PubMed Health⌕ Search

Biomedical subjects

L Unger

Publications and source records attributed to L Unger.

At least 37 records · Page 2Linked to original sources

(S)-emopamil, a novel calcium and serotonin antagonist for the treatment of cerebrovascular disorders. 1st communication: pharmacological profile.

(S)-Emopamil ((2S)-2-isopropyl-5-(methylphenethylamino)-2-phenylvaleronitril e hydrochloride) is a novel compound of the phenylalkylamine group of calcium antagonists. (S)-Emopamil was tested in comparison to verapamil and gallopamil for calcium and serotonin antagonism and for cerebroprotective activity in acute hypoxia/ischemia. In receptor binding studies with (S)-3H-devapamil, (S)-emopamil exhibited distinct affinity to the verapamil binding site of the calcium channel. In rat cerebrocortical membranes, its affinity (Ki = 38 nmol/l) equalled that of verapamil and gallopamil (Ki = 49 and 27 nmol/l, respectively), whereas it was somewhat weaker in guinea pig skeletal muscle membranes. Comparing (S)-emopamil to its (R)-enantiomer, there was no clear stereoselectivity. Additionally, (S)-emopamil showed very high affinity to the cerebral serotonin S2 receptor; its Ki value (4.4 nmol/l) for 3H-ketanserin displacement being substantially lower than that of verapamil and gallopamil (Ki = 177 and 242 nmol/l, respectively). This feature is clearly stereoselective; (S)-emopamil's affinity was distinctly higher than that of the (R)-enantiomer (Ki = 58 nmol/l). The functional significance of (S)-emopamil's receptor affinity was tested in rat aortic strips. (S)-Emopamil's serotonin antagonistic efficacy (EC50 = 4.5 nmol/l) was an order of magnitude higher than that of verapamil and gallopamil. (S)-Emopamil has a less potent calcium antagonistic effect (EC50 = 270 nmol/l) on the aorta than verapamil and gallopamil (EC50 = 35 and 14 nmol/l, respectively). In isolated electrically driven (1 Hz) left atria of guinea pigs, (S)-emopamil inhibited contractile force at a much higher concentration (EC50 = 29 mumol/l) than verapamil and gallopamil (EC50 = 1.1 and 0.19 mumol/l, respectively).(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗

Cholesterol guidelines, lipoprotein cholesterol levels, and triglyceride levels: potential for misclassification of coronary heart disease risk.

By using National Cholesterol Education Program guidelines for serum cholesterol (less than 200 mg/dl is designated "desirable," and 200 to 239 mg/dl is designated "borderline-high," and greater than or equal to 240 mg/dl is designated "high"), low-density and high-density lipoprotein (LDL, HDL) cholesterol levels and triglyceride levels were quantitated in 897 self-referred fasting subjects to assess the potential for coronary risk misclassification. With cholesterol less than 200 mg/dl, misclassification was arbitrarily identified by an LDL level greater than or equal to the 75th percentile, a triglyceride level greater than or equal to the 90th percentile, or an HDL level less than or equal to the 10th percentile. With the cholesterol level in the 200 to 239 mg/dl range, misclassification was identified by an LDL level greater than or equal to the 75th percentile, a triglyceride level greater than or equal to the 90th percentile, and an HDL level less than or equal to the 10th percentile or greater than or equal to the 90th percentile (or both). With a cholesterol level greater than or equal to 240 mg/dl, misclassification was identified by an HDL level less than or equal to the 10th percentile, or greater than or equal to the 90th percentile. With the cholesterol level less than 200 mg/dl, misclassification is rare, occurring in 14.5% of the subjects. With the cholesterol level in the 200 to 239 mg/dl range, and greater than or equal to 240 mg/dl, misclassification occurred in 46.7% and 17.6% of the subjects, respectively. The importance of routine lipoprotein analysis when the cholesterol level is greater than or equal to 240 mg/dl is emphasized by the finding that 65% of the subjects in this category had top quartile LDL levels, 8% had bottom decile HDL levels, and 30% had top decile triglyceride levels. To avoid misclassification, fasting HDL, LDL, and triglyceride levels should probably be measured in all subjects with screening cholesterol levels greater than or equal to 200. There is remarkably little misclassification with top quartile LDL or bottom decile HDL levels (or both) when the cholesterol level is less than 200 mg/dl.

Adolescent↗

[Pharmacological characterization of the new highly potent beta-adrenergic receptor blocker soquinolol].

