Discriminative stimulus effects of 8-OH-DPAT in pigeons : antagonism studies with the putative 5-HT1A receptor antagonists BMY 7378 and NAN-190
Pigeons were trained to discriminate 0.3 mg/kg of the 5-HT1A receptor agonist 8-hydroxy-2-(di-N-propylamino)tetralin (8-OH-DPAT) from saline. RU 24969 (5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole), at doses of 5.6-10 mg/kg, and eltoprazine (5.6 mg/kg), both mixed 5-HT1A/B agonists, substi...
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| Veröffentlicht in: | European journal of pharmacology 1992-07, Vol.217 (2-3), p.163-171 |
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| description | Pigeons were trained to discriminate 0.3 mg/kg of the 5-HT1A receptor agonist 8-hydroxy-2-(di-N-propylamino)tetralin (8-OH-DPAT) from saline. RU 24969 (5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole), at doses of 5.6-10 mg/kg, and eltoprazine (5.6 mg/kg), both mixed 5-HT1A/B agonists, substituted completely for 8-OH-DPAT, whereas 3.0-10 mg/kg of the 5-HT1B/C agonist TFMPP (1-(m-trifluromethylphenyl)piperazine) and 0.1-3.0 of the 5-HT3 antagonist MDL 72222 (3-tropanyl-3,5-dichlorobenzoate) yielded only saline-appropriate responses. Substitution for 8-OH-DPAT by eltoprazine and RU 24969, which does not occur in rats, provides in vivo support for the suggestion that the absence of a 5-HT1B receptor in the pigeon allows more complete expression of 5-HT1A-mediated effects. BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl)]8-azaspirol-[4.5]- decane-7,9-dione) attenuated the 8-OH-DPAT stimulus at doses from 1.0 to 10 mg/kg but, when administered alone, also resulted in approximately 40% 8-OH-DPAT-appropriate responding at the highest dose. NAN-190 (1-(2-methoxyphenyl)-4-[4-(2-phthalamido)butyl)-piperazine (0.3-3.0 mg/kg) produced a dose-dependent and complete antagonism of the 8-OH-DPAT-discriminative stimulus; administered alone NAN-190 resulted only in saline-key responding. NAN-190 also reversed the rate-decreasing effects of higher doses of 8-OH-DPAT. The beta-adrenoceptor antagonist (+/-)-pindolol (5.6-17 mg/kg) antagonized the discriminative stimulus effects of lower 8-OH-DPAT doses but was unable to block the effects of higher doses of 8-OH-DPAT. Prazosin (1.0-10 mg/kg), which like NAN-190, is an alpha 1-antagonist, neither substituted for nor blocked the discriminative stimulus effects of 8-OH-DPAT. These results suggest that NAN-190 is an effective 5-HT1A receptor antagonist in this procedure with pigeons, with no indication of agonist actions, whereas BMY 7378 and pindolol are best characterized as partial 5-HT1A receptor agonists. |
| doi_str_mv | 10.1016/0014-2999(92)90841-Q |
| format | Article |
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E ; GLEESON, S</creator><creatorcontrib>BARRETT, J. E ; GLEESON, S</creatorcontrib><description>Pigeons were trained to discriminate 0.3 mg/kg of the 5-HT1A receptor agonist 8-hydroxy-2-(di-N-propylamino)tetralin (8-OH-DPAT) from saline. RU 24969 (5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole), at doses of 5.6-10 mg/kg, and eltoprazine (5.6 mg/kg), both mixed 5-HT1A/B agonists, substituted completely for 8-OH-DPAT, whereas 3.0-10 mg/kg of the 5-HT1B/C agonist TFMPP (1-(m-trifluromethylphenyl)piperazine) and 0.1-3.0 of the 5-HT3 antagonist MDL 72222 (3-tropanyl-3,5-dichlorobenzoate) yielded only saline-appropriate responses. Substitution for 8-OH-DPAT by eltoprazine and RU 24969, which does not occur in rats, provides in vivo support for the suggestion that the absence of a 5-HT1B receptor in the pigeon allows more complete expression of 5-HT1A-mediated effects. BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl)]8-azaspirol-[4.5]- decane-7,9-dione) attenuated the 8-OH-DPAT stimulus at doses from 1.0 to 10 mg/kg but, when administered alone, also resulted in approximately 40% 8-OH-DPAT-appropriate responding at the highest dose. NAN-190 (1-(2-methoxyphenyl)-4-[4-(2-phthalamido)butyl)-piperazine (0.3-3.0 mg/kg) produced a dose-dependent and complete antagonism of the 8-OH-DPAT-discriminative stimulus; administered alone NAN-190 resulted only in saline-key responding. NAN-190 also reversed the rate-decreasing effects of higher doses of 8-OH-DPAT. The beta-adrenoceptor antagonist (+/-)-pindolol (5.6-17 mg/kg) antagonized the discriminative stimulus effects of lower 8-OH-DPAT doses but was unable to block the effects of higher doses of 8-OH-DPAT. Prazosin (1.0-10 mg/kg), which like NAN-190, is an alpha 1-antagonist, neither substituted for nor blocked the discriminative stimulus effects of 8-OH-DPAT. These results suggest that NAN-190 is an effective 5-HT1A receptor antagonist in this procedure with pigeons, with no indication of agonist actions, whereas BMY 7378 and pindolol are best characterized as partial 5-HT1A receptor agonists.