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1.
Gene Ther ; 9(17): 1139-45, 2002 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-12170377

RESUMEN

Radioactive iodide uptake (RAIU) in thyroid follicular epithelial cells, mediated by the sodium iodide symporter (NIS), is the first rate-limiting step in iodide accumulation which provides a mechanism for effective radioiodide treatment for patients with thyroid cancer. We hypothesize that NIS gene transfer to non-thyroid tumor cells will enhance intracellular radioiodide accumulation and result in better tumor control. Here, we performed non-invasive tumor imaging and (131)I therapy studies using rats bearing intracerebral F98 gliomas that have been retrovirally transduced with human NIS. Our results show that: (1) NIS is expressed in the intracerebral F98/NIS gliomas; (2) F98/NIS gliomas can be imaged by (99m)TcO(4) (whose uptake is also mediated by NIS) and (123)I scintigraphy; (3) significant amounts of radioiodide were retained in the tumors at 24 h after (123)I injection; (4) RAIU and NIS expression in the thyroid gland can be reduced by feeding a thyroxine-supplemented diet; and (5) survival time was increased in rats bearing F98/hNIS tumors by (131)I treatment. These studies warrant further investigating tumor imaging and therapeutic strategies based on NIS gene transfer followed by radioiodide administration in a variety of human cancers.


Asunto(s)
Neoplasias Encefálicas/terapia , Terapia Genética/métodos , Glioma/terapia , Simportadores/genética , Animales , Western Blotting , Neoplasias Encefálicas/radioterapia , Vectores Genéticos/administración & dosificación , Glioma/radioterapia , Humanos , Inmunohistoquímica , Radioisótopos de Yodo/uso terapéutico , Modelos Animales , Ratas , Ratas Endogámicas F344 , Retroviridae/genética , Simportadores/análisis , Glándula Tiroides/metabolismo , Tiroxina/uso terapéutico , Transducción Genética , Células Tumorales Cultivadas
4.
Am J Surg ; 177(6): 445-9, 1999 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-10414690

RESUMEN

BACKGROUND: This prospective study was performed to ascertain the added benefit of lymphoscintigraphy to a standard method of intraoperative lymphatic mapping and sentinel node biopsy for breast cancer. METHODS: Patients with invasive breast cancer were injected with 99mTc sulfur colloid prior to sentinel node biopsy; preoperative lymphoscintigraphy was then performed in half of the patient population. RESULTS: Sentinel node identification was possible in 45 of 50 patients (90%). All 14 patients (31%) with axillary nodal metastases had at least one histologically positive sentinel node (0% false negative rate). Lymphoscintigraphy revealed sentinel nodes in 17 of the 24 patients (70.8%) imaged. All 17 of these patients had one or more axillary sentinel nodes identified using intraoperative lymphatic mapping. In addition, 5 of 7 patients with a negative preoperative lymphoscintogram had an axillary sentinel lymph node(s) identified intraoperatively. None of the tumors showed drainage to the internal mammary lymph node chain by lymphoscintigraphy despite the fact that there were 5 patients with inner quadrant tumors. There was no significant advantage with respect to sentinel lymph node localization (91.7% versus 88.5%, P = not significant) or false negative rate (0%, both groups, P = not significant) in the group undergoing preoperative lymphoscintigraphy when compared with the patients in whom lymphoscintigraphy was not performed. CONCLUSIONS: Preoperative lymphoscintigraphy adds little additional information to intraoperative lymphatic mapping, and its routine use is not justified.


Asunto(s)
Neoplasias de la Mama/cirugía , Ganglios Linfáticos/diagnóstico por imagen , Metástasis Linfática/diagnóstico por imagen , Axila , Biopsia , Neoplasias de la Mama/diagnóstico por imagen , Neoplasias de la Mama/patología , Femenino , Humanos , Cuidados Intraoperatorios , Ganglios Linfáticos/patología , Metástasis Linfática/patología , Cuidados Preoperatorios , Estudios Prospectivos , Cintigrafía , Radiofármacos , Azufre Coloidal Tecnecio Tc 99m
5.
J Nucl Med Technol ; 27(4): 309-17, 1999 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-10646554

RESUMEN

Identification of sentinel lymph nodes (SLNs) using lymphoscintigraphy, the blue dye technique and intraoperative lymphatic mapping with a gamma-detecting probe has become the standard of care in diagnosing and treating melanoma. Numerous clinical studies have proven the reliability of predicting the histology of remaining lymph nodes in the lymphatic basin from the histologic evaluation of the SLNs. Technical and clinical factors presented in this paper have been shown to increase the accuracy of localization of SLNs. The nuclear medicine technologist shares a vital role in the radiopharmaceutical preparation and administration for preoperative lymphoscintigraphy and intraoperative lymphatic mapping in patients with melanoma.


