of locally recurrent disease following partial nephrectomy. Most recurrent tumors are endophytic. One patient suffered a second local recurrence, which was managed successfully with repeat cryoablation.


Asunto(s)
Carcinoma de Células Renales/cirugía , Criocirugía/métodos , Neoplasias Renales/cirugía , Nefrectomía/métodos , Nefronas/cirugía , Tratamientos Conservadores del Órgano/métodos , Administración Cutánea , Anciano , Anciano de 80 o más Años , Carcinoma de Células Renales/patología , Femenino , Estudios de Seguimiento , Humanos , Incidencia , Neoplasias Renales/patología , Masculino , Persona de Mediana Edad , Clasificación del Tumor , Recurrencia Local de Neoplasia/epidemiología , Recurrencia Local de Neoplasia/cirugía , Tomografía Computarizada por Rayos X , Insuficiencia del Tratamiento , Resultado del Tratamiento
5.
Abdom Radiol (NY) ; 48(1): 127-135, 2023 01.
Artículo en Inglés | MEDLINE | ID: mdl-34743232

RESUMEN

Primary biliary cholangitis is a rare progressive chronic inflammation of the medium and small bile ducts that abdominal radiologists may encounter, particularly if working in a tertiary setting or at a transplant center. This brief review covers current thinking about the pathophysiology and presentation of the disease, as well as the current diagnostic criteria in use by hepatologists. Imaging strategies for diagnosis will be reviewed as well as current treatment strategies and the use of imaging in monitoring response to treatment, including image-guided elastography.


Asunto(s)
Cirrosis Hepática Biliar , Humanos , Conductos Biliares
6.
Abdom Radiol (NY) ; 48(1): 106-126, 2023 01.
Artículo en Inglés | MEDLINE | ID: mdl-35201397

RESUMEN

Pathologies of the biliary tree include a wide-spectrum of benign and malignant processes. The differential for benign disease includes congenital and acquired disease with variable prognosis and management pathways. Given the ability to mimic malignancy, benign processes are difficult to diagnose by imaging. Direct cholangiography techniques with tissue sampling are the gold standards for the diagnosis of benign and malignant biliary pathologies. Non-invasive imaging with ultrasound offers a first-line diagnostic tool while MRI/MRCP offers higher specificity for identifying underlying pathology and distinguishing from malignant disease. In this review, we focus on the imaging appearance of dilatation, cystic anomalies obstruction, inflammation, ischemia, strictures, pneumobilia, and hemobilia to help construct a differential for benign processes.


Asunto(s)
Enfermedades de las Vías Biliares , Sistema Biliar , Humanos , Colangiopancreatografia Retrógrada Endoscópica/métodos , Colangiografía/métodos , Imagen por Resonancia Magnética/métodos , Ultrasonografía , Sensibilidad y Especificidad , Enfermedades de las Vías Biliares/diagnóstico por imagen
7.
Abdom Radiol (NY) ; 48(6): 1921-1932, 2023 06.
Artículo en Inglés | MEDLINE | ID: mdl-36790454

RESUMEN

The rising incidence combined with pregnancy-related physiological changes make gallbladder and biliary pathology high on the differential for pregnant patients presenting with right upper abdominal pain. Imaging plays a crucial role in determining surgical versus non-surgical management in pregnant patients with biliary or gallbladder pathology. Ultrasound (first-line) and magnetic resonance with magnetic resonance cholangiopancreatography (second-line) are the imaging techniques of choice in pregnant patients with suspected biliary pathology due to their lack of ionizing radiation. MRI/MRCP offers an excellent non-invasive imaging option, providing detailed anatomical detail without known harmful fetal side effects. This article reviews physiological changes in pregnancy that lead to gallstone and biliary pathology, key imaging findings on US and MRI/MRCP, and management pathways.


