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公开(公告)号：US4908352A
公开(公告)日：1990-03-13
申请号：US101580
申请日：1987-09-28
IPC分类号： A61K38/00 , C07K14/575
CPC分类号： C07K14/57509 , A61K38/00
摘要： Maggy UI (Urotensin I) or flathead sole urotensin, obtained from Hippoglossides Elassodon has the formula: H-Ser-Glu-Glu-Pro-Pro-Met-Ser-Ile-Asp-Leu-Thr-Phe-His-Met-Leu-Arg-Asn-Met-Ile-His-Arg-Ala-Lys-Met-Glu-Gly-Glu-Arg-Glu-Gln-Ala-Leu-Ile-Asn-Arg-Asn-Leu-Leu-Asp-Glu-Val-NH.sub.2. Analogs have been synthesized that are at least as potent as Maggy UI, and Maggy UI or such an analog or a biologically active fragment of either or pharmaceutically acceptable salts of any of the foregoing, dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals to achieve a substantial elevation of ACTH, .beta.-endorphin, .alpha.-lipotropin and corticosterone levels and/or an increase in intestinal blood flow and/or a lowering of systemic blood pressure and/or a changing of regional blood distributio over an extended period of time. In the analogs, one or more of the first three N-terminal residues is deleted and is optionally substituted by a peptide fragment up to 5 amino acids long, and/or an acylating agent containing up to 7 carbon atoms is optionally added at the N-terminus.
摘要翻译： 由Hippoglossides Elassodon得到的Maggy UI（Urotensin I）或扁平头状的单独的urotensin具有下式：H-Ser-Glu-Glu-Pro-Pro-Met-Ser-Ile-Asp-Leu-Thr-Phe-His-Met-Leu -Arg-Asn-Met-Ile-His-Arg-Ala-Lys-Met-Glu-Gly-Glu-Arg-Glu-Gln-Ala-Leu-Ile-Asn-Ar g-Asn-Leu-Leu-Asp- Glu-Val-NH2。 已经合成类似物至少与Maggy UI一样有效，Maggy UI或分散在药学上可接受的液体或固体载体中的前述任何一种或其药学上可接受的盐的类似物或生物活性片段可以是 施用于哺乳动物以实现ACTH，β-内啡肽，α-促肌动蛋白和皮质酮水平的显着升高和/或肠血流量的增加和/或全身血压的降低和/或区域血液分布的变化 延长一段时间 在类似物中，前三个N-末端残基中的一个或多个被缺失，并且任选地被长达5个氨基酸的肽片段取代，和/或任选地在N个加入含有至多7个碳原子的酰化剂 -terminus。
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公开(公告)号：US4528189A
公开(公告)日：1985-07-09
申请号：US463397
申请日：1983-02-03
IPC分类号： A61K38/00 , C07K14/575 , C07C103/52 , A61K37/02
CPC分类号： C07K14/57509 , A61K38/00
摘要： UI (Urotensin I) or white sucker urotensin, obtained from Catostomus commersoni, has the formula: H-Asn-Asp-Asp-Pro-Pro-Ile-Ser-Ile-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Asn-Met-Ile-Glu-Met-Ala-Arg-Ile-Glu-Asn-Glu-Arg-Glu-Gln-Ala-Gly-Leu-Asn-Arg-Lys-Tyr-Leu-Asp-Glu-Val-NH.sub.2. Analogs have been synthesized that are at least as potent as UI, and UI or such an analog or a fragment of either or a pharmaceutically acceptable salts of any of the foregoing, dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals to achieve a substantial elevation of ACTH, .beta.-endorphin, .beta.-lipotropin and corticosterone levels and/or an increase in intestinal blood flow and/or a lowering of systemic blood pressure and/or a changing of regional blood distribution over an extended period of time. In the analogs, one or more of the first three N-terminal residues is deleted and substituted by a peptide fragment up to 5 amino acids long and/or an acylating agent containing up to 7 carbon atoms is added at the N-terminal.
摘要翻译： 由Catostomus commersoni获得的UI（促进素I）或白色吸盘泌尿激素具有下式：H-Asn-Asp-Asp-Pro-Pro-Ile-Ser-Ile-Asp-Leu-Thr-Phe-His-Leu-Leu -Arg-Asn-Met-Ile-Glu-Met-Ala-Arg-Ile-Glu-Asn-Glu-Arg-Glu-Gln-Ala-Gly-Leu-Asn-Ar g-Lys-Tyr-Leu-Asp- Glu-Val-NH2。 已经合成至少与UI一样有效的类似物，并且分散在药学上可接受的液体或固体载体中的UI或上述任何一种或其药学上可接受的盐的类似物或片段可以施用于哺乳动物 实现ACTH，β-内啡肽，β-促性腺激素和皮质酮水平的显着升高和/或肠道血流量的增加和/或全身血压的降低和/或在长时间内区域血液分布的变化 时间。 在类似物中，前三个N-末端残基中的一个或多个被缺失并被长达5个氨基酸的肽片段取代，和/或在N-末端添加含有至多7个碳原子的酰化剂。
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公开(公告)号：US4533654A
公开(公告)日：1985-08-06
申请号：US600554
申请日：1984-04-04
IPC分类号： A61K38/00 , C07K14/575 , A61K37/00 , C07C103/52
CPC分类号： C07K14/57509 , A61K38/00 , Y10S530/857
摘要： UI (Urotensin I) or carp urotensin, obtained from Cyprinus carpio, has the formula: H-Asn-Asp-Asp-Pro-Pro-Ile-Ser-Ile-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Asn-Met-Ile-Glu-Met-Ala-Arg-Asn-Glu-Asn-Gln-Arg-Glu-Gln-Ala-Gly-Leu-Asn-Arg-Lys-Tyr-Leu-Asp-Glu-Val-NH.sub.2. UI or a biologically active fragment thereof or a pharmaceutically acceptable salt of either, dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals to achieve a substantial elevation of ACTH, .beta.-endorphin, .beta.-lipotropin and corticosterone levels and/or a lowering of systemic blood pressure over an extended period of time.
摘要翻译： PCT No.PCT / US82 / 01349 Sec。 1984日期1984年4月3日 102（e）日期1984年4月6日PCT提交1982年9月29日PCT公布。 出版物WO84 / 01378 日本2004年4月12日。从Cyprinus carpio获得的UI（促进素I）或鲤鱼尿素保护素具有下式：H-Asn-Asp-Asp-Pro-Pro-Ile-Ser-Ile-Asp-Leu-Thr-Phe -His-Leu-Leu-Arg-Asn-Met-Ile-Glu-Met-Ala-Arg-Asn-Glu-Asn-Gln-Arg-Glu-Gln-Ala-Gly-Leu-Asn-Ar g-Lys- Tyr-Leu-Asp-Glu-Val-NH2。 可以向哺乳动物施用分散在药学上可接受的液体或固体载体中的UI或其生物活性片段或其药学上可接受的盐，以实现ACTH，β-内啡肽，β-促肌酸激素和皮质酮水平的显着升高和/ 或在长时间内降低全身血压。
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