PubMed Health⌕ Search

Biomedical subjects

R C Reba

Publications and source records attributed to R C Reba.

At least 127 records · Page 7Linked to original sources
PubMed1979

Cardioselectivity of beta-adrenoceptor blocking agents 1. 1-[(4-Hydroxyphenethyl)amino]-3-(aryloxy)propan-2-ols.

A series of 1-[(4-hydroxyphenethyl)amino]-3-(aryloxy)propan-2-ols was synthesized together with several 1-[(3,4-dimethoxyphenethyl)amino]-3-(aryloxy)propan-2-ols. Their affinity to beta 1- and beta-2-adrenoceptors was determined and compared with the affinity of known beta-blockers. We were able to confirm the substantial cardioselectivity of 1-(3,4-dimethoxyphenethyl)-3-[(4-substituted aryl)oxy]propan-2-ols when compared to those with a 1-(4-hydroxyphenethyl) group. An increase in the size of the 4 substitutent of the 3-(aryloxy) moiety to caproamido leads to a substantially higher affinity for the beta 1--adrenoceptor of rat ventricular muscle in the presence of the 3,4-dimethoxyphenethyl than in the presence of the 4-hydroxyphenethyl or isopropyl group; this combination also gave the highest cardioselectivity.

Adrenergic beta-Antagonists↗
PubMed1979

Biological distribution and excretion of DTPA labeled with Tc-99m and In-111.

For the purpose of radiation dose estimates, organ assays and excretion measurements of the Tc-99m and In-111 complexes with DTPA were conducted in dogs at various time intervals up to 24 hr, and the results compared with available human data. The peak concentration of the Tc-99m complex, at 3 min after injection, was 5% of the administered dose for one kidney, 3.5% for the liver, and 3.5% for the small bowel. No organ system except the urinary tract reached a concentration higher than that in blood for several hours after the injection. The biliary excretion of these agents was extremely low, and their elimination in the feces was negligible. In man, it appears that the residual 4-5% of an administered dose not eliminated in the urine by 24 hr is widely distributed in various tissues. The distribution of the In-111 complex is similar but not identical to that of the Tc-99m complex.

Animals↗
PubMed1979

The distribution of the muscarinic acetylcholine receptor antagonists, quinuclidinyl benzilate and quinuclidinyl benzilate methiodide (both tritiated), in rat, guinea pig, and rabbit.

The distribution of [3H]quinuclidinyl benzilate and its methiodide salt was determined in rat, guinea pig, and rabbit. Accumulation in the myocardium of up to 2% of the injected dose per gram of tissue was obtained with both compounds, providing heart-to-blood ratios of approximately 30 and heart-to-lung ratios of approximately 4. The accumulation in the heart was blocked (89%) by preinjection of atropine. The distribution of tritium in rabbit heart corresponds to the muscarinic receptor densities determined in vitro. Calculation of the theoretical maximum for the bound-to-free ratio, based on in-vitro equilibrium binding isotherms, resulted in ratios in reasonable agreement with the experimental results. Because of the high accumulation in the heart with low serum concentration, we conclude that the methiodide salt of quinuclidinyl benzilate represents an ideal parent structure for the design of a receptor-binding gamma-emitting radiopharmaceutical for imaging of the myocardium.

Acetylcholine↗
PubMed1978

Radioiodinated derivatives of beta adrenoceptor blockers for myocardial imaging.

Four new beta-adrenoceptor blocking agents carrying tyramine as the amino moiety were synthesized and the distribution of their I-125-tagged derivatives evaluated in rats. This distribution was compared with the distribution of various agonists and antagonists labeled with H-3 and C-14, and with the in vitro binding affinity of the new derivatives. A radioiodinated derivative of a cardioselective blocker, alprenolol, showed poor blood clearance and no cardiac selectivity. A derivative of another cardioselective blocker, practolol, showed a promising heart-to-blood ratio (ca. 19) and cardioselectivity with a heart-to-lung ratio of ca. 2. Two additional practolol analogs showed no improvement over the practolol derivative; because of the increased lipophilicity of these derivatives, blood clearance and cardioselectivity were diminished. An inverse correlation is suggested between the dissociation constant for the beta adrenoceptor in the lung and the heart-to-blood and heart-to-lung values. We conclude that polarity plays an important role in the blood clearance and cardioselectivity of these beta-adrenoceptor derivatives.

Adrenergic beta-Antagonists↗
PubMed1977

Biological distribution of chemical analogs of fatty acids and long chain hydrocarbons containing a strong chelating agent.

