An alternative approach to developing dopamine-receptor agonists with central presynaptic actions following oral administration: A comparison between apomorphine, bromocriptine, and the novel compound RDS-127 (2-di-n-propylamino-4,7-dimethoxyindane)
✍ Scribed by Stephen P. Arnerić; Dr. John P. Long
- Publisher
- John Wiley and Sons
- Year
- 1983
- Tongue
- English
- Weight
- 712 KB
- Volume
- 3
- Category
- Article
- ISSN
- 0272-4391
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✦ Synopsis
Arneric, S. P., and J. P. Long: An alternative approach to developing dopamine-receptor agonists with central presynaptic actions following oral administration: A comparison between apomorphine, bromocriptine, and the novel compound RDS-127 (2-di-n-propylamino-4,7-dimethoxyindane). Drug. Dev. Res. 3221-231, 1983. RDS-127 (2-di-n-propylamino-4,7-dimethoxyindane) is a novel dopamine (DA) receptor agonist with potent central actions. RDS-127, apomorphine (APO), and bromocriptine (BRM) were compared for their ability to inhibit locomotor activity in rats following oral administration. APO, BRM, and RDS-127 produced time-and dose-dependent decreases in locomotor activity. While APO and BRM were equipotent in inhibiting locomotor activity, RDS-127 was 13.5 times more potent than either APO or BRM. A single oral dose of 32.0 p.rnol/kg of RDS-127 decreased locomotor activity greater than 50% for a period of 2 hr. The inhibitory effects of RDS-127 on locomotor activity were blocked by prior administration of sulpiride, suggesting the effects are mediated by DA receptors. While oral administration of APO or RDS-127 generally decreased locomotor activity, similar doses given subcutaneously increased locomotor activity.