Asunto(s)
Sistema Biliar , Vesícula Biliar , Embarazo , Femenino , Humanos , Vesícula Biliar/diagnóstico por imagen , Vesícula Biliar/patología , Pancreatocolangiografía por Resonancia Magnética/métodos , Imagen por Resonancia Magnética , Ultrasonografía
8.
Abdom Radiol (NY) ; 48(1): 166-185, 2023 01.
Artículo en Inglés | MEDLINE | ID: mdl-36289069

RESUMEN

Liver transplantation is a potentially curative treatment for patients with acute liver failure, end-stage liver disease, and primary hepatic malignancy. Despite tremendous advancements in surgical techniques and immunosuppressive management, there remains a high rate of post-transplant complications, with one of the main complications being biliary complications. In addition to anastomotic leak and stricture, numerous additional biliary complications are encountered, including ischemic cholangiopathy due to the sole arterial supply of the bile ducts, recurrence of primary biliary disease, infections, biliary obstruction from stones, cast, or hemobilia, and less commonly cystic duct remnant mucocele, vanishing duct syndrome, duct discrepancy and kinking, post-transplant lymphoproliferative disorder, retained stent, and ampullary dysfunction. This article presents an overview of biliary anatomy and surgical techniques in liver transplantation, followed by a detailed review of post-transplant biliary complications with their corresponding imaging findings on multiple modalities with emphasis on magnetic resonance imaging and MR cholangiopancreatography.


Asunto(s)
Sistema Biliar , Colestasis , Trasplante de Hígado , Complicaciones Posoperatorias , Humanos , Conductos Biliares/patología , Sistema Biliar/irrigación sanguínea , Sistema Biliar/diagnóstico por imagen , Colestasis/cirugía , Hígado , Trasplante de Hígado/efectos adversos , Complicaciones Posoperatorias/patología , Pancreatocolangiografía por Resonancia Magnética
9.
Abdom Radiol (NY) ; 48(1): 136-150, 2023 01.
Artículo en Inglés | MEDLINE | ID: mdl-36063181

RESUMEN

Primary sclerosing cholangitis is a rare chronic inflammatory disease affecting the bile ducts, which can eventually result in bile duct strictures, cholestasis and cirrhosis. Patients are often asymptomatic but may present with clinical features of cholestasis. Imaging plays an important role in the diagnosis and management. This review covers the pathophysiology, clinical features, imaging findings as well as methods of surveillance and post-transplant appearance.


Asunto(s)
Colangitis Esclerosante , Colestasis , Humanos , Colangitis Esclerosante/diagnóstico por imagen , Colangitis Esclerosante/patología , Conductos Biliares/patología , Colestasis/diagnóstico por imagen , Colestasis/patología , Cirrosis Hepática/patología , Radiólogos
10.
Bioorg Med Chem Lett ; 22(16): 5227-31, 2012 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-22796184

RESUMEN

A series of TRPV1 agonists with amide, reverse amide, and thiourea groups in the B-region and their corresponding α-methylated analogues were investigated. Whereas the α-methylation of the amide B-region enhanced the binding affinities and potencies as agonists, that of the reverse amide and thiourea led to a reduction in receptor affinity. The analysis indicated that proper hydrogen bonding as well as steric effects in the B-region are critical for receptor binding.


Asunto(s)
Canales Catiónicos TRPV/agonistas , Amidas/síntesis química , Amidas/química , Amidas/metabolismo , Metilación , Unión Proteica , Estereoisomerismo , Relación Estructura-Actividad , Canales Catiónicos TRPV/metabolismo , Tiourea/síntesis química , Tiourea/química , Tiourea/metabolismo
11.
Bioorg Med Chem ; 20(1): 215-24, 2012 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-22169633

RESUMEN

Structure-activity relationships for the A-region in a series of N-4-t-butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamides as TRPV1 antagonists have been investigated. Among them, the 3-fluoro analogue 54 showed high binding affinity and potent antagonism for both rTRPV1 and hTRPV1 in CHO cells. Its stereospecific activity was demonstrated with marked selectivity for the (S)-configuration (54S versus 54R). A docking study of 54S with our hTRPV1 homology model highlighted crucial hydrogen bonds between the ligand and the receptor contributing to its potency.


Asunto(s)
Amidas/química , Amidas/farmacología , Canales Catiónicos TRPV/antagonistas & inhibidores , Amidas/síntesis química , Animales , Sitios de Unión , Células CHO , Simulación por Computador , Cricetinae , Cricetulus , Humanos , Enlace de Hidrógeno , Unión Proteica/efectos de los fármacos , Estructura Terciaria de Proteína , Ratas , Estereoisomerismo , Relación Estructura-Actividad , Canales Catiónicos TRPV/metabolismo
12.
Bioorg Med Chem ; 20(3): 1310-8, 2012 Feb 01.
Artículo en Inglés | MEDLINE | ID: mdl-22227463

RESUMEN

On the basis of the previous lead N-4-t-butylbenzyl 2-(3-fluoro-4-methylsulfonylaminophenyl) propanamide (3) as a potent TRPV1 antagonist, structure-activity relationships for the B (propanamide part) and C-region (4-t-butylbenzyl part) have been investigated for rTRPV1 in CHO cells. The B-region was modified with dimethyl, cyclopropyl and reverse amides and then the C-region was replaced with 4-substituted phenyl, aryl alkyl and diaryl alkyl derivatives. Among them, compound 50 showed high binding affinity with K(i)=21.5nM, which was twofold more potent than 3 and compound 54 exhibited potent antagonism with K(i(ant))=8.0nM comparable to 3.