The pharmaceutical preparation, chromatography, and biological distribution of a series of new chemical analogs of palmitic acid and diethylenetriaminepentaacetic acid, ethylenediaminetetraacetic acid, or diethylenetriamine are described. The biological distribution in rabbits 30 min after intravenous administration of these 99mTc-labeled and 57Co-labeled derivatives was compared to the biological distribution of the parent compound, 3H-palmitic acid. The average myocardial uptake for these compounds was 0.04%/g, compared to 0.15%/g for palmitic acid. The heart to blood ratio at 30 min reached a maximum of 3:1 for the best physiological analog of palmitic acid, compared to an average of 30:1 for palmitic acid. Although none of these analogs appears to be clinically useful, their production methods might be applicable to the synthesis of new compounds that might increase the specificity of radiopharmaceuticals.

Animals↗
PubMed1977

Strontium-87m lung scans in pulmonary aspergillosis.

Experimental observations have indicated that radioactive strontium localizes in lesions infected with Aspergillus species. Preliminary clinical studies have recommended use of strontium lung scanning to evaluate patients thought to have pulmonary manifestations of aspergillosis. In view of the difficulty in accurately interpreting the clinical significance of recovery of Aspergillus species from sputum of patients with pulmonary disorders as well as the varied clinical presentations of pulmonary aspergillosis, we have attempted to confirm these reports. Ten patients with proven pulmonary aspergillosis and five selected control subjects without aspergillosis but with other pulmonary disorders were scanned after the injection of 2-3 mCi 87mSr citrate. The strontium lung scan correlated with the chest radiograph in four of 10 patients with aspergillosis; false positive scans were found in three of five patients with other pulmonary disorders. We conclude that strontium lung scans at present have no role in the diagnostic evaluation of patients suspected of clinically significant infections with aspergillus.

Adult↗
PubMed1977

Estrogen derivatives for the external localization of estrogen-dependent malignancy.

Four radioiodinated estrogen derivatives were studied to determine their affinity for the estrogen-binding protein found in the cytosol of rabbit and rat uteri. In vitro determination of the binding properties by competitive-binding experiments and by sucrose-gradient centrifugation indicates that one of the derivatives, iodohexestrol, binds to the cytosol estrogen-binding protein. This in vitro behavior was related to in vivo distribution. Studies in immature female rats showed high uterine uptake of iodohexestrol at 2 hr (1.69% dose/gm). Iodohexestrol also has a high nonspecific binding in both the blood and the uterine cytosol. Thyroxine can diminish the nonspecific binding in vitro; in vivo the prior injection of thyroxine increased the 2-hr uterus-to-blood ratio from 1.9 to 10.4 The in vitro receptor-assay system was helpful in predicting in vivo distribution.

Animals↗
PubMed1976

False positive 125I fibrinogen test.

125I fibrinogen test was performed in 20 selected patients who presented with symptoms suggestive of deep venous thrombosis. The incidence of a false positive study was found to be very high: 90%. An increased accumulation of fibrinogen was noted over recent, well-healed surgical incisions, diffuse or focal inflammatory sites, hematoma and also, following a venogram or arthrogram test. The large number of coincidental circumstances that result in an abnormal accumulation of 125I fibrinogen lead us to believe that venogram is the procedure of choice in patients with symptoms simulating thrombophlebitis.

False Positive Reactions↗
PubMed1976

Technetium-99m-pyridoxylideneglutamate, a new agent for gallbladder imaging: comparison with 131I-rose bengal.

Two agents used for hepatobiliary studies, 131I-rose bengal and 99mTc-pyridoxylideneglutamate, have been compared in rabbits. The 99mTc radiopharmaceutical is rapidly cleared from the blood by the liver and rapidly excreted through the common bile duct into the duodenum. Because of its rapid removal from the liver, visualization of the gallbladder and biliary passages was obtained within 15 min after injection in experimental animals.

Animals↗
PubMed1976

Iodinated bleomycin: an unsatisfactory radiopharmaceutical for tumor localization.

Cobalt-57-bleomycin is a clinically useful tumor-localizing agent, but attempts to label bleomycin (BLEO) with other radionuclides have been made because of the long physical half-life of 57Co. As an alternative labeling approach, we iodinated BLEO both directly on the imidazole ring and indirectly by reaction with N-succinimidyl 3-(4-hydroxy, 3-iodophenyl) propionate. Directly iodinated BLEO retained antibacterial activity, but in tumor-bearing rats it showed a lower tumor-to-blood ratio (2.3) at 2 hr than did 57Co-BLEO (11.8). The antibacterial activity of the indirectly labeled BLEO was markedly reduced and this material showed a tumor-to-blood ratio of 0.55 at 2 hr. The radioiodinated bleomycins are not suitable substitutes for 57Co-BLEO as tumor-imaging radiopharmaceuticals.

Adenocarcinoma↗