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(92)90841-Q</identifier><identifier>PMID: 1425937</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier</publisher><subject>8-Hydroxy-2-(di-n-propylamino)tetralin - antagonists & inhibitors ; 8-Hydroxy-2-(di-n-propylamino)tetralin - pharmacology ; Animals ; Behavioral psychophysiology ; Biological and medical sciences ; Columbidae ; Discrimination (Psychology) - drug effects ; Dose-Response Relationship, Drug ; Fundamental and applied biological sciences. Psychology ; Indoles - pharmacology ; Neurotransmission and behavior ; Pindolol - pharmacology ; Piperazines - administration & dosage ; Piperazines - pharmacology ; Prazosin - pharmacology ; Psychology. Psychoanalysis. Psychiatry ; Psychology. Psychophysiology ; Serotonin Antagonists - pharmacology</subject><ispartof>European journal of pharmacology, 1992-07, Vol.217 (2-3), p.163-171</ispartof><rights>1992 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c246t-543006faa7a360fdfe4756f570b2019a555a9503e994a25e5d98286778b838873</citedby><cites>FETCH-LOGICAL-c246t-543006faa7a360fdfe4756f570b2019a555a9503e994a25e5d98286778b838873</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27903,27904</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=5373108$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/1425937$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>BARRETT, J. E</creatorcontrib><creatorcontrib>GLEESON, S</creatorcontrib><title>Discriminative stimulus effects of 8-OH-DPAT in pigeons : antagonism studies with the putative 5-HT1A receptor antagonists BMY 7378 and NAN-190</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>Pigeons were trained to discriminate 0.3 mg/kg of the 5-HT1A receptor agonist 8-hydroxy-2-(di-N-propylamino)tetralin (8-OH-DPAT) from saline. RU 24969 (5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole), at doses of 5.6-10 mg/kg, and eltoprazine (5.6 mg/kg), both mixed 5-HT1A/B agonists, substituted completely for 8-OH-DPAT, whereas 3.0-10 mg/kg of the 5-HT1B/C agonist TFMPP (1-(m-trifluromethylphenyl)piperazine) and 0.1-3.0 of the 5-HT3 antagonist MDL 72222 (3-tropanyl-3,5-dichlorobenzoate) yielded only saline-appropriate responses. Substitution for 8-OH-DPAT by eltoprazine and RU 24969, which does not occur in rats, provides in vivo support for the suggestion that the absence of a 5-HT1B receptor in the pigeon allows more complete expression of 5-HT1A-mediated effects. BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl)]8-azaspirol-[4.5]- decane-7,9-dione) attenuated the 8-OH-DPAT stimulus at doses from 1.0 to 10 mg/kg but, when administered alone, also resulted in approximately 40% 8-OH-DPAT-appropriate responding at the highest dose. NAN-190 (1-(2-methoxyphenyl)-4-[4-(2-phthalamido)butyl)-piperazine (0.3-3.0 mg/kg) produced a dose-dependent and complete antagonism of the 8-OH-DPAT-discriminative stimulus; administered alone NAN-190 resulted only in saline-key responding. NAN-190 also reversed the rate-decreasing effects of higher doses of 8-OH-DPAT. The beta-adrenoceptor antagonist (+/-)-pindolol (5.6-17 mg/kg) antagonized the discriminative stimulus effects of lower 8-OH-DPAT doses but was unable to block the effects of higher doses of 8-OH-DPAT. Prazosin (1.0-10 mg/kg), which like NAN-190, is an alpha 1-antagonist, neither substituted for nor blocked the discriminative stimulus effects of 8-OH-DPAT. These results suggest that NAN-190 is an effective 5-HT1A receptor antagonist in this procedure with pigeons, with no indication of agonist actions, whereas BMY 7378 and pindolol are best characterized as partial 5-HT1A receptor agonists.</description><subject>8-Hydroxy-2-(di-n-propylamino)tetralin - antagonists & inhibitors</subject><subject>8-Hydroxy-2-(di-n-propylamino)tetralin - pharmacology</subject><subject>Animals</subject><subject>Behavioral psychophysiology</subject><subject>Biological and medical sciences</subject><subject>Columbidae</subject><subject>Discrimination (Psychology) - drug effects</subject><subject>Dose-Response Relationship, Drug</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Indoles - pharmacology</subject><subject>Neurotransmission and behavior</subject><subject>Pindolol - pharmacology</subject><subject>Piperazines - administration & dosage</subject><subject>Piperazines - pharmacology</subject><subject>Prazosin - pharmacology</subject><subject>Psychology. Psychoanalysis. Psychiatry</subject><subject>Psychology. Psychophysiology</subject><subject>Serotonin