Asunto(s)
Analgésicos/química , Analgésicos/farmacología , Mesilatos/química , Mesilatos/farmacología , Fenilpropionatos/química , Fenilpropionatos/farmacología , Canales Catiónicos TRPV/antagonistas & inhibidores , Animales , Células CHO , Cricetinae , Humanos , Ratas , Relación Estructura-Actividad , Canales Catiónicos TRPV/metabolismo
13.
Adv Chronic Kidney Dis ; 28(3): 262-269, 2021 05.
Artículo en Inglés | MEDLINE | ID: mdl-34906311

RESUMEN

Ultrasonography is a practical imaging technique used in numerous health care settings. It is relatively inexpensive, portable, and safe, and it has dynamic capabilities that make it an invaluable tool for a wide variety of diagnostic and interventional studies. Recently, there has been a revolution in medical imaging using artificial intelligence (AI). A particularly potent form of AI is deep learning, in which the computer learns to recognize pixel or written data on its own without the selection of predetermined features, usually through a specific neural network architecture. Neural networks vary in architecture depending on their task, and key design considerations include the number of layers and complexity, data available, technical requirements, and domain knowledge. Deep learning models offer the potential for promising innovations to workflow, image quality, and vision tasks in sonography. However, there are key limitations and challenges in creating reliable and safe AI models for patients and clinicians.


Asunto(s)
Inteligencia Artificial , Aprendizaje Profundo , Algoritmos , Humanos , Riñón/diagnóstico por imagen , Aprendizaje Automático , Ultrasonografía
14.
Abdom Radiol (NY) ; 46(2): 745-748, 2021 02.
Artículo en Inglés | MEDLINE | ID: mdl-32804256

RESUMEN

MicroRNAs expressed by germ cell tumors represent a novel approach to detection of metastatic disease during staging, surveillance, and recurrence post-therapy. It has particular promise in settings of equivocal imaging, such as clinical stage I GCT, tumor marker negative stage IIA, or after chemotherapy. These miRNAs have the potential to change typical serum marker evaluation and imaging surveillance schedules.


Asunto(s)
MicroARNs , Neoplasias de Células Germinales y Embrionarias , Neoplasias Testiculares , Biomarcadores de Tumor/genética , Humanos , Masculino , Recurrencia Local de Neoplasia/patología , Estadificación de Neoplasias , Neoplasias de Células Germinales y Embrionarias/diagnóstico por imagen , Neoplasias de Células Germinales y Embrionarias/genética , Radiólogos , Neoplasias Testiculares/patología
15.
Abdom Radiol (NY) ; 45(3): 807-811, 2020 03.
Artículo en Inglés | MEDLINE | ID: mdl-31270562

RESUMEN

PURPOSE: Retrograde pyelography (RPG) is used in some centers to further evaluate patients with incompletely opacified segments on CT urography (CTU). This study intends to evaluate the utility of this imaging combination in terms of the yield of abnormal findings on the follow up RPG. METHODS: In this retrospective study, we searched the radiology database over a three-year period (11/1/2015-10/30/2018) for patients who had a CTU and then a diagnostic RPG within 180 days. Images and reports were reviewed from this period for patients who met the inclusion criteria. RESULTS: 292 patients underwent a CTU with follow up RPG over the search period. 131/292 RPGs (44.9%) were performed because the CTU described at least one incompletely opacified ureteral segment. Of the 148 ureters evaluated in these 131 patients, 4 ureters (2.7%) showed an abnormality on follow up retrograde pyelogram-two revealed a stricture at the unfilled segment, and two revealed contour irregularity in the distal ureter (biopsy showed urothelial cell carcinoma in these two). CONCLUSION: There is a relatively low yield for detecting ureteral abnormalities when a retrograde pyelogram is performed after a CTU to evaluate an incompletely opacified ureteral segment-2.7% in our study, with only two of these incompletely opacified segments containing urothelial cancer (1.4%). In these two cases, a ureteral abnormality was visible on the CTU and RPG would seem to have a very low yield for follow up of unopacified ureteral segments if the ureters are otherwise normal-appearing on CTU and there is no hydronephrosis.


