Opioid receptors, binding

Su, T.P. Evidence for sigma opioid receptor Binding of 3H-SKF-10,047 to etorphine-inaccessible sites in guinea-pig brain. J. Pharmacol Fxp Ther 223 284-290, 1982. 

Fadda P., Martellotta M. C., De Montis M. G., Gessa G. L., Fratta W. (1992). Dopamine D1 and opioid receptor binding changes in the limbic system of sleep deprived rats. Neurochem. Int. 20 (Suppl.), 153S-156S. 

Quirion R., Pilapil C., Magnan J. Localization of kappa opioid receptor binding sites in human forebrain using [3H]U69,593 Comparison with [3H]bremazocine. Cell Mol. Neurobiol. 7 303, 1987. 

Several reports are available on the biological activities of thioamide derivatives. The thioamide derivatives have shown significant activities, such as antituberculosis drug, anti-influenza virus activity, antitumor activity, anthelmintic activity, opioid receptor binding property, etc.94 101... 

Compd. R X Ar Opioid receptor binding K, (nM) kappa mu mujkappa Ref. 

Table 3.4. OPIOID RECEPTOR BINDING SELECTIVITY OF ZT-52656A (42) COMPARED WITH OTHER KAPPA-SELECTIVE AGONISTS [63]...

Compound No. Opioid receptor binding (IC onM) Smooth muscle assay (ICso nM) ... 

Wahlstrom, A., Lenhammar, L., Ask, B., Rane, A. Tricyclic antidepressants inhibit opioid receptor binding in human brain and hepatic morphine glucuronidation. Pharmacol. Toxicol. 75(1), 23-27, 1994. 

Figure 4 Cellular effector system, activated by opioid receptor binding.

Opioid receptor binding Alfentanil is a (j-selective opioid (Cookson et al., 1983) with a receptor affinity in the range of morphine and fentanyl. 

Opioid receptor binding Buprenorphine has a mixed agonistic-antagonistic action profile with a high affinity for the p-, k-, and 5-opioid receptors (Huang et al., 2001). An approximately 100-fold lower affinity was observed for the ORL1-receptor. The compound dissociates slowly from the receptor which may explain some peculiarities in its pharmacological actions. 

Opioid receptor binding Butorphanol (Rosow, 1988) is a mixed agonist-antagonist opioid with full agonistic activity at the K-receptor and partial agonistic-antagonistic effect at the p-receptor. The compound has a high p- and k-receptor affinity. 

Opioid receptor binding Codeine has a low affinity at j-, 5-, and K-opioid receptors and the in vivo effects are predominantly induced by morphine, formed by metabolic O-demethylation. 

Opioid receptor binding Dextromoramide is a p-selective opioid with a higher receptor affinity than morphine. 

Opioid receptor binding Dextropropoxyphene has a lower p-opioid receptor binding capacity than morphine. Binding at other opioid receptors is even weaker. 

Opioid receptor binding Dezocine (Chen et al., 1993) is a mixed agonist-antagonist with binding affinity to the p-receptor in the range of morphine. The 5- and K-affinity is 10-100-fold lower (O Brien and Benfield, 1989). 

Opioid receptor binding Diamorphine (Inturrisi et al., 1983) has a 10-100fold lower p-opioid receptor binding affinity than morphine. The relevant opioid properties originate from the high p-receptor affinity of the metabolites 6-acetylmorphine and morphine (Umans and Inturrisi, 1981). 

Opioid receptor binding Dihydrocodeine has a low p-opioid receptor binding and its opioid properties are mostly due to metabolic activation to dihydromorphine. 

Opioid receptor binding Diphenoxylate and its active metabolite difenoxine (Niemegeers et al., 1972) has a high affinity and selectivity for the p-type of opioid receptor. 

Opioid receptor binding Ethylmorphine is an ethyl congener of codeine and has a low opioid receptor affinity (Chen et al., 1991). Like codeine, it is metabolized to the active principle morphine. 

Opioid receptor binding Fentanyl is a p-selective potent opioid with a similar receptor binding affinity to morphine. The higher in vivo potency results from its greater lipophilicity (Subramanian, 2000). 

Opioid receptor binding Hydrocodone has a p-opioid receptor binding that is 10-100 fold higher than codeine. In... 

Opioid receptor binding Levallorphan has a high binding affinity for the p-opioid receptor. 

Opioid receptor binding Levomethadone is the more potent and p-selective levo-enantiomer of racemic methadone (Sim, 1973). It has an opioid receptor affinity in the range of morphine. 

Opioid receptor binding Levomethadyl acetate has a moderate affinity for opioid receptors with selectivity for the p-type. Higher binding affinity is induced by the active metabolites /-alpha-nor-acetylmethadol, nor-methadol and methadol (Walczak et al., 1981 Carroll, 1976). 

Opioid receptor binding Meptazinol (Holmes and Ward, 1985) is a partial p-agonist with a high p-receptor affinity the selective action at a special p1-subtype is controversial (Pasternak et al., 1985). 

Opioid receptor binding Morphine has a high (nanomolar) binding affinity for the opioid receptor. The affinity for the 6- and k- receptor is at least 10-fold lower. 

Opioid receptor binding Nalorphine is a mixed agonist-antagonist with high affinity and low intrinsic action at the p- and K-opioid receptors. 

Opioid receptor binding Naloxone (Simantow and Snyder,... 

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