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Biomedical subjects

A Goldstein

Publications and source records attributed to A Goldstein.

At least 217 records · Page 12Linked to original sources

The naloxone test for opiate dependence.

Naloxone tests for opiate dependence were given to 296 applicants for treatment with the surrogate opiate levomethadyl acetate (LAAM, levo-alpha-acetylmethadol) and to 103 applicants for treatment with the opiate antagonist naltrexone. Thirty-five of the 296 LAAM applicants applied first for LAAM, then following detoxification, for naltrexone. There was a dramatic decrease in withdrawal signs and symptoms when the subject went from opiate-dependent to a nondependent state. From our experience, we devised a scoring guide and testing procedure based on objective signs. We propose a 2-step test, with an initial intramuscular dose, then (if necessary) an intravenous dose, to determine an applicant's eligibility for surrogate opiate or narcotic antagonist treatment.

Humans↗

Immunoreactive dynorphin in pituitary and brain.

Distribution of the potent opioid peptide dynorphin has been determined in pituitary gland (pig, beef, rat), in the various regions of rat brain, and in rat spinal cord, by using a highly specific antiserum. By gel permeation chromatography in 4 M guanidine, the porcine pituitary immunoreactivity is found in a major peak of apparent molecular weight about 1700 and a minor peak of about 3400. Similar peaks are found in rat pituitary extracts, whereas rat brain contains, in addition, two peaks of larger apparent molecular weight. In the pituitary, immunoreactive dynorphin is found predominantly in pars nervosa. In the central nervous system, it is distributed widely, with highest concentrations in hypothalamus, medulla-pons, midbrain, and spinal cord. Although dynorphin contains leucine-enkephalin, the regional distribution of dynorphin is different from that of enkephalin or of any other known opioid peptide.

Animals↗

Synthesis of 3-O-demethylfortimicins.

Treatment of fortimicin B with lithium in ethylamine gave 3-O-demethylfortimicin B. The latter was converted by methodology developed with fortimicin B to 3-O-demethylfortimicin A, 4-N-sarcosyl-3-O-demethylfortimicin B, 4-N-beta-alanyl-3-O-demethylfortimicin B, and 4-N-(beta-aminoethyl)-3-O-demethylfortimicin B. 3-O-demethylfortimicin A and the 4-N-acyl-3-O-demethylfortimicins B had appreciably higher antibacterial activities than the corresponding parent fortimicins. Most significant was the increased activity of 3-O-demethylfortimicin A relative to fortimicin A against a variety of strains of Pseudomonas aeruginosa.

Aminoglycosides↗

Plasma beta-endorphin immunoreactivity in schizophrenia.

Plasma beta-endorphin-like immunoreactivity was measured by a method that was equally sensitive to beta-endorphin and [Leu5]-beta-endorphin. Immunoreactivity in 98 schizophrenic patients did not differ greatly from that in 42 normal subjects. No immunoreactivity was detectable in dialyzates from first-time hemodialysis of eight nonpsychotic renal patients and nine schizophrenic patients. These results are not compatible with recent reports of extremely high concentrations of [Leu5]-beta-endorphin in hemodialyzates from schizophrenic patients.

Adult↗

Pharmacological and immunological characterization of the Leu5 analogue of human beta-endorphin.

The potencies of beta h-endorphin, Met (O)5-beta h-endorphin, and synthetic Leu5-beta h-endorphin have been compared in three bioassays of opioid activity, and in two radioimmunoassays. In all assays, a peptide isolated from hemodialysates from a psychotic patient behaved like Leu5-beta h-endorphin; it has been distinguished unambiguously from beta h-endorphin and Met(O)5-beta h-endorphin. Leu5-beta h-endorphin was one-fifth as potent as beta h-endorphin in guinea pig ileum myenteric plexus, but was only slightly less active in mouse vas deferens and in guinea pig brain opiate receptor binding assay. The low cross-reactivity of Leu5-beta h-endorphin relative to beta h-endorphin with an antiserum raised to beta-endorphin suggests that the preferred solution conformations of these peptides are different. In all bioassays beta h-endorphin was 2- to 3-fold less potent than beta c-endorphin.

Animals↗

Ethylene glycol-water mixture for use in ultrasound test objects.

Ethylene glycol-water mixtures have been found suitable for use in ultrasound test objects. A plot of the required percentage of ethylene glycol with room temperature for an acoustic velocity of 1540 m/sec is presented to aid the clinical user. The velocity measurements performed are shown to be dominated by near-field transient diffraction effects. A 30 percent ethylene glycol-water mixture has been found to have a constant acoustic velocity of 1638 +/- 3.5 m/sec over a wide temperature range (15.6 degrees C-38.4 degrees C). This mixture is suitable for a test object velocity standard. Proper use of the A.I.U.M. 100-mm test object is discussed.

Acoustics↗

Levo-alpha-acetylmethadol (LAAM) in the treatment of heroin addicts. I. Dosage schedule for induction and stabilization.

