Add time:08/16/2019         Source:sciencedirect.com

The object of this study was to determine if the newly developed phenanthridine derivative, CY 208–243, retains its apparent in vivo preference for dopamine D-1 receptors under conditions of dopamine depletion, as a starting point to understanding why CY 208–243 possesses antiparkinson activity and the selective D-1 agonist SKF 38393 does not. Three hours after receiving reserpine (5 mg/kg), mice were strongly sedated and completely unresponsive to the motor stimulant effects of CY 208–243 (0.1–10 mg/kg) or the selective D-2 agonist RU 24213 (0.5–5 mg/kg) administered alone. After 24 h reserpine, the akinesia was partially and dose-dependently reversed by both CY 208–243 (0.1–10 mg/kg) and RU 24213 (0.5–5 mg/kg) alone. CY 208–243 also stimulated rearing and grooming, while RU 24213 gave rise to strong head-down sniffing. The response to 1 mg/kg CY 208–243 was practically abolished by pretreatment with the D-1 antagonist SCH 23390 (0.2 mg/kg). On the other hand, blocking D-2 receptors with metoclopramide (0.25 mg/kg) unexpectedly facilitated CY 208–243-induced locomotion and rearing, but suppressed grooming. When CY 208–243 (1 mg/kg) was injected together with RU 24213 (0.5–5 mg/kg), the two drugs interacted synergistically to stimulate locomotion at all times after reserpine. These animals also exhibited of CY greater preponderance of grooming, sniffing, gnawing and oral dyskinesia. Apart from the potentiation of some elements of CY 208–243 stimulated motor behaviour by D-2 blockade, these results are qualitatively indistinguishable from those previously obtained with the prototype D-1 agonist SKF 38393. The differences between the antiparkinson efficacies of these two drugs are discussed in terms of multiple D-1 receptors, and as yet undisclosed receptor actions of CY 208–243.

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