Opioids pharmacology

Rossiter A, Souney PF. Interaction between MAOIs and opioids pharmacologic and clinical considerations. Hosp Formul 1993 28(8) 692-8. 

The morphine molecule possesses five asymmetric centers at carbons 5(R), 6(S), 9(R), 13(5), and 14(1 ), and it is this geometry that affords the familiar opioid pharmacological actions. The C-9 to C-13 ethanamino bridge restricts the number of possible optical isomers to 16 (i.e., eight racemic pairs). 

Morphine, with the opposite geometry at each of the five chiral centers, does not elicit opioid pharmacological responses. 

A study of the limits of rotational mobility of the aromatic ring relative to the piperidine unit and commensurate with opioid pharmacological responses has been commenced at NIH.(34) The importance of the torsion angle between these moieties has been a point of comment in the prodine series/35 36 By formally joining the 2 position of the phenyl ring of a 5-arylmorphan to the 6-position of the morphan moiety, a rigid congener would result (24). The NIH synthetic pathway to such a compound is outlined in Scheme 5.5. The key step is a photocyclization from 22 to the partially reduced dibenzofuran 23. 

Pasternak GW (2001) Eisights into mu opioid pharmacology die role of mu opioid receptor subtypes. Life Sci 68 2213—2219. 

Several advancements in opioid pharmacology during recent years could have a significant impact on the types of compounds used as narcotic analgesics in the future. The involve-... 

The goal of identifying potent analgesics free of the side effects of morphine and other narcotics has remained elusive. As more information has become available about opioid receptor structure, opioid pharmacology, and related systems (i.e., the ORLl receptor), this has provided new challenges to medicinal chemists to prepare compounds with unique pharmacologicalprofiles. With the diversity of... 

A. Herz, H. Akil, and E. J. Simon, Eds., Opioids I and Opioids 77, Handbook of Experimental Pharmacology, Vols. 104/1 and 104/ II, Springer-Verlag, Berlin, 1993. Two volumes containing comprehensive reviews of opioid pharmacology. 

Trescot AM, Datta S, Lee M, Hansen H (2008) Opioid pharmacology. Pain Physician 11 S133-S153... 

Prisinzano TE, Rothman RB (2008) Salvinorin A analogs as probes in opioid pharmacology. Chem Rev 108 1732-1743... 

Pasternak GW. Insights into mu opioid pharmacology the role of mu opioid receptor sub-types. Life Sci 2001 68 2213-9. 

Gourlay G K (2005). Advances in opioid pharmacology. Support Care Cancer. 13.T53-159. 

As an analgesic agent, hydrocodone bitartrate is used for the symptomatic relief of temporary pain that is moderate to moderately severe, such as acute postoperative pain. It may also be appropriate for the symptomatic treatment of pain associated with acute medical disorders, particularly in the treatment of migraine headaches. For the treatment of chronic non-malignant pain, hydrocodone bitartrate preparations should only be used when non-opioid pharmacological and non-pharmacological modalities have been exhausted and fail to provide measurable symptomatic relief. In the management of severe chronic pain associated with cancer or other terminal illness, hydrocodone... 

G. W. Pasternak, Molecular insights into p opioid pharmacology from the clinic to the bench, Clin. J. Pain, 2010, 26(Suppl. 10), S3-S9. 

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