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Molecular Pharmacology

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Research ArticleArticle

A Typical Y1 Receptor Regulates Feeding Behaviors: Effects of a Potent and Selective Y1 Antagonist, J-115814

Akio Kanatani, Mikiko Hata, Satoshi Mashiko, Akane Ishihara, Osamu Okamoto, Yuji Haga, Tomoyuki Ohe, Tetsuya Kanno, Naomi Murai, Yasuyuki Ishii, Takahiro Fukuroda, Takehiro Fukami and Masaki Ihara
Molecular Pharmacology March 2001, 59 (3) 501-505; DOI: https://doi.org/10.1124/mol.59.3.501
Akio Kanatani
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan
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Mikiko Hata
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan
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Satoshi Mashiko
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan
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Akane Ishihara
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan
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Osamu Okamoto
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan
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Yuji Haga
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan
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Tomoyuki Ohe
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan
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Tetsuya Kanno
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan
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Naomi Murai
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan
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Yasuyuki Ishii
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan
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Takahiro Fukuroda
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan
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Takehiro Fukami
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan
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Masaki Ihara
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Tsukuba, Japan
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Abstract

Neuropeptide Y (NPY) is a potent feeding stimulant. The orexigenic effect of NPY might be caused in part by the action of Y1 receptors. However, the existence of multiple NPY receptors including a possible novel feeding receptor has made it difficult to determine the relative importance of the Y1 receptor in feeding regulation. Herein we certified that the Y1 receptor is a major feeding receptor of NPY by using the potent and selective Y1 antagonist (−)-2-[1-(3-chloro-5-isopropyloxycarbonylaminophenyl)ethylamino]-6-[2-(5-ethyl-4-methyl-1,3-thiazol-2-yl)ethyl]-4-morpholinopyridine (J-115814) and Y1 receptor-deficient (Y1−/−) mice. J-115814 displaced125I-peptide YY binding to cell membranes expressing cloned human, rat, and murine Y1 receptors withK i values of 1.4, 1.8, and 1.9 nM, respectively, and inhibited NPY (10 nM)-induced increases in intracellular calcium levels via human Y1 receptors (IC50 = 6.8 nM). In contrast, J-115814 showed low affinities for human Y2 (K i > 10 μM), Y4 (K i = 640 nM) and Y5 receptors (K i = 6000 nM). Intracerebroventricular (ICV) (10–100 μg) and intravenous (IV) (0.3–30 mg/kg) administration of J-115814 significantly and dose-dependently suppressed feeding induced by ICV NPY (5 μg) in satiated Sprague-Dawley rats. Intraperitoneal (IP) administration of J-115814 (3–30 mg/kg) significantly attenuated spontaneous feeding in db/db and C57BL6 mice. Feeding induced by ICV NPY (5 μg) was unaffected by IP-injected J-115814 (30 mg/kg) in Y1−/− mice and was suppressed in wild-type and Y5−/− mice. These findings clearly suggest that J-115814 inhibits feeding behaviors through the inhibition of the typical Y1 receptor. We conclude that the Y1 receptor plays a key role in regulating food intake.

Footnotes

    • Received August 7, 2000.
    • Accepted November 9, 2000.
  • Send reprint requests to: Akio Kanatani, Ph.D., Tsukuba Research Institute, Banyu Pharmaceutical Co. Ltd., Okubo 3, Tsukuba 300-2611, Japan. E-mail: kantniak{at}banyu.co.jp

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Molecular Pharmacology: 59 (3)
Molecular Pharmacology
Vol. 59, Issue 3
1 Mar 2001
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Research ArticleArticle

A Typical Y1 Receptor Regulates Feeding Behaviors: Effects of a Potent and Selective Y1 Antagonist, J-115814

Akio Kanatani, Mikiko Hata, Satoshi Mashiko, Akane Ishihara, Osamu Okamoto, Yuji Haga, Tomoyuki Ohe, Tetsuya Kanno, Naomi Murai, Yasuyuki Ishii, Takahiro Fukuroda, Takehiro Fukami and Masaki Ihara
Molecular Pharmacology March 1, 2001, 59 (3) 501-505; DOI: https://doi.org/10.1124/mol.59.3.501

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Research ArticleArticle

A Typical Y1 Receptor Regulates Feeding Behaviors: Effects of a Potent and Selective Y1 Antagonist, J-115814

Akio Kanatani, Mikiko Hata, Satoshi Mashiko, Akane Ishihara, Osamu Okamoto, Yuji Haga, Tomoyuki Ohe, Tetsuya Kanno, Naomi Murai, Yasuyuki Ishii, Takahiro Fukuroda, Takehiro Fukami and Masaki Ihara
Molecular Pharmacology March 1, 2001, 59 (3) 501-505; DOI: https://doi.org/10.1124/mol.59.3.501
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