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M C Bindal

Publications and source records attributed to M C Bindal.

16 recordsLinked to original sources

Effect of bone injury on circadian periodicity of plasma 17-hydroxy corticosteroids (17-OHCS) in rabbits.

Bone injury inflicted at varying time intervals during 24 hr day-night cycle caused significant varying increase in plasma 17-OHCS levels in all traumatized animals and the levels remained elevated up to 24 hr after trauma. The level of plasma 17-OHCS was found to be aberrated in all the traumatized animals. Thus, adequate adrenocortical response to trauma and aberration in the adrenocortical secretory activity appears inevitable irrespective of the time at which the trauma is produced. However, the degree of response depends on the particular time at which the trauma is inflicted.

17-Hydroxycorticosteroids↗

A quantitative analysis of steric and hydrophobic effects in ribonucleoside diphosphate reductase inhibition by thiosemicarbazones.

Ribonucleoside diphosphate reductase (RDR) inhibitory activity of 2-formylpyridine and 1-formylisoquinoline thiosemicarbazones is quantitatively analysed in relation to a steric parameter (van der Waals volume, VW) and the hydrophobic parameter logP. The activity is found to be significantly correlated with VW and very poorly with logP. On the basis of this, it is inferred that RDR inhibition by thiosemicarbazones is very sensitive to steric effects and is little influenced by the hydrophobic character of the molecules.

Chemical Phenomena↗

QSAR studies on psychotomimetic phenylalkylamines.

Attempts have been made to correlate hyperthermic potencies in rabbits and LSD-like effect in rat of a series of phenylisopropylamines (amphetamines) with physico-chemical parameters. In case of 2,4,5-trisubstituted analogs, hyperthermic potencies are found to be well correlated parabolically with the hydrophobic parameter pi. However, for the same series, the LSD-like effect is found to be related with pi in combination of steric parameter of 4-substituent. It is therefore inferred that hyperthermia in rabbit may be the function only of the hydrophobic character of molecule, but the LSD-like effect is influenced by the steric hindrance of 4-substituent also.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗

Structure-activity studies on hallucinogenic phenylalkylamines using Fujita-Ban approach.

The nature of the substituents and their contribution at different ring positions to the overall hallucinogenic activity in a series of phenylalkylamines (amphetamines) are studied by using Fujita-Ban additive model. The calculated activity contributions of substituents and of parent structure, respectively, are then utilized to predict the most potent compound in the series and to remove the uncertainties in the observed activity of some phenylalkylamines. The most potent compound predicted is 2,6-dimethoxy-4-bromophenylisopropylamine.

Amines↗

Quantitative structure-activity studies on hallucinogenic mescaline analogs using modified first order valence connectivity.

Attempt is made to correlate the hallucinogenic activity of a series of mescaline analogs with Kier's molecular connectivity index (chi). In order to find a simpler and more meaningful correlation, a little modification is suggested to the first-order valence connectivity index (1 chi upsilon). The modification is found to reveal utterly simple but significant correlations between activity and 1 chi upsilon, which could describe the structural influence on the activity more vividly.

Chemical Phenomena↗

QSAR studies on phenylalkylamines interacting with the serotonin receptor.

An attempt is made to analyse the serotonin receptor binding affinity (pD2) of a small series of hallucinogenic phenylalkylamines in relation to various physical and physico-chemical parameters. It is found that pD2 can be significantly correlated with steric parameters, such as van der Waals (Vw) and molar refraction (MR). Based on the correlation equations obtained, it is suggested that the hallucination might be related with binding of drug with the serotonin receptor and that such binding might involve a van der Waals type of interaction.

Amines↗

Correlation of inhibitory activity of tryptamine derivatives on serotonin uptake in thrombocyte with van der Waals volume.

A study is made on the correlations of inhibitory activity of a series of tryptamine derivatives on serotonin uptake in thrombocyte with van der Waals volume (Vw). Bearing significant correlations, the compounds were separated into two distinct groups to conform the suggestion that two receptor sites of a sterically dissimilar nature may be involved in serotonin uptake and its inhibition. And on the basis of significance of the correlation, it was further sought to suggest that to act as inhibitors the compounds must possess the structural resemblance with serotonin at least while complexing with receptor sites.

Binding, Competitive↗

The relationship of cellular respiration inhibition activity of 7-substituted 4-hydroxyquinoline-3-carboxylic acids with van der Waals volume.

The cellular respiratory inhibition activity of 7-substituted 4-hydroxyquinoline-3-carboxylic acids recently designed by Shah and Coats is found by regression analysis to be significantly correlated with van der Waals volume (V(w)). A parabolic correlation is obtained in case of ascites cell inhibition and a linear correlation in case of malate dehydrogenase inhibition. The correlation of both types of inhibition with a single parameter, V(w), makes the process of substituent selection in designing more potent inhibitors of whole respiratory cell much simpler.

Ascitic Fluid↗