Preparation and bioevaluation of 99mTc-carbonyl complex of 5-hydroxy tryptamine derivative.

Studies on the development of imaging agents for targeting neuroreceptors is an area of considerable interest owing to the limited availability of specific as well as selective radiolabeled agents. Therefore, with an aim of developing a receptor-specific agent, iminodiacetic acid (IDA) derivative of 5-hydroxy tryptamine viz., HTIDA has been synthesized. HTIDA could be radiolabeled with the synthon [(99m)Tc(CO)(3)(H(2)O)(3)](+) in >98% yield. The biodistribution studies in normal Swiss mice showed that the (99m)Tc(CO)(3)-HTIDA crosses the blood-brain barrier successfully with a brain uptake of 0.5%ID/g at 5min post injection. The other relevant observations from biodistribution studies included no significant uptake in any other organ and fast clearance from blood, lungs and liver.     

Awareness of warning symptoms and risk factors of stroke in the general population and in survivors stroke.

Awareness among the general population of the risk factors and warning symptoms of stroke is essential for preventative purposes and for immediate effective treatment. The aim of the present study was to assess the awareness, among the general population and stroke survivors, of the risk factors and warning symptoms of stroke, to develop an educational strategy for its prevention and immediate effective treatment. Six hundred and sixty stroke patients (370 male, 290 female) and 4000 people from the general population who accompanied the patients (2800 male, 1200 female) were interviewed, using three sets of questionnaires, on the risk factors and warning symptoms of stroke. Poor knowledge or awareness of the risk factors and warning symptoms of stroke was found in both groups. Both groups suggested educational programs for stroke using printed information, audiovisual programs and community survey programs using simple and understandable information for the prevention and immediate effective treatment of stroke. Poor awareness of stroke contributes to a delay in the arrival of patients in hospital emergency departments for immediate effective treatment. Multifaceted programs regarding stroke, including printed information, audiovisual programs and stroke service programs, are advocated by both patients and the general population to improve stoke treatment and prevention.     

Short term effect of diltiazem on portal hypertension in patients with non-cirrhotic portal fibrosis

Fourteen patients of non-cirrhotic portal fibrosis (NCPF) with portal hypertension were put on oral diltiazem hydrochloride (90 mg/day) or placebo on a prospective, randomised, single blind basis for 15 days. Predrug hemodynamic and biochemical status were similar in both groups. Diltiazem produced significant reduction (p less than 0.001) in mean intrasplenic pressure: from 41.88 (SD +/- 6.18) to 21.5 (+/- 7.91) cm of normal saline as against 45.56 (+/- 9.45) to 43.33 (+/- 8.27) in the placebo group. Mean arterial pressure (MAP), heart rate and cardiac output (CO) did not change in either group. Thus, the calcium channel blocker diltiazem reduces portal pressure in patients with NCPF, independent of reduction in MAP and CO; this is advantageous in situations where compromised cardiac hemodynamics may prove deleterious.     

Painful sensory symptoms in neuroleptic-induced extrapyramidal syndromes.

OBJECTIVE: The authors tested the hypothesis that neuroleptic-induced extrapyramidal syndromes are associated with painful sensations objectively conforming to the characteristics of primary sensory symptoms as reported in idiopathic and postencephalitic parkinsonism. METHOD: The frequency of subjective painful sensory symptoms and their relation to neuroleptic-induced extrapyramidal syndromes were examined in a consecutive series of 107 psychiatric patients newly admitted to acute care units at a teaching hospital. Patients without illnesses or conditions likely to be associated with pain were included in the study if they had a diagnosis other than organic mental syndromes and were receiving psychotropic medications as prescribed by their treating physicians. Structured interviews with a modified version of the McGill Pain Questionnaire to assess sensory complaints and neurological examinations for neuroleptic-induced extrapyramidal syndromes (parkinsonism and akathisia) were conducted independently by two raters blind to each other's findings and patients' medication status. RESULTS: Fourteen (23%) of 60 patients receiving neuroleptics reported experiences of spontaneous pain subjectively attributed to pharmacological treatment, compared with only one (2%) of 47 patients receiving psychotropic medications other than neuroleptics. There was no difference between these two groups in subjective complaints of paresthesia (8% versus 9%). Twelve (55%) of the 22 patients with neuroleptic-induced extrapyramidal syndromes reported pain, compared with only two (5%) of the 38 patients who received neuroleptics but did not experience extrapyramidal syndromes. CONCLUSIONS: Although consonant with the study hypothesis, these results should be regarded as preliminary and interpreted conservatively in the light of the methodological limitations of the study.     

