Norvaline2-TRH : binding to TRH receptors in rat brain homogenates
Norvaline2-thyrotropin-releasing hormone ([Nva2]TRH) has been described as a thyrotropin-releasing hormone (TRH) analog with no thyrotropin (TSH)-releasing capacity but enhanced analeptic activity compared with TRH, as shown by the reversal of haloperidol-induced catalepsy. We have evaluated the rec...
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| Veröffentlicht in: | European journal of pharmacology 1990-05, Vol.180 (1), p.1-12 |
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| creator | VONHOF, S FEUERSTEIN, G. Z COHEN, L. A LABROO, V. M |
| description | Norvaline2-thyrotropin-releasing hormone ([Nva2]TRH) has been described as a thyrotropin-releasing hormone (TRH) analog with no thyrotropin (TSH)-releasing capacity but enhanced analeptic activity compared with TRH, as shown by the reversal of haloperidol-induced catalepsy. We have evaluated the receptor-binding properties of [Nva2]TRH in homogenates of rat anterior pituitary, hypothalamus, brainstem and cortex tissue, using [3H]TRH and [3H][3-Me-His2]TRH as radioligands. Apparent Ki values at high affinity TRH-binding sites, labelled predominantly by [3H][3-Me-His2]TRH, ranged from 17.0 to 36.9 microM in all tested regions. Additionally, [Nva2]TRH was shown to compete with [3H]TRH at low affinity TRH-binding sites with similar affinities. It is concluded that the loss of TSH-releasing activity of [Nva2]TRH appears to be due to a drastic reduction in binding affinity to the high affinity TRH receptor subtype. Its analeptic activity, however, may be mediated by low affinity TRH binding sites which are predominantly labelled by [3H]TRH or by yet unidentified mechanisms. |
| doi_str_mv | 10.1016/0014-2999(90)90586-U |
| format | Article |
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Z ; COHEN, L. A ; LABROO, V. M</creator><creatorcontrib>VONHOF, S ; FEUERSTEIN, G. Z ; COHEN, L. A ; LABROO, V. M</creatorcontrib><description>Norvaline2-thyrotropin-releasing hormone ([Nva2]TRH) has been described as a thyrotropin-releasing hormone (TRH) analog with no thyrotropin (TSH)-releasing capacity but enhanced analeptic activity compared with TRH, as shown by the reversal of haloperidol-induced catalepsy. We have evaluated the receptor-binding properties of [Nva2]TRH in homogenates of rat anterior pituitary, hypothalamus, brainstem and cortex tissue, using [3H]TRH and [3H][3-Me-His2]TRH as radioligands. Apparent Ki values at high affinity TRH-binding sites, labelled predominantly by [3H][3-Me-His2]TRH, ranged from 17.0 to 36.9 microM in all tested regions. Additionally, [Nva2]TRH was shown to compete with [3H]TRH at low affinity TRH-binding sites with similar affinities. It is concluded that the loss of TSH-releasing activity of [Nva2]TRH appears to be due to a drastic reduction in binding affinity to the high affinity TRH receptor subtype. Its analeptic activity, however, may be mediated by low affinity TRH binding sites which are predominantly labelled by [3H]TRH or by yet unidentified mechanisms.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(90)90586-U</identifier><identifier>PMID: 2163861</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier</publisher><subject>Animals ; Binding, Competitive - drug effects ; Biological and medical sciences ; Brain - drug effects ; Brain - metabolism ; Brain Stem - drug effects ; Brain Stem - metabolism ; Cerebral Cortex - drug effects ; Cerebral Cortex - metabolism ; Filtration ; Hormones. Endocrine system ; Hypothalamus - drug effects ; Hypothalamus - metabolism ; In Vitro Techniques ; Kinetics ; Male ; Medical sciences ; Pharmacology. Drug treatments ; Pyrrolidonecarboxylic Acid - analogs & derivatives ; Rats ; Rats, Inbred