| Abstract: |
Sodium ions and guanine nucleotides markedly affect the binding to μ and δ sites. Using the guinea pig cerebellum, a tissue whose opioid binding sites are almost exclusively κ, we have examined the sensitivity of [3H](-)-ethylketocyclazocine ([3H]EKC) binding to ions and guanine nucleotides. Unlike μ and δ binding, sodium ions and guanine nucleotides had little effect on the [3H]EKC binding in the guinea pig cerebellum. On the other hand, calcium and manganese at 1 mM lowered [3H]EKC binding in the guinea pig cerebellum by approximately 25%. Binding in rat brain, which was primarily μ and δ, was unaffected. These results point out additional biochemical differences between κ sites and the classic μ and δ binding sites. © 1986. |
| Keywords: |
nonhuman; comparative study; animal cell; animal; cytology; cerebellum; central nervous system; drug receptor binding; brain; rat; rats; drug monitoring; radioisotope; morphine; drug administration; sodium; pharmacokinetics; opiate receptor; guanine nucleotide; cyclazocine; enkephalin, ala(2)-mephe(4)-gly(5)-; electrolytes; drug comparison; guinea pig; enkephalin[2 dextro alanine 4 methylphenylalanine 5 glycine]; guinea pigs; receptors, opioid; guanine nucleotides; priority journal; receptors, opioid, kappa; enkephalin derivative; enkephalin, leucine-2-alanine; support, u.s. gov't, p.h.s.; enkephalins; enkephalin, leucine; enkephalin[2 alanine 5 leucine]; ethylketocyclazocine; preliminary communication; tifluadom; ethylketazocine h 3; κ site
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