One hundred and seventy-nine patients who were dependent on street narcotics were inducted into LAAM. Ninety-two were inducted using a slow schedule: 20, 20, 30, 30, 40, 40, 50, 50, 60, 60, 70, 70, 75 mg on successive clinic visits (Mon., Wed., Fri.). Only 23% of the patients followed this schedule to 50 mg; 55% requested and received a faster induction. Eighty-seven patients were inducted using a rapid schedule: 20, 30, 40, 40, 50 mg. This schedule was acceptable to the majority of patients and caused no complaints of overdosing. We suggest that this schedule be used in clinics where patients who have been shown to be dependent are inducted directly onto LAAM.

Adult↗

Dynorphin-(1-13), an extraordinarily potent opioid peptide.

We describe the opioid properties of a tridecapeptide, the sequence of which corresponds to the NH2-terminal sequence of dynorphin, a novel porcine pituitary endorphin. It contains [Leu]enkephalin. In the guinea pig ileum longitudinal muscle preparation it is about 700 times more potent than [Leu]enkephalin. Its effects in this tissue are blocked completely by naloxone, but the apparent affinity of naloxone is 1/13th that for blockade of [Leu]enkephalin or normorphine. In the mouse vas deferens, this peptide is 3 times more potent than [Leu]enkephalin. Well-washed rat brain membranes degrade the peptide rapidly, suggesting the presence of a membrane-bound degradative enzyme. The peptide displays considerable immunoreactivity in assays with antisera that have been used for the immunohistochemical localization of [Leu]enkephalin. The remarkable enhancement of the potency of [Leu]enkephalin by the COOH-terminal extension -Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys-OH suggests new interpretations concerning the structure of opiate receptors and the function of the enkephalin pentapeptides.

Amino Acid Sequence↗

Thymosin modulation of suppressor function in mice and man.

The effect of thymosin on suppressor-cell function was evaluated in vivo in a murine tumor system and in vitro on human lymphocytes. In mice, the Lewis tumor system was used. We showed that splenocytes from tumor-bearing animals were able to enhance tumor growth in a syngeneic system. This enhancement was similar when thymocytes from tumor-bearing animals were used and disappeared after anti-Thy 1-2 antiserum treatment, suggesting a T-dependence. Treatment of the tumor-growth-enhancing lymphocytes with corticosteroids or irradiation caused this effect to disappear completely suggesting that the tumor-growth-enhancing T-lymphocytes were suppressor T-cells. Furthermore thymosin (fraction 5)-treated, tumor-growth-enhancing T-lymphocytes were not able to enhance tumor growth and even significantly decreased it. In the human system we showed that Con A-stimulated lymphocytes were able to suppress the response of normal lymphocytes to PHA, PWM, and Con A, and in MLC. This effect was significantly blocked in presence of thymosin fraction 5.

Animals↗

Experimental alterations of endorphin levels in rat pituitary.

Endorphin (END) levels in rat pituitary were assessed with the opiate receptor binding assay. Procedures reported to alter hormone secretion from END-rich intermediate or anterior lobes were examined for their effect on END content. Lesions of the paraventricular nucleus (PVN) had no significant effect on END content. Ingestion of 2% NaCl reduced END levels in a significant majority of the animals. Suckling, a natural physiological stimulus, significantly elevated neurointermediate lobe END. Footshock and immobilization each evoked 40--50% reductions in anterior lobe END content. Pituitary ENDs are thus affected by many of the same stimuli that also promote release of a number of peptide hormones derived from the same biosynthetic precursor. However, separate mechanisms likely exist for control of secretion of these peptides from anterior and neurointermediate lobe.

Animals↗

Measurement of urine temperature as an alternative to observed urination in a narcotic treatment program.

Upper and lower limits have been determined for the temperature of freshly voided ur;ne. When specified procedures are followed, more than 99% of measurements lie between 32.5 and 36.7 degrees C. This provides a basis for monitoring urine collection in a drug abuse treatment program in a manner that does not invade privacy. The method is not foolproof, but it provides sufficient control if there are no penalties for illicit drug use so that there is no strong incentive to turn in a fraudulent urine sample.

Adult↗

Reduced T cell reactivity in vasectomized rhesus monkeys: association with histocompatibility type.

The capacity of peripheral lymphocytes from rhesus monkeys which had been vasectomized for 7 or 11 years to stimulate and respond to normal rhesus lymphocytes in mixed lymphocyte cultures (MLC) was tested to determine whether vasectomy affects immunologic reactivity. The ability to respond in MLC, a T cell function, was significantly reduced in the 11-year vasectomized animals and in two 7-year vasectomized animals. The ability to stimulate in MLC, a B cell function, was significantly increased in the 11-year vasectomized group. MLC reactivity of normal lymphocytes cultured in plasma from vasectomized animals and lymphocytes from vasectomized animals cultured in normal plasma was not altered, ruling out serum effects in the reduction of MLC responsiveness in these vasectomized animals. Seventy-five per cent of the vasectomized animals with markedly reduced MLC reactivity had the RhL-A determinates 19 and 24, indicating an association between the tendency toward reduced MLC reactivity after vasectomy and histocompatibility type.

Animals↗