Receptor binding of fluorinated histidine analogs of thyrotropin-releasing hormone in various regions of the rat brain
Binding properties of [4(5)-fluoro-imidazole-His 2]-TRH (4(5)-F-TRH), [2-trifluoromethyl-imidazole-His 2]-TRH (2-CF 3-TRH) and [4(5)-trifluoromethyl-imidazole-His 2]-TRH (4(5)-CF 3-TRH), three novel TRH analogs, have been evaluated in rat pituitary, hypothalamus, brainstem and cortex tissue. 4(5)-F-...
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| Veröffentlicht in: | European journal of pharmacology 1989-05, Vol.164 (1), p.77-83 |
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| container_title | European journal of pharmacology |
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| creator | Vonhof, Stefan Paakkari, Ilari Feuerstein, Giora Cohen, Louis A. Labroo, Virender M. |
| description | Binding properties of [4(5)-fluoro-imidazole-His
2]-TRH (4(5)-F-TRH), [2-trifluoromethyl-imidazole-His
2]-TRH (2-CF
3-TRH) and [4(5)-trifluoromethyl-imidazole-His
2]-TRH (4(5)-CF
3-TRH), three novel TRH analogs, have been evaluated in rat pituitary, hypothalamus, brainstem and cortex tissue. 4(5)-F-TRH, previously shown to elicit arterial pressor responses and prolactin release similar to those of TRH, binds to TRH receptors with low, micromolar affinity (K
i = 7.5−13.5
μM) 2-CF
3-TRH, an analog of less cardiovascular but increased prolactin-releasing activity, shows K
i values of 3.3–4.9 μM. 4(5)-CF
3-TRH, which shows comparable biological activity to 2-CF
3-TRH, demonstrates a binding affinity which is virtually nonspecific (K
i = 0.39−1.01 mM). It is therefore concluded that the biological effects of these analogs are mediated either through low affinity TRH binding sites not recognized by [
3H][3Me-His
2]-TRH or through mechanisms not involving TRH receptors as such. |
| doi_str_mv | 10.1016/0014-2999(89)90233-1 |
| format | Article |
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2]-TRH (4(5)-F-TRH), [2-trifluoromethyl-imidazole-His
2]-TRH (2-CF
3-TRH) and [4(5)-trifluoromethyl-imidazole-His
2]-TRH (4(5)-CF
3-TRH), three novel TRH analogs, have been evaluated in rat pituitary, hypothalamus, brainstem and cortex tissue. 4(5)-F-TRH, previously shown to elicit arterial pressor responses and prolactin release similar to those of TRH, binds to TRH receptors with low, micromolar affinity (K
i = 7.5−13.5
μM) 2-CF
3-TRH, an analog of less cardiovascular but increased prolactin-releasing activity, shows K
i values of 3.3–4.9 μM. 4(5)-CF
3-TRH, which shows comparable biological activity to 2-CF
3-TRH, demonstrates a binding affinity which is virtually nonspecific (K
i = 0.39−1.01 mM). It is therefore concluded that the biological effects of these analogs are mediated either through low affinity TRH binding sites not recognized by [
3H][3Me-His
2]-TRH or through mechanisms not involving TRH receptors as such.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(89)90233-1</identifier><identifier>PMID: 2753081</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Affinity, Receptors ; Animals ; Binding, Competitive - drug effects ; Biological and medical sciences ; Brain - drug effects ; Brain - metabolism ; Histidine - analogs & derivatives ; Histidine - pharmacology ; Hormones. Endocrine system ; Hypothalamus - drug effects ; Hypothalamus - metabolism ; Male ; Medical sciences ; Pharmacology. Drug treatments ; Rats ; Rats, Inbred Strains ; Receptors, Thyroid Hormone - drug effects ; Receptors, Thyroid Hormone - metabolism ; Time Factors ; TRH analog (fluorinated)</subject><ispartof>European journal of pharmacology, 1989-05, Vol.164 (1), p.77-83</ispartof><rights>1989</rights><rights>1989 