Morphine receptors as regulators of adenylate cyclase activity.

Морфиновые рецепторы как регуляторы активности аденилатциклазы
S K Sharma, Marshall W. Nirenberg, Werner A. Klee
1975-02-01

adenylate cyclasemorphine receptorsnaloxonenarcotic addictionneuroblastoma-glioma hybrid cells
Morphine inhibits adenylate cyclase (EC 4.6.1.1) activity of neuroblastoma times glioma hybrid cells. The inhibition is stereospecific and is reversed by the antagonist, naloxone. The relative affinities of narcotics for the opiate receptor agree well with their effectiveness as inhibitors of adenylate cyclase. Morphine-sensitive and -insensitive cell lines were found, and the degree of sensitivity was shown to be dependent upon the abundance of narcotic receptors. Thus, morphine receptors are functionally coupled to adenylate cyclase. A molecular mechanism for narcotic addiction and tolerance is proposed.
1
Cell-line sensitivity to morphine depends on the abundance of narcotic receptors, with both sensitive and insensitive lines identified.
2
Morphine inhibits adenylate cyclase activity in neuroblastoma–glioma hybrid cells.
3
Narcotic affinities for opiate receptors closely match their effectiveness in inhibiting adenylate cyclase.
4
Opiate receptors are functionally coupled to adenylate cyclase, supporting a proposed molecular mechanism for narcotic addiction and tolerance.
5
The inhibition is stereospecific and reversed by the opiate antagonist naloxone.

Morphine receptors functionally coupled to adenylate cyclase in neuroblastoma–glioma hybrid cells

Regulation and inhibition of adenylate cyclase activity by morphine receptors, including stereospecificity, naloxone antagonism, and dependence on receptor abundance

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1975-02-01
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Authors
S K Sharma
Marshall W. Nirenberg
Werner A. Klee
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