Histamine H1 receptors in human brain labelled with [3H]Doxepin

Shigenobu Kanba, Elliott Richelson

研究成果: ジャーナルへの寄稿学術誌査読

77 被引用数 (Scopus)


Doxepin, a tricyclic antidepressant, is one of the most potent histamine H1 antagonists. Therefore, the binding of [3H]doxepin to human brain membranes was examined. Scatchard analysis revealed two distinct binding sites. The high-affinity binding site with a dissociation constant (KD ± S.E.M.) of 3.1 ± 0.3 × 10-10M was pharmacologically identified as histamine H1 receptors. Dissociation curves at low concentrations of [3H]doxepin were biphasic, suggesting several possibilities about the interaction between [3H]doxepin and histamine H1 receptors. Tetracyclic antidepressants, mianserin and maprotiline, were very potent, with KDs of 3.6 ± 0.7 × 10-10M and 7.9 ± 0.5 × 10-10M, respectively. Mequitazine, a new antihistamine with a weak sedative effect, had a KD of 5.8 ± 0.8 × 10-9, making it ten times as potent as the classic antihistamine diphenyhydramine. The highest binding of [3H]doxepin to histamine H1 receptors was found in cerebral neocortex and the limbic system. The distribution of histamine H1 receptors in human central nervous system did not correlate with the previously reported distributions in rat brain and guinea pig brain determined by [3H]doxepin binding.

ジャーナルBrain Research
出版ステータス出版済み - 6月 18 1984

!!!All Science Journal Classification (ASJC) codes

  • 神経科学一般
  • 分子生物学
  • 臨床神経学
  • 発生生物学


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