Pharmacology of (±)-, (+)- and (–)-2:2-Diphenyl-3-Methyl-4-Morpholino-Butyrylpyrrolidine

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Abstract
(±)-2:2-Diphenyl-3-methyl-4-morpholino-butyrylpyrrolidine (R610) is a more active analgesic agent in mice, rats and guinea pigs than morphine. The analgesic activity is due to the (+)-isomer (R875). The (–)-isomer (R898) is nearly inactive. R610 lowers the body temperature to below control levels in immobilised rats, inhibits the respiration in unnarcotised rats, lowers the blood pressure in unnarcotised rats with experimental renal hypertension, and causes mydriasis in mice. It also augments the action of barbiturates in mice. In all these respects the (+)-isomer is the active compound of the racemic mixture. The (–)-isomer is almost as toxic as the (+)-isomer, which has a broader therapeutic margin than the (±)-form. The dosage-toxicity relation of highly active analgesic agents in mice and rats is irregular especially in the lower dosage range.

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