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- W2000687022 abstract "1 Rats received an intraperitoneal injection of 1.6 mg kg−1 N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) to achieve an irreversible inactivation of presynaptic release-modulating α2-autoreceptors. Cerebral cortex slices were prepared at different times after the injection (24, 48, 96, 192, 336, 774 h), incubated with [3H]-noradrenaline ([3H]-NA), superfused and stimulated electrically with 4 pulses at 100 Hz (= autoinhibition-free condition). Overflow of radioactivity was used to measure release. Furchgott analysis was used to estimate agonist dissociation constants (KA) and pool size of resynthesized receptors (q). 2 The KA values of the three α2-autoreceptor agonists, bromoxidine (UK-14304), clonidine and noradrenaline (NA) were 187 nm, 72 nm, and 1202 nm, respectively. 3 The release-inhibiting effects of the agonists returned considerably faster than the receptor pool. The calculated half-lives for the recovery of the maximal release-inhibiting effects of bromoxidine, clonidine and NA were 30.7, 63.6 and 20.8 h, respectively, whereas the half-life for the recovery of the receptor pool was 445 h. 4 The data indicate a large receptor reserve at presynaptic α2-autoreceptors for the agonists used and validate the use of EEDQ as a tool for the determination of agonist dissociation constants." @default.
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- W2000687022 date "1993-02-01" @default.
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- W2000687022 title "Central α2-autoreceptors: agonist dissociation constants and recovery after irreversible inactivation" @default.
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- W2000687022 doi "https://doi.org/10.1111/j.1476-5381.1993.tb12811.x" @default.
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