TRANSDERMAL IONTOPHORESIS OF GONADOTROPIN-RELEASING HORMONE (LHRH) AND 2 ANALOGS
TRANSDERMAL IONTOPHORESIS OF GONADOTROPIN-RELEASING HORMONE (LHRH) AND 2 ANALOGS
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DOI：
10.1002/jps.2600790607
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发表时间：
1990-06-01
影响因子：
3.8
通讯作者：
RIVIER, J
中科院分区：
文献类型：
--
作者：
MILLER, LL;KOLASKIE, CJ;RIVIER, J
Gonadotropin releasing hormone (GnRH), as well as an antagonist [Ac-D2Nal1, D4ClPhe2, D3Pal3, NicLys5, DNicLys6, ILys8, DAla10] GnRH .cntdot. HOAc (1) and a superagonist [DTrp6, Pro9-NHEt]GnRH (2), have been electrochemically driven across exercised hairless mouse skin. Determined by HPLC analyis, the delviery rate from aqueous solution into isotonic saline at 0.5 mA cm-2 was as high as 19 nM cm-2 h-1 for 2. Because of its insolubility in water, analogue 1 could only be delivered from an acidic donor solution. Analogue 2 was also delivered in pulsatile fashion using current on/off cycles. For all three peptides, passive transport was negligible and stability is evident when in contact with the stratum corneum. Slow metabolism occurs when GnRH contacts the dermal side of hairless mouse skin.
