Opioid Analgesics

Medicinal Neurochemistry
MNPC III (46:132)
Instructor: Dr. Horacio F. Olivo

1. General Information

2. Morphine and the Opiates

3. Analogs/Derivatives of Morphine

4. Morphinan Derivatives

5. Benzomorphan Derivatives

6. Piperidine Derivatives

7. "Open chain" Analgesics [Methadone-type compounds]

8. Analgesic Antagonists

9. Analgesic Receptor Theory & Endogenous Opiates

Other sites on opioids you can visit

1. General Information --Syllabus--Click here to download a pdf file

• A. Analgesics
• B. Somatic Pain
• C. Visceral Pain
• Schedule of Controlled Substances (PDF format)

2. Morphine and the Opiates Index

• A. The Opium Poppy
• B. Morphine: Structure, 2D and 3D Drawings.
• C. Isolation.
• D. Metabolism.
• E. Structure Activity Relationships.
• Review Problems (pdf format)
• Handout-1

3. Analogs/Derivatives of Morphine

• heroin
• codeine
• hydromorphone
• hydrocodone
• oxymorphone
• oxycodone
• metopon
• apomorphine
• normorphine
• N-(2-phenylethyl)-normorphine
• thebaine and Diels-Alder Adducts:
• etorphine
• buprenorphine
• Review Problems. Click here to download a PDF file.
• Synthesis of some derivatives of morphine. click here.
• Handout-2

4. Morphinan Derivatives

• racemorphan
• levorphanol
• dextromethorphan
• butorphanol
• levallorphan
• cyclorphan
• Handout-3

5. Benzomorphan Derivatives

• phenazocine
• pentazocine
• cyclazocine
• Handout-4

6. Piperidine Derivatives

• meperidine
• anileridine
• piminodine
• ethoheptazine
• alphaprodine
• betaprodine
• (MPTP)
• diphenoxylate
• loperamide
• fentanil
• sufentanil
• alfentanil
• remifentanil
• Handout-5
• Review Problems. Click here to download a PDF file.

7. "Open chain" Analgesics [Methadone-type compounds]

• Methadone
• isomethadone
• propoxyphene
• LAAM
• Handout-7

8. Analgesic Antagonists

• buprenorphine
• cyclazocine
• cyclorphan
• levallorphan
• nalbuphine
• nalmefene
• nalorphine
• naloxone
• naltrexone
• oxilorphan
• pentazocine
• Handout-8

9. Analgesic Receptor Theory & Endogenous Opiates

• Receptor theories. Click here to download figures used in class.
• Isolation of opiate receptor
• Isolation of endogenous analgesics
• Classification of opioid receptors
• Handout-9

Other sites on opioids you can visit:

• CORD Center for Opioid Research and Design, University of Minnesota
• Chemistry of Opioid Analgesics A Medchem tutorial prepared by Dr. Patrick M. Woster, Wayne State University.
• Ibogaine The Ibogaine Dossier
• Learning Module for Analgesic Drug Design by J.G. Henkel. (This link needs update)
• Narcotic Analgesics. Introduction to Opioids. Notes by Jack De Ruiter (PDF file)
• Narcotic Analgesics. Morphine and Morphine Modified Analogues. Notes by Jack De Ruiter (PDF file)
• Narcotic Analgesics Nuclear Modified Morphine. Notes by Jack De Ruiter (PDF file)