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KMID : 0614020030180010037
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Journal of Pharmaceutical Sciences (C.N.U.)
2003 Volume.18 No. 1 p.37 ~ p.42
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Effect of Leuprolide Acetate, Lorelin, on Rat Brain and Testosterone suppression
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Seo Seong-Kon
Kim Won-Sik
Park Mork-Soon
Park Jin-Kyu
Myung Pyung-Keun
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Abstract
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Leuprolide acetate is a potent luteinizing hormone-releasing hormone analogue [leuprorelin, (des-Glyl0-D-Leu6-Pro-NHEt9)-LHRH acetate]. Lorelin depot, which is composed of leuprolide acetate, was designed for one-month release injectable and biodegradable microsphere of multiple high doses Here we compared the efficacy of microsphere lorelin depot with that of Takeda microsphere (Lucrin Depot). Lorelin (leuprolide 375 mg/kg of body weight) was administered sc to male rats, and the serum was obtained from rat tail vein. Enzyme immunoassay (EIA) for testosterone was carried out to assess the effect of lorelin depot. The rats were sacrificed 42 days after the lorelin β injection. and c-Fos changes of brain were observed by indirect immunofluorescence method. Results showed that the testosterone secretion was inhibited and the expression of c-Fos was also inhibited in the brain.
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KEYWORD
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Leuprolide acetate, Lorelin, testosterone suppression, c-Fos
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