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The nature of alpha adrenergic receptors in human cerebral arteries was characterized and alteration of these receptors after subarachnoid hemorrhage (SAH) was examined using a radioligand binding assay. The specific 3H-prazosin binding to human cerebral arteries was saturable and of high affinity (KD = 4.1 nM) with a Bmax of 92 fmol/mg protein. Specific 3H-yohimbine binding to these tissues was also saturable and of high affinity (KD = 23 nM) with a Bmax 250 fmol/mg protein. IC50 values of adrenergic agents for 3H-prazosin binding were as follows: prazosin, 1.2 X 10(-10) M; phentolamine, 1.3 x 10(-6) M; yohimbine, 1.2 x 10(-5); norepinephrine, 4.9 x 10(-4) M; epinephrine greater than 1 x 10(-3) M. IC50 values of adrenergic agents for 3H-yohimbine binding were as follows: phentolamine, 1.7 x 10(-7) M; yohimbine, 4.2 x 10(-7) M; prazosin, 1.9 x 10(-5) M; epinephrine, 4.4 x 10(-5) M; norepinephrine, 7.9 x 10(-4) M. KD and Bmax of 3H-prazosin and 3H-yohimbine binding after SAH were compared with findings in the non-SAH group. KD and Bmax of 3H-prazosin binding of SAH group were 6 +/- 3 nM and 90 +/- 10 fmol/mg protein, respectively (N = 3). KD and Bmax of 3H-yohimbine binding of SAH group were 42 +/- 6 nM and 460 +/- 30 fmol/mg protein, respectively (N = 5). On the other hand, KD and Bmax of 3H-prazosin binding in the non-SAH group were 4 +/- 1 nM and 90 +/- 20 fmol/mg protein, respectively (N = 5), KD and Bmax of 3H-yohimbine binding of non-SAH group were 20 +/- 5 nM and 260 +/- 30 fmol/mg protein, respectively (N = 6).(ABSTRACT TRUNCATED AT 250 WORDS)

Alterations in alpha adrenergic receptors in human cerebral arteries after subarachnoid hemorrhage.