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c386t-c23f4a40740303a32790e7d07b293ae6c6b34c679967aed9dac0fa4ad36608863</citedby><cites>FETCH-LOGICAL-c386t-c23f4a40740303a32790e7d07b293ae6c6b34c679967aed9dac0fa4ad36608863</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0014-2999(89)90233-1$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=7357216$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2753081$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Vonhof, Stefan</creatorcontrib><creatorcontrib>Paakkari, Ilari</creatorcontrib><creatorcontrib>Feuerstein, Giora</creatorcontrib><creatorcontrib>Cohen, Louis A.</creatorcontrib><creatorcontrib>Labroo, Virender M.</creatorcontrib><title>Receptor binding of fluorinated histidine analogs of thyrotropin-releasing hormone in various regions of the rat brain</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>Binding properties of [4(5)-fluoro-imidazole-His
2]-TRH (4(5)-F-TRH), [2-trifluoromethyl-imidazole-His
2]-TRH (2-CF
3-TRH) and [4(5)-trifluoromethyl-imidazole-His
2]-TRH (4(5)-CF
3-TRH), three novel TRH analogs, have been evaluated in rat pituitary, hypothalamus, brainstem and cortex tissue. 4(5)-F-TRH, previously shown to elicit arterial pressor responses and prolactin release similar to those of TRH, binds to TRH receptors with low, micromolar affinity (K
i = 7.5−13.5
μM) 2-CF
3-TRH, an analog of less cardiovascular but increased prolactin-releasing activity, shows K
i values of 3.3–4.9 μM. 4(5)-CF
3-TRH, which shows comparable biological activity to 2-CF
3-TRH, demonstrates a binding affinity which is virtually nonspecific (K
i = 0.39−1.01 mM). It is therefore concluded that the biological effects of these analogs are mediated either through low affinity TRH binding sites not recognized by [
3H][3Me-His
2]-TRH or through mechanisms not involving TRH receptors as such.</description><subject>Affinity, Receptors</subject><subject>Animals</subject><subject>Binding, Competitive - drug effects</subject><subject>Biological and medical sciences</subject><subject>Brain - drug effects</subject><subject>Brain - metabolism</subject><subject>Histidine - analogs & derivatives</subject><subject>Histidine - pharmacology</subject><subject>Hormones. Endocrine system</subject><subject>Hypothalamus - drug effects</subject><subject>Hypothalamus - metabolism</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Receptors, Thyroid Hormone - drug effects</subject><subject>Receptors, Thyroid Hormone - metabolism</subject><subject>Time Factors</subject><subject>TRH analog (fluorinated)</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1989</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1r3DAURUVpSCdJ_0ELXpSSLtw8SR7J2gRK6EcgUCjtWjxLzzMqHmkqeQby72t3zCy7eot77uNyGHvD4SMHru4AeFMLY8xtaz4YEFLW_AVb8VabGjQXL9nqjLxiV6X8BoC1EetLdin0WkLLV-z4gxztx5SrLkQf4qZKfdUPh5RDxJF8tQ1lDFNAFUYc0qbMwLh9zmnMaR9inWkgLHNzm_IuTWCI1RFzSIdSZdqEFJcOVRnHqssY4g276HEo9Hq51-zXl88_H77VT9-_Pj58eqqdbNVYOyH7BhvQDUiQKIU2QNqD7oSRSMqpTjZOaWOURvLGo4MeG_RSKWhbJa_Z-9PffU5_DlRGuwvF0TBgpGmf1YZDM7mawOYEupxKydTbfQ47zM-Wg51129mlnV3a1th_ui2fam-X_4duR_5cWvxO-bslx-Jw6DNGF8oZ03KtBZ9n3p8wmlwcA2VbXKDoyIdMbrQ-hf_v-AtXa51H</recordid><startdate>19890502</startdate><enddate>19890502</enddate><creator>Vonhof, Stefan</creator><creator>Paakkari, Ilari</creator><creator>Feuerstein, Giora</creator><creator>Cohen, Louis A.</creator><creator>Labroo, Virender M.