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A Bashir

Publications and source records attributed to A Bashir.

42 records · Page 3Linked to original sources

Differences in nuclear triiodothyronine binding in rat brain cells suggest phylogenetic specialization of neuronal functions.

The central nervous system depends on thyroid hormones (TH) in regard to its development, maturation, and maintenance of normal functions. As there is much evidence to suggest that the effects of TH are mainly mediated through specific nuclear binding sites, we have studied the anatomical distribution of T3 nuclear receptors in different regions of adult rat brain, and the localization of receptors in the fractionated neuronal and glial nuclei of neocortex, paleocortex, and cerebellum. Purified nuclei from the various brain regions were prepared by ultracentrifugation in 2.2 M sucrose. Purified neuronal and glial fractions were obtained by discontinuous sucrose gradient centrifugation in 2.2 and 2.4 M sucrose. The washed nuclear fractions were used for T3 binding assay at 37 C for 30 min and the data analyzed by least squares nonlinear regression analysis. Nonfractionated nuclei from all regions studied were found to have similar dissociation constant (Kd) values (1.04-1.38 nM) and Eadie-Hofstee plots indicated the presence of an apparently ubiquitous single class of high affinity, low capacity binding sites. The increase in binding from cerebellum (54 +/- 24 fmol/mg DNA; mean +/- SE) to neocortex (666 +/- 89 fmol/mg DNA) showed a caudo-cranial pattern. In fractionated neuronal nuclei, the same trend was observed, only to a greater degree (1628 +/- 266, 994 +/- 76 and 212 +/- 29 fmol/mg DNA in neocortex, paleocortex, and cerebellum, respectively); the difference between corresponding values for glial nuclei of neocortex and paleocortex (357 +/- 139 and 250 +/- 92 fmol/mg DNA, respectively) was not statistically significant, and no specific T3 binding was found in cerebellar glial nuclei. These data suggest that TH may have an important role in neurons from phylogenetically newer regions, concerned with higher mental functions. The caudo-rostral distribution pattern may also indicate a gradient of TH actions in central nervous system regions.

Animals↗

Haemodynamics and plasma concentrations following sublingual GTN and intravenous, or inhaled, isosorbide dinitrate.

We measured plasma nitrate levels and haemodynamics following sublingual glyceryl trinitrate (GTN) (0.5 mg), or isosorbide dinitrate (ISDN) administered intravenously (0.5 mg) or by inhalation (1.25 mg) in 23 patients undergoing cardiac catheterisation for investigation of chest pain. Peak levels were detected at 90 s and 5 min following intravenous and inhaled ISDN respectively and at 3 min following sublingual GTN. Intravenous and inhaled ISDN produced similar plasma levels at 30 s and both were significantly greater than following sublingual GTN. Plasma levels were maintained for longer following inhaled ISDN than intravenous ISDN or sublingual GTN. Haemodynamic responses were qualitatively similar following each treatment; reduction in pulmonary vascular resistance and pressure and left ventricular end diastolic pressure occurred in each group. Heart rate, cardiac output and LV dP/dt.P-1 remained unchanged. Maximal haemodynamic responses were greater following ISDN than GTN, with little difference between the two preparations of ISDN. Haemodynamic responses were more sustained following inhaled ISDN than following sublingual GTN or intravenous ISDN, the latter two being similar in this respect. These findings suggest that inhaled ISDN may provide more rapid and sustained relief from angina than sublingual GTN.

Absorption↗

Pharmacokinetic studies of various preparations of glyceryl trinitrate.

1 The pharmacokinetics and pharmacodynamics of five pharmaceutical preparations of glyceryl trinitrate (GTN) have been studied in six healthy volunteers. 2 Peak plasma GTN levels of 1.4 +/- 0.1 ng/ml were achieved at 3 min after sublingual administration (0.5 mg); 2.8 +/- 0.6 ng/ml and 2.5 +/- 0.3 ng/ml at 2 h and 4 h after Nitrocontin (6.4 mg) and Sustac (6.4 mg) respectively; 2.7 +/- 0.1 ng/ml and 2.5 +/- 0.2 ng/ml at 30 min after the cream (23 mg) and ointment (35 mg) respectively. 3 The mean times to reach half peak plasma GTN levels were 4.2 +/- 0.7 min after sublingual GTN, 6.5 +/- 0.9 h after Nitrocontin, 4.1 +/- 0.7 h after Sustac, 46.1 +/- 10.2 min after the ointment and 50.2 +/- 39.2 min after the cream. 4 Plasma nitrate (NO3) levels were undetectable after sublingual administration; peak NO3 levels were 0.48 +/- 0.03 microgram/ml at 4 h after Nitrocontin, 0.45 +/- 0.02 microgram/ml at 6 h after Sustac, 0.68 +/- 0.04 microgram/ml at 6 h (end of study) after the ointment and 0.63 microgram/ml at 4 h after the cream. 5 Plasma nitrite (NO2) was undetectable after sublingual GTN and peak NO2 levels were 0.48 +/- 0.04 microgram/ml at 2 h after Nitrocontin, 0.48 +/- 0.02 microgram/ml at 2 h after Sustac, 0.69 +/- 0.02 microgram/ml at 1 h after the ointment and 0.64 +/- 0.02 microgram/ml at 1 h after the cream. 6 Blood pressure (BP) declined throughout the 11 min of the study after sublingual GTN but did not change significantly after Nitrocontin or Sustac. After the ointment and the cream BP fell to the lowest level 30-60 min after administration and remained low throughout the 6 h of the study. 7 Heart rate (HR) increased to a maximum 5 min after sublingual administration with no significant increase after Nitrocontin or Sustac. After the ointment and the cream HR increased gradually to a maximum 30-60 min after administration remaining high throughout the rest of the study.

Adult↗

Clinical efficacy of codergocrine mesylate in children with learning difficulties.

A double-blind placebo-controlled study in children showed codergocrine mesylate to be effective in improving cognitive functions and behavioural symptoms associated with learning disorders. Forty randomly grouped children of either sex were given an increasing dosage of codergocrine mesylate and followed up for 12 weeks. A significant improvement was noted in speech (acquisition of new words, comprehensibility/meaningfulness of speech), sociability, attention/concentration, comprehension and memory. Improvement in behaviour (emotional lability and cooperativeness) was also noted. Problems of assessing cognitive progress in very young children with culturally appropriate methods were encountered.

Adolescent↗