Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application.

A set of 56 8-phenylxanthines, previously tested for adenosine antagonism (adenosine A1 receptor affinity), was analyzed by quantitative structure-activity relationship (QSAR) techniques. The resulting QSAR revealed that (1) the most potent receptor binders had already been made in this series and thus suggested the termination of synthesis of compounds with additional phenyl substituents to increase potency and (2) potency was much more strongly affected by changes in ortho than para phenyl substitution. On the basis of this study, an additional 20 compounds were synthesized that contained primarily para substituents designed to increase aqueous solubility.

The effects of serum on the in vitro adherence and maturation of bovine monocytes.

Serum concentration was found to affect both the initial adherence and subsequent in vitro maturation of bovine monocytes. Bovine monocytes cultured in the absence of serum remained small and reduced in number, whereas monocytes cultured in an adequate concentration of either autologous adult bovine or fetal bovine serum developed into large macrophage-like cells. Heat inactivation (56 degrees C for 30 minutes) did not affect the ability of bovine sera to promote monocyte maturation in vitro.

Development of sign-based perception by deaf children.

In this study the sign-based perceptual abilities of 59 deaf children are investigated. Like many hearing speaking children, deaf signing children appear to perceive isolated lexical items based on the formational parameters of those items. Also, deaf signers show trends similar to those exhibited by hearing speakers for the development of the perceptual ability necessary to distinguish between minimal pairs within their respective language systems.

Effects of atomic bomb radiation on the differentiation of B lymphocytes and on the function of concanavalin A-induced suppressor T lymphocytes.

The differentiation of peripheral blood B lymphocytes into immunoglobulin-producing cells (Ig-PC) by pokeweed mitogen (PWM) and the function of concanavalin A (Con A)-induced suppressor T lymphocytes were examined to elucidate the late effects of atomic bomb radiation. A total of 140 individuals, 70 with an exposure dose of 100 rad or more and an equal number with an exposure dose of 0 rad matched by sex and age, were selected from the Nagasaki Adult Health Study (AHS) sample. Both the differentiation of peripheral blood B lymphocytes into Ig-PC by PWM and the function of Con A-induced suppressor T lymphocytes tended to be more depressed in the exposed group than in the control group, but a statistically significant difference could not be observed between the two groups.

Clinical application of basic research on continuous passive motion for disorders and injuries of synovial joints: a preliminary report of a feasibility study.

Since 1970, when the concept of continuous passive motion (CPM) was originated by one of the authors (R.B.S.

C4-substituted 1-beta-D-ribofuranosylpyrazolo[3,4-d]pyrimidines as adenosine agonist analogues.

The synthesis of four novel C4-substituted 1-beta-D-ribofuranosylpyrazolo[3,4-d]pyrimidines is reported, and the compounds were examined as adenosine receptor agonist analogues. Neither receptor affinity nor biological activity was as potent as the purine counterparts. Adenosine agonists appear to be sensitive to modification of the purine base, with a nitrogen atom in the 7 position necessary for efficacy.

The frequency among Japanese of heterozygotes for deficiency variants of 11 enzymes.

Eleven human enzymes, chosen for this study because of relatively small coefficients of variation for mean activity, have been surveyed for the frequency with which activities less than or equal to 66% of the mean value occur. This criterion should detect almost all heterozygotes for variants lacking any activity plus a fraction of the persons with variants characterized by markedly depressed activity and/or instability. The enzymes surveyed are TPI, PGK, AK1, LDH, GAPD, GPI, PK, 6PGD, G6PD, GOT1, and HK.

The relationship of hepatitis B surface antigen and antibody to atomic bomb radiation in the Adult Health Study sample, 1975-1977.

A frequency of positive hepatitis B surface antigen (HBsAg) and antibody (anti-HBs) was determined among 2566 atomic bomb survivors in Hiroshima and Nagasaki, Japan during the two-year period 1975 to 1977. The frequency of positive HBsAg (79% of subjects remained persistently antigen positive) was significantly higher in those exposed to 100 rad or more than in the controls. This difference between exposure groups was more marked among the younger age groups.

Peripheral lymphocyte response to PHA and T cell population among atomic bomb survivors.

The percentage of T lymphocytes of atomic bomb survivors showed no change as a function of age or exposure dose. The percentage of T cells was slightly lower in malignant-tumor patients than in the control group, but was significantly higher in the group with chromosomal aberrations than in the control group. The percentages of phytohemagglutinin (PHA)-induced transformation of peripheral lymphocytes decreased significantly with age in the 0 rad control group and the 200+ rad exposure group, particularly so in the latter.

Leukocyte counts and coronary heart disease in a Japanese cohort.

Coronary heart disease incidence during 1958-1974, in a cohort of Hiroshima and Nagasaki residents, was found to relate significantly (p = 0.01) to total leukocyte count, taken an average of two years earlier. Relative risks, as a function of leukocyte count, did not appear to depend on sex or cigarette smoking status, but may be larger for subjects less than 65 years of age than for older persons.

Search for mutations affecting protein structure in children of atomic bomb survivors: preliminary report.

A total of 289,868 locus tests, based on 28 different protein phenotypes and using one-dimensional electrophoresis to detect variant proteins, has yielded one probable mutation in the offspring of "proximally exposed" parents, who received an estimated average gonadal exposure of 31 to 39 rem in the atomic bombings of Hiroshima and Nagasaki. There were no mutations in 208,196 locus tests involving children of "distally exposed" parents, who had essentially no radiation exposure.

False-negative results for urinary phenothiazines and imipramine in Forrest's qualitative assays.

When a series of patients' urine samples supplemented in vitro with chlorpromazine or imipramine was assayed with the Forrest qualitative assays, we observed an occasional false-negative result, which we found was attributable to interference by ascorbic acid. It interferes with the reagent, not with the analytes, in both assays. We easily eliminated this interference with the phenothiazine test by using an anion-exchange resin.