Asunto(s)
Ganglios Linfáticos/diagnóstico por imagen , Melanoma/cirugía , Neoplasias Cutáneas/cirugía , Humanos , Periodo Intraoperatorio , Metástasis Linfática , Melanoma/diagnóstico por imagen , Melanoma/secundario , Cintigrafía , Radiofármacos , Colorantes de Rosanilina , Neoplasias Cutáneas/patología , Azufre Coloidal Tecnecio Tc 99m
6.
Clin Nucl Med ; 23(6): 345-9, 1998 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-9619317

RESUMEN

In the majority of cases, carcinoma of the thyroid presents as a cold nodule by radioiodine and Tc-99m sodium pertechnetate scintigraphy. Whereas the presence of a hot nodule usually implies a benign entity, it does not provide complete assurance against thyroid malignancy. Presented is a rare case of metastatic pure papillary thyroid carcinoma appearing as a hot nodule on Tc-99m sodium pertechnetate and I-123 sodium iodide scintigraphy. The implications of such a case, its management, and review of the pertinent literature are discussed.


Asunto(s)
Carcinoma Papilar/diagnóstico por imagen , Neoplasias de la Tiroides/diagnóstico por imagen , Nódulo Tiroideo/diagnóstico por imagen , Adolescente , Carcinoma Papilar/secundario , Femenino , Humanos , Radioisótopos de Yodo , Cintigrafía , Radiofármacos , Yoduro de Sodio , Pertecnetato de Sodio Tc 99m , Neoplasias de la Tiroides/patología
7.
Clin Nucl Med ; 23(3): 160-2, 1998 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-9509930

RESUMEN

The authors report atypical findings of discordant bone scans and radiography seen in a patient with transient osteoporosis of the hip (TOH). Presented in the case of a 60-year-old man who had spontaneous onset of left hip pain which worsened for 2 months with weight-bearing on the affected side. Initial and follow-up radiographs of the let hip were normal. Bone scan demonstrated intense uptake of Tc-99m MDP in the affected femoral head and neck, corresponding to characteristics of abnormal signal intensity of TOH or transient bone marrow edema syndrome on MRI. This discordant pattern of bone scan and radiographs has rarely been reported in the literature. Its possible mechanism of causation and clinical implication in TOH, together with a review of the literature, are discussed in this report.


Asunto(s)
Cabeza Femoral/diagnóstico por imagen , Cuello Femoral/diagnóstico por imagen , Osteoporosis/diagnóstico por imagen , Médula Ósea/patología , Edema/diagnóstico , Cabeza Femoral/patología , Cuello Femoral/patología , Articulación de la Cadera/diagnóstico por imagen , Humanos , Imagen por Resonancia Magnética , Masculino , Persona de Mediana Edad , Osteoporosis/diagnóstico , Radiografía , Cintigrafía , Medronato de Tecnecio Tc 99m
8.
Surgery ; 118(6): 1105-13; discussion 1113-4, 1995 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-7491530

RESUMEN

BACKGROUND: The present study evaluates 111In-pentetreotide scanning as a method for detection of gastrinomas. Operative findings serve as the benchmark for comparison of the efficacy of 111In-pentetreotide versus conventional imaging studies. METHODS: Twelve patients (seven female and five male; age, 37 to 80 years) with histologic confirmation of gastrinoma underwent thin section dynamic computed tomography (CT) scanning and 111In-pentetreotide scanning. The sensitivity, specificity, positive predictive value, negative predictive value, and accuracy of 111In-pentetreotide and CT scanning are compared on the basis of tumor size and location. RESULTS: Thirty discrete foci of intrahepatic and extrahepatic tumors were detected at operation. CT scanning detected three of nine pancreaticoduodenal lesions, whereas eight of these nine extrahepatic primary tumors were imaged by 111In-pentetreotide scanning. No false-positive 111In-pentetreotide scans were noted. The sensitivity of CT scanning for detection of metastatic disease was 56% versus 94% for the 111In-pentetreotide scan. Successful CT imaging was highly dependent on tumor size. No tumor smaller than 1 cm was imaged by CT, whereas four of seven lesions greater than 1 cm were imaged by 111In-pentetreotide scintigraphy. The smallest gastrinoma imaged by 111In-pentetreotide scanning was a 4 mm duodenal tumor. CONCLUSIONS: 111In-pentetreotide scanning was superior to CT scanning for localizing gastrinomas. Further studies are required to determine whether 111In-pentetreotide scans will complement or replace traditional imaging methods.


