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  • Title: Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP).
    Author: Bøgesø KP, Arnt J, Lundmark M, Sundell S.
    Journal: J Med Chem; 1987 Jan; 30(1):142-50. PubMed ID: 3806591.
    Abstract:
    Eight indolizidine and quinolizidine derivatives of 3-PPP were synthesized and tested for possible dopamine (DA) autoreceptor activity. The equatorial indolizidine derivative 19e had the profile of a selective autoreceptor agonist and was half as active as 3-PPP. However, resolution of the compound revealed that the 8R enantiomer was an unselective DA agonist with a profile similar to (+)-3-PPP, while the 8S enantiomer was a weak DA antagonist without any DA agonist activity. The unsaturated quinolizidine derivative 21 also had the profile of a DA antagonist while the axial quinolizidine derivative 18a had an amphetamine-like profile in 6-OHDA-lesioned rats. All other derivatives were inactive. The observed structure-activity relationships were in agreement with existing DA receptor models, although these models are not apparently detailed enough to explain why the 8S enantiomer of 19e is inactive as a DA agonist.
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