TY - JOUR
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.
KW - Irreversible receptor inactivation
KW - N-Ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline
KW - [H]5-HT release
KW - [H]NA release
KW - [H]RX-781094 binding
KW - α-Receptors
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U2 - 10.1016/0014-2999(85)90200-6
DO - 10.1016/0014-2999(85)90200-6
M3 - Article
C2 - 2865161
AN - SCOPUS:0022414001
SN - 0014-2999
VL - 116
SP - 175
EP - 178
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
IS - 1-2
ER -