Behavioural activation

DA antagonists are anti-emetic, elevate plasma prolactin and have major motor and behavioural effects. Thus DA must be involved in the initiation of vomiting, the secretion of prolactin and control of motor and behavioural activity. Its role in emesis and as the prolactin release inhibitory factor have been adequately covered above. Its motor and behavioural function will now be considered. 

Although some studies show that noradrenaline inhibits neuronal firing it is generally considered to increase behavioural activity and arousal. This impression is borne out to the extent that CNS stimulants, like amphetamine, increase release of noradrenaline and produce behavioural and EEG arousal, while reserpine, which reduces noradrenaline storage and hence release, causes psychomotor retardation. It is also supported by... 

DR Cooper, C Marrel, H Van de Waterbeemd, B Testa, P Jenner, C D Marsden. L-Dopa esters as potential prodrugs Behavioural activity in experimental models of parkinson s disease. J Pharm Pharmacol 39 627-635, 1987. 

Structure elucidation of the female-produced sex pheromones of Trogo-derma spp. has a rather confused history. Extracts of females of T. inclusum were shown to contain (Z)-14-methyl-8-hexadecenol and the methyl ester of the respective carboxylic acid [215]. The corresponding compounds showing (E)-configuration were shown to be present and behaviourally active in T. inclusum [216]. Finally, investigations of head space collections, obtained with live females, revealed the presence of 14-methyl-8-hexadecenal, an aldehyde... 

Weevils do not seem to be very sensitive to the presence of non-natural stereoisomers of their pheromones, since racemic mixtures proved to be active in the field. This greatly facilitates their use in large-scale integrated pest management. Some species also contain ketones, corresponding to the pheromone alcohols however, they do not show behavioural activity. 

D. R. Cooper, C. Marrel, H. van de Waterbeemd, B. Testa, P. Jenner, C. D. Marsden, l-Dopa Esters as Potential Prodrugs Behavioural Activity in Experimental Models of Parkinson s Disease , J. Pharm. Pharmacol. 1987, 39, 627 - 635 D. R. Cooper, C. Marrel, H. van de Waterbeemd, B. Testa, P. Jenner, C. D. Marsden, L-Dopa Esters as Potential Prodrugs Effect on Brain Concentration of Dopamine Metabolites in Reserpi-nized Mice , J. Pharm. Pharmacol. 1987, 39, 809-818. 

Nilsson OG, Kalen P, Rosengren E, Bjorklund A. 1990. Acetylcholine release in the rat hippocampus as studied by microdialysis is dependent on axonal impulse flow and increases during behavioural activation. Neuroscience 36(2) 325-338. 

Central nervous system - behavioural activity, sensory/motor responses and body temperature... 

The influence of chain length and side-chain modifications of ACTH-derived peptides on active avoidance behaviour in rats will be discussed. H-Met(02)-Glu-His--Phe-D-Lys-Phe-OH (Org 2766) emerged from these studies as an orally active peptide with an increased potency and selectivity of action. Physico-chemical data (from the literature) on the reference peptide ACTH--(4-10) did not point to a preferred conformation in solution, whereas in the crystalline state an antiparallel 3-pleated sheet structure was found. At the receptor site we suggested an a-helical conformation in which the Phe and Met residues are close together. Additional support for this suggestion came from the behavioural activity of [des-Tyr", Met ]enkephalin and of cyclo--(-Phe-Met-cAhx-), eAhx merely serving as a spacer. 

The relationship between the structure of a series of peptides derived from the adrenocorticotropic hormone ACTH, and the behavioural activity in an active avoidance behaviour test, has been studied over the past 10-20 years. The results obtained were quite different from those in which endocrine activity relationships were studied. From the outcome of a quantitative study on the structure--behavioural activity of the ACTH-related peptides, suggestions about the spatial interactions at the receptor site were made. This receptor-bound conformation differed from those suggested by solution experiments or found in crystal structures. 

In this paper we will illustrate the line of research that was followed in the structure-behavioural activity work and that resulted... 

Strategy and results of the structure-behavioural activity studies... 

In a chromatographic separation procedure the parameters of the chromatographic system (stationary phase, flow, temperature, etc.) have to be selected respectively optimized with respect to some criterion (resolution, time, etc.). In gas chromatography retention data series are published and used for the sttidy of solvent/solute interaction, prediction of the retention behaviour, activity coefficients, and other relevant information usable for optimization and classification. Several clKmometrk techniques of data anal s have been employed, e.g. PCA, numerical taxonomic methods, information theory, and j ttern recognition. 

Figure 6.1. Schematic drawing of the holeboard apparatus used to record behaviour of rats. The box is 70 70 cm and has 32 holes in the floor (circles). The position of photobeams recording nonspecific behavioural activity (variable x,) are indicated by black triangles. These photobeams also record the two locomotion variables (x2 and x3) indicated by arrows. The frequency and accumulated duration of hole visits, comer visits and raising on the hind-legs (variables x4-x9) are recorded by separate photocells [2J. The 10th variable is the ratio between the activity during the second and the first half...

Stone EA, Lin Y, Rosengarten H, Kramer HK, Quartermain D. Emerging evidence for a central epinephrine-innervated ai-adrenoceptor system that regulates behavioural activation and is impaired in depression. Neuropsychopharmacology 2003 28 1387-1399. 

If attempts to relate biochemical with behavioural events are to be meaningful, the dynamic character of the two sets of events must be adequately controlled for. A powerful way of obtaining such control is to exploit the stability of inherited differences between strains of animals. Data from a number of experiments illustrating this genetic approach are described. Further it is argued that biochemical events can be directly related to behavioural activity with the use of biometrical genetics. 

Butler PD, Weiss JM, Stout JC et al. Corticotropin-releasing factor produces fear-enhancing and behavioural activating effects following infusion into the locus ceruleus. J Neurosci 1990 10 176-183. 

It is not always easy to find direct correlations between the heats of adsorption and the catalytic behaviour (activity and/or selectivity). Various attempts at establishing such correlations have been reported in the literature. For instance, a comparison of microcalorimetric measurements with kinetic studies performed over acidic zeolites for methylamine disproportionation reactions, methanol dehydration, and reactions of methanol and dimethylether with methylamines, suggests that acid sites are required in these reactions for the strong adsorption of ammonia and methylamines, while weak adsorption sites are required to facilitate desorption of adsorbed amine species from the acid sites [147]. 

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