Correlation of opiate receptor affinity with analgetic effects of meperidine homologs

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Abstract
The affinity for opiate receptor sites in brain tissue in a series of N-substituted meperidine homologs was compared with the analgetic potency of these compounds in mice. There is a good correlation between affinity for opiate receptor binding sites assayed in the presence of Na and analgetic potency for homologs whose N-substituent has 6 or fewer carbons. The apparent discrepancy between the weak affinity of these drugs for opiate receptors and their fairly potent analgetic effects in vivo can be explained by meperidine''s efficient penetration into brain.