Protection with phencyclidine against inactivation of 5-HT2 receptors by sulfhydryl-modifying reagents

Toshitaka Nabeshima, Ishikawa Kazuhiro, Yamaguchi Kazumasa, Furukawa Hiroshi, Kameyama Tsutomu

研究成果: Article

15 引用 (Scopus)

抄録

We investigated whether phencyclidine (PCP)-induced head-twitch was antagonized in rats by ritanserin, a selective serotonin2 (5-HT2) receptor antagonist, to confirm the involvement of 5-HT neurons in PCP action and to discover whether PCP could protect the binding sites of [3H]PCP and [3H]ketanserin from the inhibitory effect of protein-modifying reagents which affect sulfhydryl groups. PCP (7.5,10 and 12.5 mg/kg, i.p.)-induced head-twitch was completely antagonized by ritanserin (1 mg/kg, s.c.). Scatchard plots of specific [3H]PCP and [3H]ketanserin binding showed that sulfhydryl-modifying reagent, N-ethylmaleimide (NEM, 100 μM) caused a significant decrease in Bmax without changing Kd. PCP (10 μM) and ritanserin (1 μM) protected [3H]PCP and [3H]ketanserin binding sites from the decrease in the number induced by NEM (100 μM). 5-HT protected [3H]5-HT binding sites from inactivation by NEM, but PCP and ritanserin did not show any effect. On the basis of the present findings, it is concluded that PCP can interact with 5-HT2 receptors directly or allosterically, and 5-HT2 receptors may locate at PCP binding sites in membranes.

元の言語English
ページ(範囲)3277-3283
ページ数7
ジャーナルBiochemical Pharmacology
37
発行部数17
DOI
出版物ステータスPublished - 01-09-1988
外部発表Yes

Fingerprint

Ritanserin
Phencyclidine
Sulfhydryl Reagents
Ketanserin
Binding Sites
Serotonin
Head
Serotonin 5-HT2 Receptor Antagonists
Ethylmaleimide
Neurons
Rats
Membranes
Proteins

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Pharmacology

これを引用

Nabeshima, Toshitaka ; Kazuhiro, Ishikawa ; Kazumasa, Yamaguchi ; Hiroshi, Furukawa ; Tsutomu, Kameyama. / Protection with phencyclidine against inactivation of 5-HT2 receptors by sulfhydryl-modifying reagents. :: Biochemical Pharmacology. 1988 ; 巻 37, 番号 17. pp. 3277-3283.
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abstract = "We investigated whether phencyclidine (PCP)-induced head-twitch was antagonized in rats by ritanserin, a selective serotonin2 (5-HT2) receptor antagonist, to confirm the involvement of 5-HT neurons in PCP action and to discover whether PCP could protect the binding sites of [3H]PCP and [3H]ketanserin from the inhibitory effect of protein-modifying reagents which affect sulfhydryl groups. PCP (7.5,10 and 12.5 mg/kg, i.p.)-induced head-twitch was completely antagonized by ritanserin (1 mg/kg, s.c.). Scatchard plots of specific [3H]PCP and [3H]ketanserin binding showed that sulfhydryl-modifying reagent, N-ethylmaleimide (NEM, 100 μM) caused a significant decrease in Bmax without changing Kd. PCP (10 μM) and ritanserin (1 μM) protected [3H]PCP and [3H]ketanserin binding sites from the decrease in the number induced by NEM (100 μM). 5-HT protected [3H]5-HT binding sites from inactivation by NEM, but PCP and ritanserin did not show any effect. On the basis of the present findings, it is concluded that PCP can interact with 5-HT2 receptors directly or allosterically, and 5-HT2 receptors may locate at PCP binding sites in membranes.",
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Protection with phencyclidine against inactivation of 5-HT2 receptors by sulfhydryl-modifying reagents. / Nabeshima, Toshitaka; Kazuhiro, Ishikawa; Kazumasa, Yamaguchi; Hiroshi, Furukawa; Tsutomu, Kameyama.

:: Biochemical Pharmacology, 巻 37, 番号 17, 01.09.1988, p. 3277-3283.

研究成果: Article

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T1 - Protection with phencyclidine against inactivation of 5-HT2 receptors by sulfhydryl-modifying reagents

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AU - Kazuhiro, Ishikawa

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AU - Hiroshi, Furukawa

AU - Tsutomu, Kameyama

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N2 - We investigated whether phencyclidine (PCP)-induced head-twitch was antagonized in rats by ritanserin, a selective serotonin2 (5-HT2) receptor antagonist, to confirm the involvement of 5-HT neurons in PCP action and to discover whether PCP could protect the binding sites of [3H]PCP and [3H]ketanserin from the inhibitory effect of protein-modifying reagents which affect sulfhydryl groups. PCP (7.5,10 and 12.5 mg/kg, i.p.)-induced head-twitch was completely antagonized by ritanserin (1 mg/kg, s.c.). Scatchard plots of specific [3H]PCP and [3H]ketanserin binding showed that sulfhydryl-modifying reagent, N-ethylmaleimide (NEM, 100 μM) caused a significant decrease in Bmax without changing Kd. PCP (10 μM) and ritanserin (1 μM) protected [3H]PCP and [3H]ketanserin binding sites from the decrease in the number induced by NEM (100 μM). 5-HT protected [3H]5-HT binding sites from inactivation by NEM, but PCP and ritanserin did not show any effect. On the basis of the present findings, it is concluded that PCP can interact with 5-HT2 receptors directly or allosterically, and 5-HT2 receptors may locate at PCP binding sites in membranes.

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