Alterations in alpha adrenergic receptors in human cerebral arteries after subarachnoid hemorrhage.
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)
Tsukahara
T
T
Taniguchi
T
T
Fujiwara
M
M
Handa
H
H
Nishikawa
M
M
D000368:Aged; D002536:Cerebral Arteries / Q000378:metabolism*; D004837:Epinephrine / Q000494:pharmacology; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D009638:Norepinephrine / Q000494:pharmacology; D010646:Phentolamine / Q000494:pharmacology; D011224:Prazosin / Q000037:antagonists & inhibitors / Q000378:metabolism; D011942:Receptors, Adrenergic, alpha / Q000032:analysis / Q000187:drug effects / Q000378:metabolism*; D013345:Subarachnoid Hemorrhage / Q000378:metabolism*; D015016:Yohimbine / Q000037:antagonists & inhibitors / Q000378:metabolism
D011942:Receptors, Adrenergic, alpha; D015016:Yohimbine; D009638:Norepinephrine; D011224:Prazosin; D004837:Epinephrine; D010646:Phentolamine