Asunto(s)
Gastrinoma/diagnóstico por imagen , Radioisótopos de Indio , Somatostatina/análogos & derivados , Adulto , Anciano , Anciano de 80 o más Años , Neoplasias Duodenales/diagnóstico , Neoplasias Duodenales/diagnóstico por imagen , Femenino , Gastrinoma/diagnóstico , Humanos , Neoplasias Hepáticas/diagnóstico , Neoplasias Hepáticas/diagnóstico por imagen , Metástasis Linfática/diagnóstico , Metástasis Linfática/diagnóstico por imagen , Masculino , Persona de Mediana Edad , Neoplasias Pancreáticas/diagnóstico , Neoplasias Pancreáticas/diagnóstico por imagen , Cintigrafía , Sensibilidad y Especificidad , Tomografía Computarizada por Rayos X
9.
J Cardiol ; 26(5): 263-72, 1995 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-8523258

RESUMEN

Previous studies have shown a good correlation between exercise-induced changes of Q-, R-, and S-waves (Athens QRS score) and the number of the obstructed coronary arteries. The present study was undertaken to test the hypothesis that abnormal Athens QRS score is related to exercise-induced myocardial ischemia. Patients who had exercise radionuclide ventriculography (n = 150) or thallium-201 scintigraphy (n = 124) within 1 month of cardiac catheterization were studied. Athens QRS score was calculated based on the exercise-induced changes of the Q-, R-, and S-waves. Changes in Athens QRS score were compared to the number of obstructed coronary arteries, segmental contraction abnormalities, and exercise-induced myocardial perfusion defects. Athens QRS score and coronary artery disease: The Athens QRS score was decreased as the number of obstructed coronary arteries increased (normal coronary arteries 3.7 mm, confidence interval 1.0 to 3.9, one vessel disease 1.2 mm, two vessel disease -0.6 mm, three vessel disease -1.3 mm, p < 0.001). Athens QRS score and segmental contraction abnormalities: The Athens QRS score decreased as the number of segmental contraction abnormalities increased (no segmental contraction abnormalities 2.5 mm, confidence interval 1.0 to 3.9, one segmental contraction abnormality -0.4 mm, two segmental contraction abnormalities -1.5 mm, three segmental contraction abnormalities -2.6 mm, p < 0.001). Athens QRS score and reversible myocardial perfusion defects: The Athens QRS score was decreased as the number of exercise-induced myocardial perfusion defects increased (no perfusion defect 2.4 mm, confidence interval 0.9 to 3.9, one perfusion defect -0.7 mm, two perfusion defects -2.6 mm, three perfusion defects -3.3 mm, p < 0.001). Abnormal values of the Athens QRS score were better correlated with the number of exercise-induced segmental contraction abnormalities or the myocardial perfusion defects than the number of obstructed coronary arteries (p < 0.001). Exercise-induced changes in Athens QRS score were directly related to the number of obstructed coronary arteries, to exercise-induced segmental contraction abnormalities and to exercise-induced myocardial perfusion defects. However, Athens QRS score changes were more closely related to the number of exercise-induced segmental contraction abnormalities or to the exercise-induced myocardial perfusion defects than to the number of obstructed coronary arteries. The data suggest that exercise-induced QRS changes, Athens QRS score are related to exercise-induced myocardial ischemia.