Strains ; Receptors, Neurotransmitter - metabolism ; Receptors, Thyrotropin-Releasing Hormone ; Thyrotropin-Releasing Hormone - analogs & derivatives ; Thyrotropin-Releasing Hormone - metabolism</subject><ispartof>European journal of pharmacology, 1990-05, Vol.180 (1), p.1-12</ispartof><rights>1990 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c1781-a293a89671bda3f2564160410bac628141431b22eedeb064988bd6297bb914df3</citedby><cites>FETCH-LOGICAL-c1781-a293a89671bda3f2564160410bac628141431b22eedeb064988bd6297bb914df3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=6893281$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2163861$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>VONHOF, S</creatorcontrib><creatorcontrib>FEUERSTEIN, G. Z</creatorcontrib><creatorcontrib>COHEN, L. A</creatorcontrib><creatorcontrib>LABROO, V. M</creatorcontrib><title>Norvaline2-TRH : binding to TRH receptors in rat brain homogenates</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>Norvaline2-thyrotropin-releasing hormone ([Nva2]TRH) has been described as a thyrotropin-releasing hormone (TRH) analog with no thyrotropin (TSH)-releasing capacity but enhanced analeptic activity compared with TRH, as shown by the reversal of haloperidol-induced catalepsy. We have evaluated the receptor-binding properties of [Nva2]TRH in homogenates of rat anterior pituitary, hypothalamus, brainstem and cortex tissue, using [3H]TRH and [3H][3-Me-His2]TRH as radioligands. Apparent Ki values at high affinity TRH-binding sites, labelled predominantly by [3H][3-Me-His2]TRH, ranged from 17.0 to 36.9 microM in all tested regions. Additionally, [Nva2]TRH was shown to compete with [3H]TRH at low affinity TRH-binding sites with similar affinities. It is concluded that the loss of TSH-releasing activity of [Nva2]TRH appears to be due to a drastic reduction in binding affinity to the high affinity TRH receptor subtype. Its analeptic activity, however, may be mediated by low affinity TRH binding sites which are predominantly labelled by [3H]TRH or by yet unidentified mechanisms.</description><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>Brain Stem - drug effects</subject><subject>Brain Stem - metabolism</subject><subject>Cerebral Cortex - drug effects</subject><subject>Cerebral Cortex - metabolism</subject><subject>Filtration</subject><subject>Hormones. Endocrine system</subject><subject>Hypothalamus - drug effects</subject><subject>Hypothalamus - metabolism</subject><subject>In Vitro Techniques</subject><subject>Kinetics</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Pyrrolidonecarboxylic Acid - analogs & derivatives</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Receptors, Neurotransmitter - metabolism</subject><subject>Receptors, Thyrotropin-Releasing Hormone</subject><subject>Thyrotropin-Releasing Hormone - analogs & derivatives</subject><subject>Thyrotropin-Releasing Hormone - metabolism</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1990</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kN9LwzAQx4Moc07_A4U-iOhDNZemac43HeqEoSDbc0jadFa6Ziad4H9v68qe7rjvD7gPIedAb4GCuKMUeMwQ8RrpDdJUinh5QMYgM4xpBuyQjPeWY3ISwhelNEWWjsiIgUikgDF5fHP-R9dVY1m8-JhF95GpmqJqVlHrov7gbW43rfMhqprI6zYyXnfbp1u7lW10a8MpOSp1HezZMCdk-fy0mM7i-fvL6_RhHueQSYg1w0RLFBmYQiclSwUHQTlQo3PBJHDgCRjGrC2soYKjlKYQDDNjEHhRJhNytevdePe9taFV6yrktq51Y902qAxlyjmDzsh3xty7ELwt1cZXa-1_FVDVo1M9F9VzUUjVPzq17GIXQ__WrG2xDw2sOv1y0HXIdV163eRV2NuExKR7I_kDemxz6w</recordid><startdate>19900503</startdate><enddate>19900503</enddate><creator>VONHOF, S</creator><creator>FEUERSTEIN, G. Z</creator><creator>COHEN, L. A</creator><creator>LABROO, V. M</creator><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>19900503</creationdate><title>Norvaline2-TRH : binding to TRH receptors