The present pharmacological test results characterize soquinolol (5-[3-tertiary butylamino-2-hydroxypropoxy]-2-formyl-1,2,3,4- tetrahydroisoquinoline mucate, We 704, Sertum) as a highly potent non-subtype-selective beta-adrenergic receptor blocker, which is devoid of any intrinsic sympathomimetic activity. Its localanaesthetic activity (membrane stabilizing effect) is very weak. It also shows good enteral efficacy and long duration of action. In binding studies with heart (Ki beta 1 = 3.25 nmol/l) and lung membranes (Ki beta 2 = 0.85 nmol/l) its binding profile was found to be similar to that of propranolol. Soquinolol inhibits the isoprenaline-induced tachycardia (EC50% = 48 micrograms/l) in the guinea-pig Langendorff heart in vitro to the same degree as propranolol. However, in the conscious dog soquinolol's beta 1-adrenergic blocking activity (ED 50%) on intravenous injection (5.5 micrograms/kg) and oral administration (5.8 micrograms/kg) is about twice as great as that of pindolol and 19 times (i.v.) or 138 times (p.o.) greater than that of propranolol. These results suggest 95% enteral efficacy for soquinolol (pindolol 88%, propranolol 13%). The differences in soquinolol's and propranolol's efficacy detected in vitro and in vivo are partially attributable to differences in their kinetic properties namely the lower protein binding and the higher distribution volume of soquinolol. In the conscious dog, soquinolol inhibits beta 1-(ED 50% = 4.0 micrograms/kg) and beta 2-receptors (ED 50% = 2.7 micrograms/kg) at dose levels which do not differ significantly.(ABSTRACT TRUNCATED AT 250 WORDS)

Adrenergic beta-Antagonists↗

Know your cholesterol: population screening.

To facilitate the goal that all adult Americans know their total serum cholesterol levels, our specific aim was to evaluate the effectiveness, practicality, and cost of total cholesterol sampling in nonfasting self-referred subjects with use of venous blood and mailed results (n = 3844), and to compare these results with capillary blood total cholesterol levels (n = 1167), with immediate turnaround. We used consensus cut points of total cholesterol levels greater than 200, greater than 220, and greater than 240 mg/dl for moderate risk of coronary heart disease and greater than 220, greater than 240, and greater than 260 for high risk for aged 20 through 29, 30 through 39, and greater than 40 years. Total cholesterol level was in the moderate- or high-risk range in 45% and 37% of the venous and capillary cohorts, respectively. Median venous and capillary total cholesterol values were approximately 20 and 10 mg/dl greater than the total cholesterol values in the Lipid Research Clinics Prevalence Study, a difference contributed to by nonfasting versus fasting conditions, use of serum versus plasma, and self-referral bias for subjects with a family history of premature coronary heart disease. The cost per subject in the venous and capillary studies was $5.09 and $7.12 respectively, and $11.40 and $ 18.63 for each subject in the moderate- to high-risk range. Resampling with the subject fasting and follow-up were stressed, and were made available for moderate- and high-risk subjects.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗

New class of limited-host-range Agrobacterium mega-tumor-inducing plasmids lacking homology to the transferred DNA of a wide-host-range, tumor-inducing plasmid.

Biotype 1 and 2 strains of Agrobacterium tumefaciens were isolated from crown gall tumors of Lippia canescens plants growing as ground cover in Arizona. The isolates were agrocin 84 sensitive, did not catabolize octopine, nopaline, agropine, or mannopine, and were limited in their tumorigenic host range. One biotype 2 strain, AB2/73, showed the most limited host range; it incited tumors only on Lippia strains, the cucurbit family of plants, and Nicotiana glauca. Megaplasmids were detected in the isolates by vertical agarose gel electrophoresis. The unusual host range, as well as sensitivity to agrocin 84, were plasmid specified since they were conjugally cotransferred with plasmids from donor strain AB2/73. Correlation of deletions with concomitant loss of virulence and agrocin 84 sensitivity identified the megaplasmid pAtAB2/73d as the virulence element in strain AB2/73. The estimated size of this tumor-inducing plasmid was 500 kilobases. Axenic growth of tumor tissue incited by strains carrying pAtAB2/73d was phytohormone independent. Although the limited-host-range megaplasmid pAtAB2/73d lacked any detectable homology to the phytohormone-biosynthetic genes in wide-host-range transferred DNA (tms-1, tms-2, tmr), it showed homology to the wide-host-range virB, virC, virD, and virG loci. Therefore, pAtAB2/73d represents a new class of tumor-inducing plasmids distinguished by its large size, the absence of determinants for the catabolism of several known opines, the presence of agrocin 84 sensitivity, and its lack of homology to wide-host-range transferred DNA contrasted with its conservation of sequences from the wise-host-range vir region.