Asunto(s)
Enfermedad Coronaria/diagnóstico por imagen , Prueba de Esfuerzo , Isquemia Miocárdica/diagnóstico por imagen , Angiografía Coronaria , Electrocardiografía , Femenino , Humanos , Masculino , Persona de Mediana Edad , Ventriculografía con Radionúclidos , Radioisótopos de Talio
10.
Semin Nucl Med ; 25(3): 251-61, 1995 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-7570044

RESUMEN

Somatostatin, a naturally occurring 14-amino acid peptide, can be thought of as an anti-growth hormone and functional down-regulator of sensitive tissue. Most neuroendocrine tumors seem to possess somatostatin receptors in sufficient abundance to allow successful scintigraphic imaging with radiolabeled somatostatin congeners. Several of these, including Indium-III-DTPA Pentetreotide (Octreoscan [Mallinckrodt Medical, St. Louis, MO]), which was approved for clinical use by the Food and Drug Administration in June 1994, have been of considerable value in scintigraphically identifying various neuroendocrine tumors. The Octreoscan compares favorably with other imaging modalities. The success of somatostatin receptor imaging in evaluating patients with suspected neuroendocrine tumors, including identifying otherwise radiographically occult lesions, has resulted in ranking somatostatin receptor imaging as the prime imaging procedure in patients with suspected neuroendocrine tumors at The Ohio State University.


Asunto(s)
Radioisótopos de Indio , Tumores Neuroendocrinos/diagnóstico por imagen , Octreótido/análogos & derivados , Ácido Pentético/análogos & derivados , Receptores de Somatostatina/análisis , Humanos , Dosis de Radiación , Cintigrafía
11.
J Vasc Interv Radiol ; 5(4): 567-72, 1994.
Artículo en Inglés | MEDLINE | ID: mdl-7949712

RESUMEN

PURPOSE: To compare the acute thrombogenicity of polyurethane-coated stents with that of bare tantalum stents. MATERIALS AND METHODS: Thirty stents (15 coated with polyurethane) were balloon expanded in 8-mm x 80-cm sections of polytetrafluoroethylene grafts (six stents per graft). Under sterile conditions, 8- and 10-F vascular sheaths were placed percutaneously in the femoral artery and vein of a 100-lb (45-kg) swine. Platelets were labeled with indium-111 and reinjected for quantitative assay. The stented grafts were connected to the arterial and venous sheaths to create an ex vivo fistula. Each fistula was opened for 5, 10, 30, 60, or 120 minutes, exposing heparinized blood to fully expanded stents. The fistulas were closed, flushed with saline until clear, and fixed with formalin. Stents were explanted, placed in a radionuclide well counter, and scanned with electron microscopy. RESULTS: Quantitatively, there were considerably fewer platelets on coated versus uncoated stents. At 60 minutes, coated stents averaged 12.93 platelets per 1,000 microns 2 compared with 75.88 platelets per 1,000 microns 2 for bare metallic stents. At 120 minutes, there were 23.22 platelets/1,000 microns 2 versus 102.31 platelets/1,000 microns 2, respectively. Electron microscopy of coated stents demonstrated few scattered platelets at 5, 10, and 30 minutes. There was a uniform layer of platelets at 60 and 120 minutes. Uncoated stents demonstrated random areas of platelet clumping at 5, 10, and 30 minutes. At 60 and 120 minutes, uncoated stents showed extensive layering of platelets and fibrin. CONCLUSION: Polyurethane coating decreases platelet adhesion, relative to bare tantalum, at all time intervals tested.


Asunto(s)
Adhesividad Plaquetaria , Politetrafluoroetileno , Stents , Tantalio , Animales , Arteria Femoral , Vena Femoral , Radioisótopos de Indio , Microscopía Electrónica , Propiedades de Superficie , Porcinos
12.
Am Heart J ; 126(6): 1320-5, 1993 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-8249788

RESUMEN

The objective of this study was to investigate the effect of myocardial ischemia on the QRS duration in patients with coronary artery disease since acute myocardial ischemia decreases conduction velocity through the ischemic myocardium and may produce QRS prolongation on the surface electrocardiogram. One hundred fifty patients who underwent cardiac catheterization and exercise radionuclide ventriculography within 1 month of each other were studied. Forty patients had normal coronary arteries and 110 had coronary artery disease. QRS duration decreased with exercise in patients with normal coronary arteries (-3.0 msec, confidence limits -6.2 to 0.2), but increased in patients with coronary artery disease; exercise-induced QRS prolongation was directly related to the number of diseased vessels (4.8 msec in patients with one, 7.8 msec in patients with two, and 13.3 msec in patients with three-vessel disease, p < 0.001). Likewise, QRS duration decreased with exercise in patients without exercise-induced segmental contraction abnormalities (-1.8 msec, confidence limits -3.7 to 0.1), but increased in patients with segmental contraction abnormalities (6.7 msec in patients with one, 13.5 msec in patients with two, and 21 msec in patients with three segmental contraction abnormalities, p < 0.0001). Exercise-induced QRS prolongation was better related to the number of segmental contraction abnormalities than to the number of diseased vessels (p < 0.01). It was concluded that exercise produces QRS prolongation in patients with coronary artery disease in direct relation to the number of diseased vessels and to exercise-induced segmental contraction abnormalities.(ABSTRACT TRUNCATED AT 250 WORDS)


