[3H]rauwolscine labels alpha 2-adrenoceptors and 5-HT1A receptors in human cerebral cortex.
[3H]Rauwolscine binds with high affinity to alpha 2-adrenoceptors (Kd = 4.8 +/- 1.3 nM, Bmax = 79 +/- 26 fmol/mg protein, micromolar affinity for 5-HT) as well as to 5-HT1-like receptors (Kd = 13 +/- 2.7 nM, Bmax = 147 +/- 11.4 fmol/mg protein, nanomolar affinity for 5-HT) in human brain cortex membranes. The Ki values of 11 serotonergic compounds for the latter receptors agreed closely with those previously reported for 5-HT1A sites but not with those for 5-HT1B, 5-HT1C and 5-HT1D sites.
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Department of Protein Chemistry, Instituut voor Moleculaire Biologie, Brussels, Belgium.
De Keyser
J
J
De Backer
J P
JP
Vauquelin
G
G
D002540:Cerebral Cortex / Q000032:analysis*; D006801:Humans; D011942:Receptors, Adrenergic, alpha / Q000032:analysis*; D011985:Receptors, Serotonin / Q000032:analysis*; D015016:Yohimbine
D011942:Receptors, Adrenergic, alpha; D011985:Receptors, Serotonin; D015016:Yohimbine