Terguride as a New Anti-Hyperprolactinemic Agent: Characterization in Rats and Dogs in Comparison with Bromocriptine.
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概要
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Terguride, a derivative of the ergot alkaloid, was characterized as a new anti-hyperprolactinemic agent in rats and dogs in comparison with bromocriptine. Terguride was found to bind selectively to the pituitary dopamine D<SUB>2</SUB>-receptors with a high affinity (K<SUB>d</SUB>=0.39 nM). In reserpinized rats, terguride at 0.03 mg/kg, p.o. significantly reduced the serum prolactin (PRL) level. The PRL lowering effect and the effective dose were longer lasting and about 30 times lower than those of bromocriptine, respectively. In rats bearing estrogen-induced pituitary prolactinoma, chronic terguride induced shrinkage of the prolactinoma as well as reduction of the high serum PRL level. In lactating rats, terguride (1.0 mg/kg, s.c.) reduced milk production in the mammary gland, whereas bromocriptine showed no significant effect up to 10 mg/kg, s.c. Terguride (10 mg/kg, p.o.) did not induce any stereotypy and hypermotility in reserpinized rats, while bromocriptine induced both stereotypy and hypermotility significantly at 10 mg/kg, p.o. In dogs, terguride, like bromocriptine, reduced the serum PRL level, but did not affect the serum levels of growth hormone and luteinizing hormone. In dogs, bromocriptine induced both emesis and PRL-lowering at almost the same dose, whereas emesis-inducing doses of terguride were about 100 times higher than the PRL-lowering dose. These results suggest that terguride as a dopamine D<SUB>2</SUB>-agonist is a potent inhibitor of PRL secretion with less neurotropic side effects compared to bromocriptine, and thus a useful drug for the treatment of galactorrhea and hyperprolactinemia including prolactinoma.
- 公益社団法人 日本薬理学会の論文
著者
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Akai Tetsuo
Research Department Institute Of Pharma Research Development And Medical Science Nihon Schering K.k.
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Yamaguchi Motonori
Research Department Institute Of Pharma Research Development And Medical Science Nihon Schering K.k.
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WACHTEL Helmut
Research Laboratories, Schering AG, Berlin
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Yamaguchi Motonori
Research Department, Nihon Schering K.K.
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Akai Tetsuo
Research Department, Nihon Schering K.K.
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Mizokawa Tatsuo
Research Department, Nihon Schering K.K.
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Nakada Yukie
Research Department, Nihon Schering K.K.
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Nakagawa Hidehiko
Research Department, Nihon Schering K.K.
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Hasan Syed
Research Laboratories, Schering AG
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Rettig Klaus-Juergen
Research Laboratories, Schering AG
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