Biologically active quinazoline derivatives — A patent review

Pharmaceutical Chemistry Journal -     

Institutional alternatives to psychotherapy. A study of growth center users.

Are growth centers used as alternative institutions to traditional mental health facilities? Survey methods compared growth centers (N=426) and National Training Laboratories (N=108) participants with clinic patients (N=89). Symptoms, life stress, motivations for participation, process expectations, and various attitudes toward authority, time, and help were assessed prior to participation. Comparisons on degree of psychological distress and avowed motivation indicated that most who attend such activities do so for "psychotherapeutic purposes." Growth centers were found not to be an alternative to traditional psychotherapy, but rather an addition. Eighty percent of the growth center sample had previous or current psychotherapeutic experience. Of the people studied, most go to both rather than to one or the other, and from the perspective of the participants, the institutions do not differ greatly in what they offer, how long the process will take, or what goals will be met.     

Controversy: endoscopic approaches to metastatic thoracic disease

Traditional approaches to thoracic metastases and spinal cord compression have been well worked out and validated in the literature. Anterior decompression is clearly superior to laminectomy; vertebrectomy and reconstruction are indicated for sagittal collapse, instability, and pain; and surgical decompression is necessary in cases of bony impingement. The role of endoscopic and minimally invasive techniques in treatment of metastatic disease is evolving. Dr. Lieberman advocates the use of thoracoscopic anterior approaches as the principal application in these patients, whereas Dr. McLain has found that endoscopic assistance has vastly improved his results with posterolateral decompression. The two authors weigh the relative advantages and disadvantages of these approaches for the selected patient with metastatic thoracic disease.     

Tissue Inhibitor of Metalloproteinase-1 Concentrations are Attenuated in Peritoneal Fluid and Sera of Women with Endometriosis and Restored in Sera by Gonadotropin-Releasing Hormone Agonist Therapy

Objective: To establish tissue inhibitor of metalloproteinase-1 (TIMP-1) concentrations in peritoneal fluid (PF) and sera of women with endometriosis and compare them to disease-free controls.

Design: Prospective randomized study.

Setting: Academic medical center.

Patient(s): Women with laparoscopically documented endometriosis and disease-free women of reproductive age.

Intervention(s): Peritoneal fluid and sera were collected, and some women received gonadotropin-releasing hormone agonist (GnRH-a) therapy for endometriosis.

Main Outcome Measure(s): Peritoneal fluid and sera TIMP-1 concentrations were measured with a specific RIA.

Result(s): The TIMP-1 concentrations were significantly lower in PF and sera of women with endometriosis compared with disease-free women. The GnRH-a therapy restored serum TIMP-1 concentrations.

Conclusion(s): Aberrant expression and localization of TIMP-1 may derange the proteolytic milieu of the peritoneal cavity and contribute to the etiology and underlying physiologic sequelae associated with endometriosis. Measurement of TIMP-1 in serum may aid in diagnosing endometriosis and assist with monitoring treatment efficacy in women with this disease.     

长期服抗精神病药病人的隐性运动障碍

目的：评估抗精神病药对迟发性运动障碍（ＴＤ）的掩盖,即隐性运动障碍（ｃｏｖｅｒｔ ｄｙｓｋｉｎｅ－ｓｉａ）状况。方法应用Ｓｉｍｐｓｏｎ运动障碍评分表评定ＴＤ。入组的６９例病人有２３例病人完成了减药之前、停药三周后和再服药四个月后的ＴＤ评定,６９例次检查都给于隶像,并且两个评定者按照录像独立评定ＴＤ是否存在,评定ＴＤ的一致性良好（ＩＣＣ＝０．７５）。结果完成整个调查的２３例病人中,减药前ＴＤ出现率为     

Characterizing and dating the onset of symptoms in psychotic illness: the Symptom Onset in Schizophrenia (SOS) inventory

Prodromal symptoms, including disturbances of perceptions, beliefs, cognition, affect, and behavior, are often the first symptoms of schizophrenia. Little is understood about the initial, prodromal stage of schizophrenia, despite the compelling research and clinical need. The development and psychometric properties of a new, time-efficient instrument to characterize and date the initial symptoms of a psychotic illnesses, the Symptom Onset in Schizophrenia (SOS) scale, is described in this paper. The SOS rates the presence and dates the onset of 16 general prodromal, positive, negative, and disorganizational symptoms, as well as a clinician, family, and patient global rating of onset of illness. Inter-rater reliability for the presence of each symptom in 35 patients with schizophrenia, schizoaffective, or schizophreniform disorder was good to excellent, with kappa coefficient >0.7 for 12 items, and >0. 5 for all items. Agreement on symptom duration was good to excellent for individual items (ICC=0.7-1.0) and for global rating of duration of illness (ICC=0.97). Our data indicate that the SOS is a reliable, valid, time-efficient tool useful to retrospectively assess the onset of schizophrenia and related psychotic disorders. Further study is underway to evaluate other psychometric properties of the SOS, including test-retest reliability and predictive validity.     

Electrocardiographic ST-segment changes during acute, severe isovolemic hemodilution in humans

BACKGROUND: Controversy exists regarding the lowest blood hemoglobin concentration that can be safely tolerated. The authors studied healthy resting humans to test the hypothesis that acute isovolemic reduction of blood hemoglobin concentration to 5 g/dl would produce an imbalance in myocardial oxygen supply and demand, resulting in myocardial ischemia. METHODS: Fifty-five conscious healthy human volunteers were studied. Isovolemic removal of aliquots of blood reduced blood hemoglobin concentration from 12.8 +/- 1.2 to 5.2 +/- 0.5 g/dl (mean +/- SD). Removed blood was replaced simultaneously with intravenous fluids to maintain constant isovolemia. Hemodynamics and arterial oxygen content (Cao2) were measured before and after removal of each aliquot of blood. Electrocardiographic (ECG) changes were monitored continuously using a Holter ECG recorder for detection of myocardial ischemia. RESULTS: During hemodilution, transient, reversible ST-segment depression developed in three subjects as seen on the electrocardiogram during hemodilution. These changes occurred at hemoglobin concentrations of 5-7 g/dl while the subjects were asymptomatic. Two of three subjects with ECG changes had significantly higher heart rates than those without ECG changes at the same hemoglobin concentrations. When evaluating the entire study period, the subjects who had ECG ST-segment changes had significantly higher maximum heart rates than those without ECG changes, despite having similar baseline values. CONCLUSION: With acute reduction of hemoglobin concentration to 5 g/dl, ECG ST-segment changes developed in 3 of 55 healthy conscious adults and were suggestive of, but not conclusive for, myocardial ischemia. The higher heart rates that developed during hemodilution may have contributed to the development of an imbalance between myocardial supply and demand resulting in ECG evidence of myocardial ischemia. However, these ECG changes appear to be benign because they were reversible and not accompanied by symptoms.     

Properties of vascular ADP-ase

The properties of vascular ADP-ase were investigated in microsomal preparations of rabbit aortic cell homogenates. The enzyme was found to have a Km of 9 microM. Its activity was not affected by substrates for other purine nucleoside phosphatases nor by substrates for non-specific phosphatases. However, ATP and beta-gamma-methylene ATP inhibited the enzyme. None of sodium fluoride, ouabain, neuraminidase affected ADP-ase activity whereas oligomycin potentiated the activity. The enzyme had an SH requirement and a divalent cation requirement.