Asunto(s)
Arritmias Cardíacas/etiología , Enfermedad Coronaria/fisiopatología , Electrocardiografía , Isquemia Miocárdica/fisiopatología , Esfuerzo Físico/fisiología , Adulto , Anciano , Arritmias Cardíacas/fisiopatología , Angiografía Coronaria , Enfermedad Coronaria/complicaciones , Enfermedad Coronaria/diagnóstico , Prueba de Esfuerzo , Femenino , Humanos , Masculino , Persona de Mediana Edad , Contracción Miocárdica , Isquemia Miocárdica/diagnóstico , Isquemia Miocárdica/diagnóstico por imagen , Ventriculografía con Radionúclidos
13.
J Vasc Surg ; 9(6): 806-11, 1989 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-2724466

RESUMEN

Because of the high incidence of coronary artery disease (CAD) in patients undergoing aortic surgery, and because myocardial oxygen consumption is proportional to blood pressure x heart rate (HR) (pressure-rate product), it is important to prevent increases in these parameters postoperatively. The effect of verapamil, a calcium channel antagonist, on these parameters was evaluated in 30 patients undergoing abdominal aortic reconstruction. Postoperatively HR increased 27% in 19 patients without CAD and 47% in 11 patients with CAD. Pressure-rate product (blood pressure x HR) increased 17% and 31% in these two groups, respectively. Verapamil was able to reduce postoperative HR by 3% in patients without CAD and by 13% in patients with CAD. Verapamil reduced pressure-rate product 8% and 18%, respectively, in the two groups. These reductions were statistically significant in patients with CAD and occurred without reductions in cardiac output or left ventricular ejection fraction. Thus the postoperative increases in myocardial oxygen demand appeared to be primarily related to increased HR after aortic surgery, and these were reduced by verapamil without impairing blood flow or cardiac function.


Asunto(s)
Aorta Abdominal/cirugía , Hemodinámica/efectos de los fármacos , Verapamilo/uso terapéutico , Anciano , Presión Sanguínea/efectos de los fármacos , Enfermedad Coronaria/complicaciones , Enfermedad Coronaria/fisiopatología , Frecuencia Cardíaca/efectos de los fármacos , Humanos , Persona de Mediana Edad , Miocardio/metabolismo , Consumo de Oxígeno/efectos de los fármacos , Periodo Posoperatorio , Verapamilo/farmacología
14.
Am J Cardiol ; 63(19): 64I-68I, 1989 Jun 05.
Artículo en Inglés | MEDLINE | ID: mdl-2729126

RESUMEN

Hemodynamic and left ventricular function parameters were measured in patients with mild to moderate hypertension and compromised left ventricular function who were given dilevalol, an antihypertensive agent with selective beta 2-agonism and nonselective beta-antagonist activity. After a 2- to 3-week placebo washout period, 9 patients were given dilevalol titrated upward from 100 to 600 mg twice daily over a 7-week period to achieve a supine diastolic blood pressure of less than 90 mm Hg with a decrease of greater than or equal to 10 mm Hg from baseline. Multigated radionuclide ventriculography and systolic and diastolic time intervals were performed after the pretreatment placebo washout, at the end of 2 weeks' maintenance dosing, and after a 7- to 10-day post-treatment discontinuation and placebo washout period. At an average daily dose of dilevalol, 444 mg, heart rate at rest decreased significantly (p less than 0.01) during treatment and increased during post-treatment placebo. Systolic and diastolic blood pressures at rest decreased significantly (p less than 0.01) during treatment and increased during post-treatment placebo. At maximal exercise, changes in blood pressure and heart rate were significantly blunted (p less than 0.05) during treatment. Ejection fraction at rest increased significantly (p less than 0.01) during treatment, with no significant change occurring during exercise, and decreased during post-treatment placebo. Preejection period decreased significantly during treatment (p less than 0.005) and increased during post-treatment placebo.(ABSTRACT TRUNCATED AT 250 WORDS)