in rat brain homogenates</title><author>VONHOF, S ; FEUERSTEIN, G. Z ; COHEN, L. A ; LABROO, V. M</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c1781-a293a89671bda3f2564160410bac628141431b22eedeb064988bd6297bb914df3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1990</creationdate><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>Brain Stem - drug effects</topic><topic>Brain Stem - metabolism</topic><topic>Cerebral Cortex - drug effects</topic><topic>Cerebral Cortex - metabolism</topic><topic>Filtration</topic><topic>Hormones. Endocrine system</topic><topic>Hypothalamus - drug effects</topic><topic>Hypothalamus - metabolism</topic><topic>In Vitro Techniques</topic><topic>Kinetics</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Pyrrolidonecarboxylic Acid - analogs & derivatives</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Receptors, Neurotransmitter - metabolism</topic><topic>Receptors, Thyrotropin-Releasing Hormone</topic><topic>Thyrotropin-Releasing Hormone - analogs & derivatives</topic><topic>Thyrotropin-Releasing Hormone - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>VONHOF, S</creatorcontrib><creatorcontrib>FEUERSTEIN, G. Z</creatorcontrib><creatorcontrib>COHEN, L. A</creatorcontrib><creatorcontrib>LABROO, V. 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M</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Norvaline2-TRH : binding to TRH receptors in rat brain homogenates</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1990-05-03</date><risdate>1990</risdate><volume>180</volume><issue>1</issue><spage>1</spage><epage>12</epage><pages>1-12</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>Norvaline2-thyrotropin-releasing hormone ([Nva2]TRH) has been described as a thyrotropin-releasing hormone (TRH) analog with no thyrotropin (TSH)-releasing capacity but enhanced analeptic activity compared with TRH, as shown by the reversal of haloperidol-induced catalepsy. We have evaluated the receptor-binding properties of [Nva2]TRH in homogenates of rat anterior pituitary, hypothalamus, brainstem and cortex tissue, using [3H]TRH and [3H][3-Me-His2]TRH as radioligands. Apparent Ki values at high affinity TRH-binding sites, labelled predominantly by [3H][3-Me-His2]TRH, ranged from 17.0 to 36.9 microM in all tested regions. Additionally, [Nva2]TRH was shown to compete with [3H]TRH at low affinity TRH-binding sites with similar affinities. It is concluded that the loss of TSH-releasing activity of [Nva2]TRH appears to be due to a drastic reduction in binding affinity to the high affinity TRH receptor subtype. Its analeptic activity, however, may be mediated by low affinity TRH binding sites which are predominantly labelled by [3H]TRH or by yet unidentified mechanisms.</abstract><cop>Amsterdam</cop><pub>Elsevier</pub><pmid>2163861</pmid><doi>10.1016/0014-2999(90)90586-U</doi><tpages>12</tpages></addata></record> |
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| subjects | Animals Binding, Competitive - drug effects Biological and medical sciences Brain - drug effects Brain - metabolism Brain Stem - drug effects Brain Stem - metabolism Cerebral Cortex - drug effects Cerebral Cortex - metabolism Filtration Hormones. Endocrine system Hypothalamus - drug effects Hypothalamus - metabolism In Vitro Techniques Kinetics Male Medical sciences Pharmacology. Drug treatments Pyrrolidonecarboxylic Acid - analogs & derivatives Rats Rats, Inbred Strains Receptors, Neurotransmitter - metabolism Receptors, Thyrotropin-Releasing Hormone Thyrotropin-Releasing Hormone - analogs & derivatives Thyrotropin-Releasing Hormone - metabolism |
| title | Norvaline2-TRH : binding to TRH receptors in rat brain homogenates |
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