</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>19890502</creationdate><title>Receptor binding of fluorinated histidine analogs of thyrotropin-releasing hormone in various regions of the rat brain</title><author>Vonhof, Stefan ; Paakkari, Ilari ; Feuerstein, Giora ; Cohen, Louis A. ; Labroo, Virender M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c386t-c23f4a40740303a32790e7d07b293ae6c6b34c679967aed9dac0fa4ad36608863</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1989</creationdate><topic>Affinity, Receptors</topic><topic>Animals</topic><topic>Binding, Competitive - drug effects</topic><topic>Biological and medical sciences</topic><topic>Brain - drug effects</topic><topic>Brain - metabolism</topic><topic>Histidine - analogs & derivatives</topic><topic>Histidine - pharmacology</topic><topic>Hormones. Endocrine system</topic><topic>Hypothalamus - drug effects</topic><topic>Hypothalamus - metabolism</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Receptors, Thyroid Hormone - drug effects</topic><topic>Receptors, Thyroid Hormone - metabolism</topic><topic>Time Factors</topic><topic>TRH analog (fluorinated)</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Vonhof, Stefan</creatorcontrib><creatorcontrib>Paakkari, Ilari</creatorcontrib><creatorcontrib>Feuerstein, Giora</creatorcontrib><creatorcontrib>Cohen, Louis A.</creatorcontrib><creatorcontrib>Labroo, Virender M.</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>Vonhof, Stefan</au><au>Paakkari, Ilari</au><au>Feuerstein, Giora</au><au>Cohen, Louis A.</au><au>Labroo, Virender M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Receptor binding of fluorinated histidine analogs of thyrotropin-releasing hormone in various regions of the rat brain</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1989-05-02</date><risdate>1989</risdate><volume>164</volume><issue>1</issue><spage>77</spage><epage>83</epage><pages>77-83</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>Binding properties of [4(5)-fluoro-imidazole-His
2]-TRH (4(5)-F-TRH), [2-trifluoromethyl-imidazole-His
2]-TRH (2-CF
3-TRH) and [4(5)-trifluoromethyl-imidazole-His
2]-TRH (4(5)-CF
3-TRH), three novel TRH analogs, have been evaluated in rat pituitary, hypothalamus, brainstem and cortex tissue. 4(5)-F-TRH, previously shown to elicit arterial pressor responses and prolactin release similar to those of TRH, binds to TRH receptors with low, micromolar affinity (K
i = 7.5−13.5
μM) 2-CF
3-TRH, an analog of less cardiovascular but increased prolactin-releasing activity, shows K
i values of 3.3–4.9 μM. 4(5)-CF
3-TRH, which shows comparable biological activity to 2-CF
3-TRH, demonstrates a binding affinity which is virtually nonspecific (K
i = 0.39−1.01 mM). It is therefore concluded that the biological effects of these analogs are mediated either through low affinity TRH binding sites not recognized by [
3H][3Me-His
2]-TRH or through mechanisms not involving TRH receptors as such.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>2753081</pmid><doi>10.1016/0014-2999(89)90233-1</doi><tpages>7</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0014-2999 |
| ispartof | European journal of pharmacology, 1989-05, Vol.164 (1), p.77-83 |
| issn | 0014-2999 1879-0712 |
| language | eng |
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| subjects | Affinity, Receptors Animals Binding, Competitive - drug effects Biological and medical sciences Brain - drug effects Brain - metabolism Histidine - analogs & derivatives Histidine - pharmacology Hormones. Endocrine system Hypothalamus - drug effects Hypothalamus - metabolism Male Medical sciences Pharmacology. Drug treatments Rats Rats, Inbred Strains Receptors, Thyroid Hormone - drug effects Receptors, Thyroid Hormone - metabolism Time Factors TRH analog (fluorinated) |
| title | Receptor binding of fluorinated histidine analogs of thyrotropin-releasing hormone in various regions of the rat brain |
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