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Metabolic activity, factors modifying

Factors Which Modify Target-Tissue Metabolic Activity ... [Pg.37]

However, there are still many experimental conditions to be considered before this can become the standard method. The observed mutagenic activity is modified by various factors the S-9 fraction is affected by the animal source and the inducers used to enhance drug-metabolizing enzymes in the liver the presence of cofactors, such as ATP and flavin, greatly affects the detection of certain types of chemicals preincubation, which was not carried out in the original method described by Ames et is essential for detection of certain... [Pg.42]

Tables 6.8-6.11 illustrate the wide range of C3 side-chain modified A -THC analogues that have been reported in the literature, together with associated in vitro and in vivo data. The affinity of classical cannabinoid analogues for the CBi receptor has been shown to correlate with depression of spontaneous activity and the production of antinociception, hypothermia and catalepsy in mice, and with psychomimetic activity in humans [93]. However, in some cases, there were unexplained differences between the observed trends in binding affinity and the trends in activity in mouse behavioural models. This may point to differences in efficacy among full agonists, partial agonists and antagonists/inverse agonists, or may reflect differences in in vivo metabolism or blood-brain barrier penetration or a combination of these factors. Tables 6.8-6.11 illustrate the wide range of C3 side-chain modified A -THC analogues that have been reported in the literature, together with associated in vitro and in vivo data. The affinity of classical cannabinoid analogues for the CBi receptor has been shown to correlate with depression of spontaneous activity and the production of antinociception, hypothermia and catalepsy in mice, and with psychomimetic activity in humans [93]. However, in some cases, there were unexplained differences between the observed trends in binding affinity and the trends in activity in mouse behavioural models. This may point to differences in efficacy among full agonists, partial agonists and antagonists/inverse agonists, or may reflect differences in in vivo metabolism or blood-brain barrier penetration or a combination of these factors.

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Active factors

Activity factor

Activity modifier

Metabolic activation

Metabolic factors

Metabolism activation

Metabolism active

Metabolism/metabolic activity

Modifying factor

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