Narcotic agonists and antagonists

Pharmacology Nalbuphine is a potent analgesic with narcotic agonist and antagonist actions. Its analgesic potency is essentially equivalent to that of morphine on a milligram basis. 

Cho TM, Law PY, Loh HH. A proposed mode of action for narcotic agonists and antagonists. In Loh HH, Ross DH, eds. Neurochemical Mechanisms of Opiates and Endorphins. New York Raven Press, 1979 69-102. 

General Procedure for the Isolation and Identification of 6-a- and 6-3-Hydroxy Metabolites of Narcotic Agonists and Antagonists with Hydromor-phone Structure... 

Inhibition constants (Kj) of 26 narcotic analgesic agonists and antagonists as obtained in 4 receptor binding tests (EKC, DHM, DADLE and NAL) [45],... 

Dextromethorphan, contained in many nonprescription cough medicines, will produce a heavy psychedelic trip, but the nausea characteristic of the opiates may constitute a problem. Kosterlitz and Villareal (Eds.) AGONIST AND ANTAGONIST ACTIONS OF NARCOTIC ANALGESIC DRUGS (1972) and Braude et al. (Eds.) NARCOTIC ANTAGONISES (1973) are useful. 

Pentazocine (Talwin) Narcotic analgesic that causes more CNS adverse effects, including confusion and hallucinations, more commonly than other narcotic drugs. Additionally, it is a mixed agonist and antagonist. High... 

H W Kosterhtz, H O J Collier, and J E Villarreal, eds, Agonist and Antagonist Actions of Narcotic Analgesic Drugs, University Park Press, Baltimore (1973)... 

Agonist and antagonist ligands are influenced in the same way by the presence of a phenolic hydropxyl at C-3, as is evident from relative potencies of many free phenol- O-methylated pairs of antagonists (e.g., 32).(32) However, like 3-deoxymorphines and morphinans (p. 119), absence of this feature in antagonists may be compensated by a 4-methoxy substituent. Thus the 4-methoxy derivatives 33 all have had narcotic antagonist action with at least pentazocine-level antinociceptive effects in mice.(86)... 

Narcotic agonist-antagonists are medications that have both agonist and antagonist effects on the opioid receptors. 

Hughes, J., Kosterlitz, H. W., and Leslie, F. M., 1975a, Effect of morphine on adrenergic transmission in the mouse vas deferens. Assessment of agonist and antagonist potencies of narcotic analgesics, Br.J. Pharmacol. 53 371-381. 

Naloxone (XVlIa) Is t only reported narcotic antagonist without other biological activity. This can be demonstrated by an acetylcholine release assay which measures both agonist and antagonist actions of narcotics, as well as by pharmacological studies. In contrast, analogs... 

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