Homologous series of N-methyl-, N-allyl-, and N-cyclopropylmethylmorphinans, differing only in the position of the phenolic hydroxy group, were examined with respect to their binding affinities for the opiate receptor.IC₅₀'s were determined for competition with [³H]naltrexone in the presence and absence of 100 mM NaCl.Compounds with the hydroxy in the 3-position had the highest affinity, but corresponding mols. with the hydroxy in the 2- or 4- position had significant binding affinity ranging from 30 nM in the cyclopropylmethyl series to 400 nM for the 2-hydroxy-N-methylmorphinan.The sodium indexes were also very similar to those of the corresponding 3-hydroxy compoundsThe only 1-hydroxy derivative available was ∼20% as strong as the corresponding 2- and 4-hydroxy compoundsCovering or removing the hydroxy group greatly weakened the binding, but did not totally destroy it.There was good correlation between binding affinity and pharmacol. potency for all except the methoxy compoundsTheir high potency is consonant with in vivo hydrolysis of the Me ether.

03 Feb 1979·The Journal of Clinical PharmacologyQ3 · MEDICINE

Phase I½ Evaluation and Methodology of RO 20–2230 in Postoperative Patients

Q3 · MEDICINE

Article

Author: A R N Carol Canup ; Frank H. Sarnquist ; Colin R. Brown

This report presents the rationale and methodology of our "phase 1 1/2" model for drug evaluation and reports the results of a typical study. We found that Ro 20-2230, and investigational agonist-antagonist analgesic, was well tolerated in therapeutic doses, with 15 mg intramuscular Ro 20-2230 approximately equivalent to 10 mg intramuscular morphine sulfate.

01 Nov 1978·Clinical Pharmacology & TherapeuticsQ2 · MEDICINE

(−)‐2‐Hydroxy‐N‐cyclopropylmethylmorphinan: Radioimmunoassay and pharmacokinetic profile

Q2 · MEDICINE

Article

Author: Erno Mohacsi ; Richard Young ; Harold Boxenbaum ; Alice Holazo ; David Malarek ; Stanley Kaplan ; James Moore ; Ross Dixon ; Mia Parsonnet

The pharmacokinetic profile of (−)‐2‐hydroxy‐N‐cyclopropylmethylmorphinan (HCMM), a narcotic antagonist and analgesic, has been evaulated in man following administration of 25 to 50 mg of the drug orally and 10 to 15 mg intramuscularly. A specific radioimmunoassay procedure was developed for the determination of HCMM in plasma and urine. The drug had a mean “apparent” elimination half‐life in plasma of about 11 hr following both routes of administration. A mean of 47% of the oral dose was excreted in the urine as unconjugated and conjugated HCMM and only 5% of the dose was excreted as intact HCMM. In one subject studied, the plasma levels of conjugated HCMM were as much as 5‐fold higher than the levels of un conjugated drug. Although there was considerable intersubject variability following both routes of administration, the overall pharmacokinetic parameters suggest that oral and intramuscular doses are bioequivalent.

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Indication	Highest Phase	Country/Location	Organization	Date
Pain	Phase 1	-	F. Hoffmann-La Roche Ltd.	-

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