Asunto(s)
Insuficiencia Cardíaca/tratamiento farmacológico , Hemodinámica/efectos de los fármacos , Hipertensión/tratamiento farmacológico , Labetalol/farmacología , Anciano , Prueba de Esfuerzo , Insuficiencia Cardíaca/complicaciones , Frecuencia Cardíaca/efectos de los fármacos , Humanos , Hipertensión/complicaciones , Masculino , Persona de Mediana Edad , Volumen Sistólico/efectos de los fármacos
15.
Clin Nucl Med ; 11(11): 769-70, 1986 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-3791785

RESUMEN

A 64-year-old man was found to have isolated focal rib lesion(s) by radiographs and radionuclide bone scan. A biopsy of one of the lesions located by imaging was done. The histologic diagnosis was sclerosing (ossifying) xanthoma. A literature search disclosed that xanthomatous lesions of bone are only one of the manifestations in hyperlipidemic patients. These benign lesions should be included among the causes of discrete hot rib abnormalities visualized on bone scan.


Asunto(s)
Enfermedades Óseas/diagnóstico por imagen , Costillas , Xantomatosis/diagnóstico por imagen , Biopsia , Enfermedades Óseas/patología , Diagnóstico Diferencial , Humanos , Masculino , Persona de Mediana Edad , Radiografía , Cintigrafía , Costillas/diagnóstico por imagen , Costillas/patología , Medronato de Tecnecio Tc 99m , Xantomatosis/patología
18.
J Comput Assist Tomogr ; 2(4): 400-3, 1978 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-701518

RESUMEN

During computed tomography (CT) scanning of the liver, the inferior vena cava can be identified as a separate structure of lesser density adjacent to the caudate lobe in two-thirds of patients without known hepatocellular disease. In patients with alcoholic (portal) cirrhosis of moderate to severe degree, intrahepatic portal veins may not be identified on CT scans, even though their inferior vena cavas can be definitely distinguished from the caudate lobe. Portal cirrhosis causes distortion and obliteration of the portal triads, which is presumably reflected by lack of visualization of intrahepatic portal veins during CT scanning.


Asunto(s)
Cirrosis Hepática/diagnóstico por imagen , Hígado/diagnóstico por imagen , Sistema Porta/diagnóstico por imagen , Tomografía Computarizada por Rayos X , Humanos
19.
J Clin Ultrasound ; 6(3): 165-6, 1978 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-97318

RESUMEN

A case report is presented concerning a patient with a dilated loop of bowel that was misinterpreted on ultrasound examination. Attention is called to this entity as part of the differential diagnosis of an intra-abdominal fluid collection demonstrated by ultrasound.


Asunto(s)
Obstrucción Intestinal/diagnóstico , Yeyuno , Quiste Pancreático/diagnóstico , Ultrasonografía , Adulto , Diagnóstico Diferencial , Humanos , Masculino
20.
J Med Chem ; 21(4): 391-3, 1978 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-650667

RESUMEN

A series of substituted 5alpha-androstan-17beta-ols was synthesized and evaluated for their potential use in the development of a prostate imaging agent. The ability of the synthesized compounds to compete with [3H]-5alpha-dihydrotestosterone for rat prostate androgen receptor protein served as the screening assay. For 3-substituted derivatives, the order of binding to the androgen receptor protein was =O greater than -OH greater than H approximately or equal to F. 3beta-Fluoro-5alpha-androstan-17beta-ol was found to have approximately 5% the androgenic activity of testosterone propionate in the castrated rat. The low biological activity for the 3beta-fluoro derivatives, coupled with the synthetic obstacles associated with introducing fluorine-18, has led us to search for more suitable halo steroids as potential radiodiagnostics.


Asunto(s)
Androstanos/síntesis química , Próstata/diagnóstico por imagen , Androstanos/metabolismo , Animales , Unión Competitiva , Dihidrotestosterona/metabolismo , Técnicas In Vitro , Masculino , Cintigrafía , Ratas , Receptores Androgénicos/metabolismo
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