Observation on serum prolactin in hepatic cirrhosis.

Serum prolactin assays in patients of hepatic cirrhosis were analysed. Patients with cirrhosis had higher values of serum prolactin (27.2 +/- 5.1 ng/ml in males and 38.4 +/- 4.1 ng/ml in females) as compared to control subjects (p less than 0.05). Majority of patients of cirrhosis with suspected portal-systemic encephalopathy had significantly higher serum prolactin than those without encephalopathy (p less than 0.05). Significantly higher values of serum prolactin on admission had positive correlation with mortality (p less than 0.01). Clinico-biochemical severity of hepatic dysfunction was directly correlated with level of serum prolactin. The present study reveals the possibility of diagnostic and prognostic values of serum prolactin in cirrhosis, specially in clinical/sub-clinical subsets of portal-systemic encephalopathy.     

Transmission of dengue virus-induced helper signal to B cell via macrophages.

The helper T cells (TH) generated in dengue type 2 virus (DV) infection of mice produce a soluble helper cytokine (HF) which enhances the clonal expansion of DV-specific IgM antibody plaque forming cells (PFC). The present study was undertaken to investigate the mechanism of transmission of the helper signal from TH and HF to B cells. It was observed that TH could transmit the helper signal to B cells by direct cell to cell contact, but HF could not do so without the presence of live macrophages (M phi). HF was adsorbed by both heat killed and live M phi but the former could not transmit it to B cells. Both the polypeptide chains of HF bind to M phi. HF remains on the surface of M phi and can be retrieved completely by contact with B cells for 40 min. The helper signal from TH or HF-adsorbed M phi could not be transmitted to B cells when they were separated from each other by a cell impermeable membrane. The enhancement of PFC count is greater when the signal is transmitted by HF-adsorbed M phi as compared to that by TH alone. Thus, even with lower frequency of TH a significant number of B cells may be triggered with the help of HF and M phi. The findings thus show that the DV-specific helper signal could be transmitted only by a close physical contact of the plasma membranes of the signal presenting cells (TH or HF-adsorbed M phi) and B cells.     

Clastogenic effect of fenfluramine in mice bone marrow cells in vivo

Fenfluramine, an amphetamine derivative used in the treatment of obesity, has been evaluated in vivo in the bone marrow cells of Swiss albino mice using two cytogenetic endpoints for assessing its genotoxic and clastogenic potentials. Concentrations of 0.75, 1.5, 3.0, and 5.0 mg/kg b.w. were administered orally for the study of sister chromatid exchange frequencies and chromosome aberrations (CA). SCE frequencies showed a positive dose response; 1.5 mg/kg being the minimum effective concentration. Fen caused a prolongation of cell cycle at all concentrations. Except for the minimum therapeutic dose (0.75 mg), all other doses (1.5, 3.0, and 5.0 mg) showed a significant increase in the percentage of damaged cells over that of the vehicle control. The degree of clastogenicity was directly proportional to the dosage used and inversely related with the duration of treatment. A gradual reduction of the clastogenic potential was observed after 12 and 24 hr of exposure, indicating that the maximum effect occurs at the middle or late synthetic phase of the cell cycle. This study, probably the first detailed screening of the drug for its genotoxicity, shows that Fen is moderately clastogenic and a DNA damaging agent in vivo.