Characteristics and metabolism of alpha 1 adrenergic receptors in a nonfusing muscle cell line.
作者： J.P. Mauger , F. Sladeczek , J. Bockaert
DOI: 10.1016/S0021-9258(19)68279-7
关键词:
摘要: The BC3H1 nonfusing muscle cell line possesses binding sites for [3H]prazosin. These are typically alpha 1 adrenergic receptors as shown by their greater affinity (3700-fold) prazosin than yohimbine. Both kinetic and equilibrium analyses indicated that [3H]prazosin interacted with only one category of independent the following characteristics. KD = 0.13 +/- 0.01 nM. Bmax 97 5 fmol/mg protein corresponding to 25,000 sites/cell (n 17). Biosynthesis receptor was investigated at confluency (when number cells total content were constant). Phenoxybenzamine (10(-9) M) irreversibly blocked 50% in intact cells. More 95% blockade obtained 10(-7) M phenoxybenzamine. After this blockade, new reappeared monoexponential kinetics. corresponded synthesized since appearance cycloheximide (1 micrograms/ml). action reversible. If makes simple probable hypotheses production is constant degradation a process, analysis kinetics reappearance allows determination rate (k 0.03 h-1) (r 3.2 fmol/mg/h) synthesis about 760 receptors/cell/h. half-life 23 h.
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