Asunto(s)
Carcinoma de Células Transicionales/diagnóstico por imagen , Tomografía Computarizada por Rayos X/métodos , Enfermedades Ureterales/diagnóstico por imagen , Neoplasias de la Vejiga Urinaria/diagnóstico por imagen , Urografía/métodos , Adulto , Anciano , Anciano de 80 o más Años , Femenino , Humanos , Masculino , Persona de Mediana Edad , Estudios Retrospectivos
16.
ACS Nano ; 14(8): 10187-10197, 2020 08 25.
Artículo en Inglés | MEDLINE | ID: mdl-32692538

RESUMEN

Computed tomography (CT) is an X-ray-based medical imaging technique commonly used for noninvasive gastrointestinal tract (GIT) imaging. Iodine- and barium-based CT contrast agents are used in the clinic for GIT imaging; however, inflammatory bowel disease (IBD) imaging is challenging since iodinated and barium-based CT agents are not specific for sites of inflammation. Cerium oxide nanoparticles (CeNP) can produce strong X-ray attenuation due to cerium's k-edge at 40.4 keV but have not yet been explored for CT imaging. In addition, we hypothesized that the use of dextran as a coating material on cerium oxide nanoparticles would encourage accumulation in IBD inflammation sites in a similar fashion to other inflammatory diseases. In this study, therefore, we sought to develop a CT contrast agent, i.e., dextran-coated cerium oxide nanoparticles (Dex-CeNP) for GIT imaging with IBD. We synthesized Dex-CeNP, characterized them using various analytical tools, and examined their in vitro biocompatibility, CT contrast generation, and protective effect against oxidative stress. In vivo CT imaging was done with both healthy mice and a dextran sodium sulfate induced colitis mouse model. Dex-CeNP's CT contrast generation and accumulation in inflammation sites were compared with iopamidol, an FDA approved CT contrast agent. Dex-CeNP was found to be protective against oxidative damage. Dex-CeNP produced strong CT contrast and accumulated in the colitis area of large intestines. In addition, >97% of oral doses were cleared from the body within 24 h. Therefore, Dex-CeNP can be used as a potential CT contrast agent for imaging GIT with IBD while protecting against oxidative damage.


Asunto(s)
Cerio , Colitis , Enfermedades Inflamatorias del Intestino , Nanopartículas , Animales , Colitis/inducido químicamente , Colitis/diagnóstico por imagen , Medios de Contraste , Dextranos , Enfermedades Inflamatorias del Intestino/diagnóstico por imagen , Enfermedades Inflamatorias del Intestino/tratamiento farmacológico , Ratones
17.
Histopathology ; 55(1): 46-52, 2009 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-19614766

RESUMEN

AIMS: The prognosis in surgically resected oesophageal carcinoma (OC) is dependent on the number of regional lymph nodes (LN) involved, but no guidance exists on how many LNs should be examined histopathologically to give a reliable pN status. The aim of this study was to determine whether the number of LNs examined after OC resection has a significant effect on the assessment of prognosis. METHODS AND RESULTS: Routinely generated pathology reports from 237 consecutive patients undergoing oesophagectomy for OC were examined and analysed in relation to survival. The main outcome measure was survival from date of diagnosis. Lymph node count (LNC) correlated strongly with survival; a plateau was reached after a count of 10. Median and 2-year survival was 30 months and 42%, respectively, if <10 nodes were examined (n = 88), compared with 51 months and 61% if >10 nodes were examined (P = 0.005). This effect was greatest in pN0 cases. The prognostic value of the absolute number of LN metastases (<4) and LN ratio (<0.4) was strongly dependent on a LNC of >10. CONCLUSIONS: These results demonstrate the importance of careful pathological examination and lymph node retrieval after OC resection. At least 10 nodes should be examined to designate an OC as pN0.