Adenine Nucleotides↗

Conduct disorder and its synonyms: diagnoses of dubious validity and usefulness.

Psychiatrically hospitalized adolescents from city and voluntary services who had been diagnosed as having conduct disorder were compared with psychiatrically hospitalized adolescents who had never been so diagnosed. There were no significant symptomatic differences. The major factor distinguishing adolescents ever diagnosed as having conduct disorder was violence, regardless of other symptoms. The most common discharge diagnosis of those who had formerly been diagnosed as having conduct disorder was schizophrenia. However, even violence did not distinguish those discharged with a diagnosis of conduct disorder from those whose diagnoses were subsequently changed. With its focus on manifest behaviors and its lack of clear exclusionary criteria, the conduct disorder diagnosis obfuscates other potentially treatable neuropsychiatric disorders.

Adolescent↗

Morbidity in minor gynaecological surgery: a comparison of halothane, enflurane and isoflurane.

A comparison was made between halothane, enflurane and isoflurane with regard to their suitability for minor gynaecological procedures in patients who would be leaving the hospital within 24 h of the anaesthetic. Seventy-five healthy patients were randomly allotted to one of three groups which received one of these anaesthetics. In respect of patient acceptance and postoperative morbidity there were no significant differences between halothane and enflurane, but after isoflurane there was a significantly greater frequency of minor sequelae (headache, nausea, dizziness and coughing) and its pungent odour made it unacceptable to some patients.

Adult↗

Formation of Escherichia coli Hfr strains by integrative suppression with the P group plasmid RP1.

Hfr strains of Escherichia coli were obtained by integrative suppression of a dnaA(Ts) mutation by the Inc P-1 plasmid RP1 without prior creation of an unnatural homology between the plasmid and the E. coli chromosome. Unmodified RP1 mobilized the polarized transfer of the chromosome in a counterclock-wise direction from a distinct origin between 81 min (pyrE) and 82 min (dnaA) with pyrE as a leading marker. Inheritance of RP1-Hfr chromosomal and antibiotic resistance genes was due to recombination with the recipient chromosome, as shown by the need for a functional recA system. The acquisition of temperature resistance and donor ability was accompanied by the disappearance of free plasmid when the selection pressure for integration was maintained (growth at 41 degrees C); the loss of temperature resistance and donor ability was accompanied by the reappearance of autonomous RP1 when the selection pressure was removed (growth at 30 degrees C).

Conjugation, Genetic↗

[Unusual cases of maternal death caused by amniotic fluid embolism].

Five cases of amnion fluid embolism are reported. In the first case the cause of the death was the obstruction of the lung-vessels. In the lung tissue calcium embolia could also been detected. In the second case embolization started--at unruptured amnionsac--with ecclampsia-like convulsions, later it was followed by coagulopathia. In the third case amnion fluid embolism was complicated by coagulopathia. In the fourth case in addition to amnion fluid embolism endometritis purulenta complicated by endotoxinaemia and coagulopathia were also present. In all four cases rupture of the uterus was revealed. In the fifth case amnion fluid embolism developed without the rupture of the uterus. At the autopsy of cases of maternal death the possibility of amnion fluid embolism should always be considered. Although macroscopic changes seen at amnion fluid embolism are not pathognomic, when clinical and pathological symptoms of haemorrhagic diathesis are present, there always arises the suspicion of amnion fluid embolism. Since lungs are relatively resistant to putrefaction amnion fluid embolism in optimal cases can be diagnosed histologically even in exhumated lung specimen. Reliable diagnosis of amnion fluid embolism in cases of sudden maternal death gives possibility to exclude medical negligence.

Adult↗

Hamartomatous polyp of the esophagus.

Hamartomatous polyp of the cervical esophagus in a 60-year-old man was treated by local resection, and the patient did well. The histopathologic findings showed a predominance of cartilaginous tissue, but the specimen also contained glandular structures and adipose tissue. The diagnosis was choristoma or hamartoma. Review of the literature shows this to be the third case reported.

Esophageal Neoplasms↗