Recovery of α2-adrenoceptor binding and function after irreversible inactivation by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ)

C. H. Adler; E. Meller; M. Goldstein

doi:10.1016/0014-2999(85)90200-6

Recovery of α₂-adrenoceptor binding and function after irreversible inactivation by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ)

C. H. Adler, E. Meller, M. Goldstein

Neurology

Research output: Contribution to journal › Article › peer-review

41 Scopus citations

Abstract

Treatment of rats with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) resulted in a pronounced loss of α₂-adrenoceptor binding ([³H]RX-781094) and a marked reduction in the ability of the α₂-agonist UK-14,304 to inhibit K⁺-stimulated release of both [³H]NA and [³H]5-HT in cerebral cortex. Repopulation of α₂-anderoceptors was monoexponential with a t_{1 2} of 4.1 days; functional recovery was also monoexponential, with t_{1 2} values of 2.4 and 4.6 days for restoration of α₂-mediated inhibition of [³H]NA and [³H]5-HT release, respectively. Other studies suggest the difference in functional recovery rate may reflect the presence of a large receptor reserve for autoreceptors relative to heteroreceptors.

Original language	English (US)
Pages (from-to)	175-178
Number of pages	4
Journal	European Journal of Pharmacology
Volume	116
Issue number	1-2
DOIs	https://doi.org/10.1016/0014-2999(85)90200-6
State	Published - Oct 8 1985

Keywords

Irreversible receptor inactivation
N-Ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline
[H]5-HT release
[H]NA release
[H]RX-781094 binding
α-Receptors

ASJC Scopus subject areas

Pharmacology

Access to Document

10.1016/0014-2999(85)90200-6

Cite this

@article{678ed5f9306349d0858b3b6c703d170e,

title = "Recovery of α2-adrenoceptor binding and function after irreversible inactivation by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ)",

abstract = "Treatment of rats with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) resulted in a pronounced loss of α2-adrenoceptor binding ([3H]RX-781094) and a marked reduction in the ability of the α2-agonist UK-14,304 to inhibit K+-stimulated release of both [3H]NA and [3H]5-HT in cerebral cortex. Repopulation of α2-anderoceptors was monoexponential with a t 1 2 of 4.1 days; functional recovery was also monoexponential, with t 1 2 values of 2.4 and 4.6 days for restoration of α2-mediated inhibition of [3H]NA and [3H]5-HT release, respectively. Other studies suggest the difference in functional recovery rate may reflect the presence of a large receptor reserve for autoreceptors relative to heteroreceptors.",

keywords = "Irreversible receptor inactivation, N-Ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline, [H]5-HT release, [H]NA release, [H]RX-781094 binding, α-Receptors",

author = "Adler, {C. H.} and E. Meller and M. Goldstein",

note = "Funding Information: We thank Ms. Judi Scheer for preparation of the manuscript. Supported by USPHS Grants MH-35976 and MH-14024, NINCDS 06801 and MH 02717. C.H. Adler was supported in part by NIH Training Grant No. 5T32GM07308 from the National Institutes of General Medical Sciences.",

year = "1985",

month = oct,

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doi = "10.1016/0014-2999(85)90200-6",

language = "English (US)",

volume = "116",

pages = "175--178",

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T1 - Recovery of α2-adrenoceptor binding and function after irreversible inactivation by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ)

AU - Adler, C. H.

AU - Meller, E.

AU - Goldstein, M.

N1 - Funding Information: We thank Ms. Judi Scheer for preparation of the manuscript. Supported by USPHS Grants MH-35976 and MH-14024, NINCDS 06801 and MH 02717. C.H. Adler was supported in part by NIH Training Grant No. 5T32GM07308 from the National Institutes of General Medical Sciences.

PY - 1985/10/8

Y1 - 1985/10/8

N2 - Treatment of rats with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) resulted in a pronounced loss of α2-adrenoceptor binding ([3H]RX-781094) and a marked reduction in the ability of the α2-agonist UK-14,304 to inhibit K+-stimulated release of both [3H]NA and [3H]5-HT in cerebral cortex. Repopulation of α2-anderoceptors was monoexponential with a t 1 2 of 4.1 days; functional recovery was also monoexponential, with t 1 2 values of 2.4 and 4.6 days for restoration of α2-mediated inhibition of [3H]NA and [3H]5-HT release, respectively. Other studies suggest the difference in functional recovery rate may reflect the presence of a large receptor reserve for autoreceptors relative to heteroreceptors.

AB - Treatment of rats with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) resulted in a pronounced loss of α2-adrenoceptor binding ([3H]RX-781094) and a marked reduction in the ability of the α2-agonist UK-14,304 to inhibit K+-stimulated release of both [3H]NA and [3H]5-HT in cerebral cortex. Repopulation of α2-anderoceptors was monoexponential with a t 1 2 of 4.1 days; functional recovery was also monoexponential, with t 1 2 values of 2.4 and 4.6 days for restoration of α2-mediated inhibition of [3H]NA and [3H]5-HT release, respectively. Other studies suggest the difference in functional recovery rate may reflect the presence of a large receptor reserve for autoreceptors relative to heteroreceptors.

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KW - α-Receptors

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