Locomotor activity in reserpinised rats

Both compounds 34 and 35 induced a significant increase in locomotor activity in reserpinised rats (Figure 4.5). The basal level of locomotor activity of reserpinised rats is maximally 48.5 18.8 counts per 15 min (n = 4) as measured upon s.c. administration of saline. When comparing their maximum effect on locomotor activity as measured by the number of counts over 15 min, compound 34, in a dose of 10 pmol/kg, induced an increase in locomotor activity to 600 counts/15 min, which returned to basal levels after 60 min. In a dose of 30 pmol/kg the maximum effect was 750 counts/15 min, which returned to basal levels after 90 min. The effects of compound 35 in the same doses were less pronounced than those for compound 34. In a dose of 10 pmol/kg compound 35 induced an increase in locomotor activity to maximally 300 counts/15 min and in a dose of 30 pmol/kg the maximum effect was 650 counts/15 min The latter returned to basal levels after 105 min. 

In the present study, a series of thiophene analogues of 2-aminotetralins and hexahydronaphthoxazines were studied in vivo for their ability to decrease striatal dopamine release, their effects on locomotor activity, and their behavioural characteristics in reserpinised rats, in order to investigate whether a thiophene moiety can act as a bioisostere for the phenol moiety. 

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