Antidiuretic activity and release of Factor VIII by vasopressin analogues
Vasopressin and in particular its structural analogue dDAVP (1-deamino-8-D-arginine vasopressin) can increase plasma concentrations of Factor VIII and tissue plasminogen activator (tPA) in some species of animals and in humans. For this reason dDAVP is used therapeutically in the treatment of bleedi...
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| Veröffentlicht in: | European journal of pharmacology 1993-03, Vol.232 (2), p.223-226 |
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| container_title | European journal of pharmacology |
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| creator | Vilhardt, Hans Barth, Tomislav Melin, Per Aurell, Carl-Johan |
| description | Vasopressin and in particular its structural analogue dDAVP (1-deamino-8-D-arginine vasopressin) can increase plasma concentrations of Factor VIII and tissue plasminogen activator (tPA) in some species of animals and in humans. For this reason dDAVP is used therapeutically in the treatment of bleeding episodes in patients suffering from haemophilia A and Von Willebrand's disease. However, the high antidiuretic activity of dDAVP constitutes and unwanted effect in this context. In the present study, a large number of analogues of vasopressin were designed, synthesized and tested in monkeys with the aim of producing compounds in which the Factor VIII-releasing activity was selectively isolated from the vasopressor and antidiuretic actions of the peptide. The results indicate that it is possible to separate these biological activities; however, none of the analogues tested so far possessed Factor VIII potencies comparable to that of dDAVP. |
| doi_str_mv | 10.1016/0014-2999(93)90777-F |
| format | Article |
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For this reason dDAVP is used therapeutically in the treatment of bleeding episodes in patients suffering from haemophilia A and Von Willebrand's disease. However, the high antidiuretic activity of dDAVP constitutes and unwanted effect in this context. In the present study, a large number of analogues of vasopressin were designed, synthesized and tested in monkeys with the aim of producing compounds in which the Factor VIII-releasing activity was selectively isolated from the vasopressor and antidiuretic actions of the peptide. 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For this reason dDAVP is used therapeutically in the treatment of bleeding episodes in patients suffering from haemophilia A and Von Willebrand's disease. However, the high antidiuretic activity of dDAVP constitutes and unwanted effect in this context. In the present study, a large number of analogues of vasopressin were designed, synthesized and tested in monkeys with the aim of producing compounds in which the Factor VIII-releasing activity was selectively isolated from the vasopressor and antidiuretic actions of the peptide. The results indicate that it is possible to separate these biological activities; however, none of the analogues tested so far possessed Factor VIII potencies comparable to that of dDAVP.</description><subject>Amino Acid Sequence</subject><subject>Animals</subject><subject>Antidiuretic activity</subject><subject>Biological and medical sciences</subject><subject>Blood Pressure - drug effects</subject><subject>Callithrix</subject><subject>Diuresis - drug effects</subject><subject>Factor VIII</subject><subject>Factor VIII - metabolism</subject><subject>Female</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Molecular Sequence Data</subject><subject>Monkey</subject><subject>Peptides - chemical synthesis</subject><subject>Peptides - pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Urinary system</subject><subject>Vasopressin analogues</subject><subject>Vasopressins - pharmacology</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1993</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kEFLwzAUx4MoOqffQKEHET1Uk6ZtmoswhtPCwIt6DenLq0S6dibtYN_ezJUdPb3D__d_7_Ej5IrRB0ZZ_kgpS-NESnkn-b2kQoh4cUQmrBAypoIlx2RyQM7IuffflNJMJtkpOS3SXBSZnJBy1vbW2MFhbyHS0NuN7beRbk3ksEHtMerqaBGCzkWfZVlG1TbaaN-tHXpv20Dqpvsa0F-Qk1o3Hi_HOSUfi-f3-Wu8fHsp57NlDLzI-7hiDDmHVGYVNyZJdZUUoI3RYHLBclobzCtMgFVVDcIIgVxCzTPgTDBdCz4lt_u9a9f9hLu9WlkP2DS6xW7wSmS5TKnIApjuQXCd9w5rtXZ2pd1WMap2BtVOj9rpUZKrP4NqEWrX4_6hWqE5lEZlIb8Zc-1BN7XTLVh_wNKsCFgRsKc9hsHFxqJTHiy2gMY6hF6Zzv7_xy9W8I3r</recordid><startdate>19930302</startdate><enddate>19930302</enddate><creator>Vilhardt, Hans</creator><creator>Barth, Tomislav</creator><creator>Melin, Per</creator><creator>Aurell, Carl-Johan</creator><general>Elsevier B.V</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19930302</creationdate><title>Antidiuretic activity and release of Factor VIII by vasopressin analogues</title><author>Vilhardt, Hans ; Barth, Tomislav ; Melin, Per ; Aurell, Carl-Johan</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c386t-b11e33c495b3dd24ab28caddacd67160fde6be2c1bbfc7d77e39cf35c3171af73</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1993</creationdate><topic>Amino Acid Sequence</topic><topic>Animals</topic><topic>Antidiuretic activity</topic><topic>Biological and medical sciences</topic><topic>Blood Pressure - drug effects</topic><topic>Callithrix</topic><topic>Diuresis - drug effects</topic><topic>Factor VIII</topic><topic>Factor VIII - metabolism</topic><topic>Female</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Molecular Sequence Data</topic><topic>Monkey</topic><topic>Peptides - chemical synthesis</topic><topic>Peptides - pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Urinary system</topic><topic>Vasopressin analogues</topic><topic>Vasopressins - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Vilhardt, Hans</creatorcontrib><creatorcontrib>Barth, Tomislav</creatorcontrib><creatorcontrib>Melin, Per</creatorcontrib><creatorcontrib>Aurell, Carl-Johan</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Vilhardt, Hans</au><au>Barth, Tomislav</au><au>Melin, Per</au><au>Aurell, Carl-Johan</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Antidiuretic activity and release of Factor VIII by vasopressin analogues</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1993-03-02</date><risdate>1993</risdate><volume>232</volume><issue>2</issue><spage>223</spage><epage>226</epage><pages>223-226</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>Vasopressin and in particular its structural analogue dDAVP (1-deamino-8-D-arginine vasopressin) can increase plasma concentrations of Factor VIII and tissue plasminogen activator (tPA) in some species of animals and in humans. For this reason dDAVP is used therapeutically in the treatment of bleeding episodes in patients suffering from haemophilia A and Von Willebrand's disease. However, the high antidiuretic activity of dDAVP constitutes and unwanted effect in this context. In the present study, a large number of analogues of vasopressin were designed, synthesized and tested in monkeys with the aim of producing compounds in which the Factor VIII-releasing activity was selectively isolated from the vasopressor and antidiuretic actions of the peptide. The results indicate that it is possible to separate these biological activities; however, none of the analogues tested so far possessed Factor VIII potencies comparable to that of dDAVP.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>8467859</pmid><doi>10.1016/0014-2999(93)90777-F</doi><tpages>4</tpages></addata></record> |
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| ispartof | European journal of pharmacology, 1993-03, Vol.232 (2), p.223-226 |
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| subjects | Amino Acid Sequence Animals Antidiuretic activity Biological and medical sciences Blood Pressure - drug effects Callithrix Diuresis - drug effects Factor VIII Factor VIII - metabolism Female Male Medical sciences Molecular Sequence Data Monkey Peptides - chemical synthesis Peptides - pharmacology Pharmacology. Drug treatments Urinary system Vasopressin analogues Vasopressins - pharmacology |
| title | Antidiuretic activity and release of Factor VIII by vasopressin analogues |
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