Block of calcium channels by enkephalin and somatostatin in neuroblastoma-glioma hybrid NG108-15 cells.
Open accessAbstract
Leucine-enkephalin, methionine-enkephalin, and morphine caused a reversible block of Ca2+ channel currents in neuroblastoma-glioma hybrid cells (NG108-15). The long-lasting (type 2) component of the Ca2+ channel current was blocked by leucine-enkephalin, while the transient (type 1) component was not affected. The enkephalin-induced blocking action was antagonized by naloxone and appears to be mediated by delta-opiate receptors. Two different aspects of the blocking effect were detected, a resting block and a recovery from block during prolonged depolarizing pulses. Recovery from block was more complete, and its time course was more rapid, with depolarization to more positive potentials. The dose dependence of the type 2 channel block at rest indicated a one-to-one binding stoichiometry, with an apparent dissociation constant of 8.8 nM. Somatostatin exerted a similar selective blocking action on the type 2 Ca2+ channel. The time- and voltage-dependent block of type 2 Ca2+ channels may provide a mechanism underlying the enkephalinergic presynaptic inhibition of transmitter release and the somatostatin block of pituitary growth hormone release.
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“All three receptor types are GI protein-coupled receptors that are inhibitory when activated (Burns et al. 1983; Tsunoo et al. 1986; North et al. 1987; for a review, see Knapp et al. 1995).”
- Authors
- Tsunoo, A., Yoshii, M., & Narahashi, T.
- Venue
- Proceedings of the National Academy of Sciences
- Publisher
- National Academy of Sciences
- Published
- 1986-12
- Volume
- 83
- Issue
- 24
- Pages
- 9832-9836
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- PMC
- PMC387236
- OpenAlex
- W2073711199
- Cited by
- 218
- References
- 37
- Citations by year
- 2022: 2 · 2020: 1 · 2019: 2 · 2018: 1 · 2017: 2 · 2016: 2 · 2015: 2 · 2014: 1 · 2013: 2 · 2012: 2
- FWCI
- 6.77
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Proceedings of the National Academy of Sciences (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Heart, Lung, and Blood Institute (HL32577)
- National Institute of Neurological Disorders and Stroke (NS-14144)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion channel regulation and function
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Keywords
- calcium channel blockade, enkephalin, somatostatin, NG108-15 cells, delta opioid receptor, naloxone, leu-enkephalin, met-enkephalin, morphine, recovery from block, depolarization, growth hormone secretion, receptor stoichiometry
- MeSH terms
- Animals, Calcium, Calcium Channel Blockers, Cell Line, Dose-Response Relationship, Drug, Electric Conductivity, Enkephalin, Leucine, Glioma, Ion Channels, Naloxone, Neuroblastoma, Somatostatin, Rats
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