Asunto(s)
Adenocarcinoma/diagnóstico , Adenocarcinoma/patología , Carcinoma de Células Escamosas/diagnóstico , Carcinoma de Células Escamosas/patología , Neoplasias Esofágicas/diagnóstico , Neoplasias Esofágicas/patología , Ganglios Linfáticos/patología , Adenocarcinoma/mortalidad , Carcinoma de Células Escamosas/mortalidad , Errores Diagnósticos/prevención & control , Neoplasias Esofágicas/mortalidad , Femenino , Estudios de Seguimiento , Humanos , Metástasis Linfática , Masculino , Persona de Mediana Edad , Pronóstico , Estudios Prospectivos , Tasa de Supervivencia
18.
Eur Radiol ; 19(4): 935-40, 2009 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-18958473

RESUMEN

Pre-morbid weight loss and low body mass index (BMI) have been reported to be associated with decreased odds of misclassification of the defined stage of oesophageal cancer by endoluminal ultrasound (EUS). The aim of this study was to assess the strengths of agreement between the perceived preoperative radiological T and N stage compared with the final histopathological stage related to four categories of BMI (low <20, normal 20-24.9, high 25-30, and obese >30 kg/m(2)). One hundred sixty-six patients with oesophageal carcinoma were studied. Strength of agreement between the CT and EUS stages and histopathological stage was determined by the weighted kappa statistic (Kw). Kw for EUS T stage related to increasing BMI category was 0.840 (P = 0.0001) to 0.620 (P = 0.001), compared with 0.415 (P = 0.018) to 0.260 (P = 0.011) for CT. Kw for EUS N stage related to increasing BMI category was 0.438 (P = 0.067) to 0.513 (P = 0.010), compared with 0.143 (P = 0.584) to 0.582 (P = 0.030) for CT. EUS was good at predicting tumour infiltration irrespective of BMI when compared with CT, while CT N staging accuracy improved with higher BMIs. Multidisciplinary teams should be aware of these limitations when planning treatment strategies.


Asunto(s)
Endosonografía/métodos , Neoplasias Esofágicas/diagnóstico por imagen , Neoplasias Esofágicas/diagnóstico , Tomografía Computarizada por Rayos X/métodos , Adulto , Anciano , Anciano de 80 o más Años , Índice de Masa Corporal , Endoscopía/métodos , Femenino , Humanos , Masculino , Errores Médicos/prevención & control , Persona de Mediana Edad , Estadificación de Neoplasias , Estudios Prospectivos , Ultrasonografía/métodos
19.
Bioorg Med Chem ; 17(2): 690-8, 2009 Jan 15.
Artículo en Inglés | MEDLINE | ID: mdl-19135377

RESUMEN

A series of non-vanillyl resiniferatoxin analogues, having 4-methylsulfonylaminophenyl and fluorophenyl moieties as vanillyl surrogates, have been investigated as ligands for rat TRPV1 heterologously expressed in Chinese hamster ovary cells. Although lacking the metabolically problematic 4-hydroxy substituent on the A-region phenyl ring, the compounds retained substantial agonist potency. Indeed, the 3-methoxy-4-methylsulfonylaminophenyl analog (1) was modestly (2.5-fold) more potent than RTX, with an EC(50)=0.106 nM. Further, it resembled RTX in its kinetics and pattern of stimulation of the levels of intracellular calcium in individual cells, as revealed by imaging. Compound 1 displayed modestly enhanced in vitro stability in rat liver microsomes and in plasma, suggesting that it might be a pharmacokinetically more favorable surrogate of resiniferatoxin. Molecular modeling analyses with selected analogues provide evidence that the conformational differences could affect their binding affinities, especially for the ester versus amide at the B-region.


Asunto(s)
Diterpenos/farmacología , Canales Catiónicos TRPV/agonistas , Animales , Células CHO , Calcio/metabolismo , Cricetinae , Cricetulus , Diterpenos/sangre , Diterpenos/química , Diterpenos/farmacocinética , Microsomas Hepáticos/metabolismo , Modelos Moleculares , Ratas , Relación Estructura-Actividad
20.
Ultrasound Q ; 35(4): 355-375, 2019 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-30921101

RESUMEN

Endometriosis is a common disease of reproductive-age women that is often first encountered with ultrasound. Therefore, familiarity with the variety of manifestations of endometriosis is important for appropriate diagnosis and management. The aim of this article is to review the spectrum of appearance of pelvic endometriosis and to discuss potential mimics on ultrasound. Given that magnetic resonance imaging is an important problem-solving tool in female pelvic imaging, magnetic resonance imaging correlation is also provided.


Asunto(s)
Endometriosis/diagnóstico , Ultrasonografía/métodos , Diagnóstico Diferencial , Femenino , Humanos , Reproducibilidad de los Resultados
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