Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Conjugate addition of pyrrolidine or piperidine to methyl crotonate, and hydrolysis of the resulting methyl butyrates gave the (+/-)-3-pyrrolidino or piperidinobutyric acids 17 and 18, respectively. Coupling of these racemic acids to arylalkylamines, L-phenylalaninamide or L-phenylalanine methyl ester gave the N-substituted butyramides 3-14 which were tested as analgesics using the hot-plate method. (+/-)-N-(2-Phenethyl)-3-(1-pyrrolidinyl)butyramide (6) showed naloxone-attenuated analgesia but was considerably less potent than morphine and of shorter duration of action. Diastereomeric butyramides containing Phe residue (11-14) were less active than 6, but unlike N-arylalkylsubstituted derivatives, showed no toxic effects on locomotor activity at the high doses (30-60 mg/kg) used for testing. In all cases, analgesia was accompanied by an inhibition of spontaneous motor activity and sedation.
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PMID:Synthesis and analgesic activity of N-aryl/arylalkyl 3-(1-pyrrolidinyl/piperidinyl)butyramides. 1048 11