Antagonists - pharmacology</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1992</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkU1v1DAQhi0EKtvCPwDJB4TgYBjbcWz3trTAIpWWSsuBk-VNxq1RvoidIn4Ff5ksWbWnkWae9z08Q8gLDu848PI9AC-YsNa-seKtBVNwdv2IrLjRloHm4jFZ3SNPyXFKPwFAWaGOyBEvhLJSr8jf85iqMbax8zneIU05tlMzJYohYJUT7QM17GrDzr-ttzR2dIg32HeJnlLfZX_TdzG1c2qqIyb6O-Zbmm-RDlNe-hTbbPmajljhkPvxITRXf_j6g2qpzbys6eX6knELz8iT4JuEzw_zhHz_9HF7tmEXV5-_nK0vWCWKMjNVSIAyeK-9LCHUAQutyqA07ARw65VS3iqQaG3hhUJVWyNMqbXZGWmMlifk9dI7jP2vCVN27SwCm8Z32E_JaSmMXsBiAauxT2nE4IZZlx__OA5u_we3l-z2kp0V7v8f3PUce3non3Yt1g-hRfx8f3W4-1T5Joy-q2K6x9SMcDDyH9FFjaU</recordid><startdate>19920707</startdate><enddate>19920707</enddate><creator>BARRETT, J. E</creator><creator>GLEESON, S</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>19920707</creationdate><title>Discriminative stimulus effects of 8-OH-DPAT in pigeons : antagonism studies with the putative 5-HT1A receptor antagonists BMY 7378 and NAN-190</title><author>BARRETT, J. E ; GLEESON, S</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c246t-543006faa7a360fdfe4756f570b2019a555a9503e994a25e5d98286778b838873</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1992</creationdate><topic>8-Hydroxy-2-(di-n-propylamino)tetralin - antagonists & inhibitors</topic><topic>8-Hydroxy-2-(di-n-propylamino)tetralin - pharmacology</topic><topic>Animals</topic><topic>Behavioral psychophysiology</topic><topic>Biological and medical sciences</topic><topic>Columbidae</topic><topic>Discrimination (Psychology) - drug effects</topic><topic>Dose-Response Relationship, Drug</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Indoles - pharmacology</topic><topic>Neurotransmission and behavior</topic><topic>Pindolol - pharmacology</topic><topic>Piperazines - administration & dosage</topic><topic>Piperazines - pharmacology</topic><topic>Prazosin - pharmacology</topic><topic>Psychology. Psychoanalysis. Psychiatry</topic><topic>Psychology. Psychophysiology</topic><topic>Serotonin Antagonists - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>BARRETT, J. E</creatorcontrib><creatorcontrib>GLEESON, S</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>BARRETT, J. E</au><au>GLEESON, S</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Discriminative stimulus effects of 8-OH-DPAT in pigeons : antagonism studies with the putative 5-HT1A receptor antagonists BMY 7378 and NAN-190</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1992-07-07</date><risdate>1992</risdate><volume>217</volume><issue>2-3</issue><spage>163</spage><epage>171</epage><pages>163-171</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>Pigeons were trained to discriminate 0.3 mg/kg of the 5-HT1A receptor agonist 8-hydroxy-2-(di-N-propylamino)tetralin (8-OH-DPAT) from saline. RU 24969 (5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole), at doses of 5.6-10 mg/kg, and eltoprazine (5.6 mg/kg), both mixed 5-HT1A/B agonists, substituted completely for 8-OH-DPAT, whereas 3.0-10 mg/kg of the 5-HT1B/C agonist TFMPP (1-(m-trifluromethylphenyl)piperazine) and 0.1-3.0 of the 5-HT3 antagonist MDL 72222 (3-tropanyl-3,5-dichlorobenzoate) yielded only saline-appropriate responses. Substitution for 8-OH-DPAT by eltoprazine and RU 24969, which does not occur in rats, provides in vivo support for the suggestion that the absence of a 5-HT1B receptor in the pigeon allows more complete expression of 5-HT1A-mediated effects. BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl)]8-azaspirol-[4.5]- decane-7,9-dione) attenuated the 8-OH-DPAT stimulus at doses from 1.0 to 10 mg/kg but, when administered alone, also resulted in approximately 40% 8-OH-DPAT-appropriate responding at the highest dose. NAN-190 (1-(2-methoxyphenyl)-4-[4-(2-phthalamido)butyl)-piperazine (0.3-3.0 mg/kg) produced a dose-dependent and complete antagonism of the 8-OH-DPAT-discriminative stimulus; administered alone NAN-190 resulted only in saline-key responding. NAN-190 also reversed the rate-decreasing effects of higher doses of 8-OH-DPAT. The beta-adrenoceptor antagonist (+/-)-pindolol (5.6-17 mg/kg) antagonized the discriminative stimulus effects of lower 8-OH-DPAT doses but was unable to block the effects of higher doses of 8-OH-DPAT. Prazosin (1.0-10 mg/kg), which like NAN-190, is an alpha 1-antagonist, neither substituted for nor blocked the discriminative stimulus effects of 8-OH-DPAT. These results suggest that NAN-190 is an effective 5-HT1A receptor antagonist in this procedure with pigeons, with no indication of agonist actions, whereas BMY 7378 and pindolol are best characterized as partial 5-HT1A receptor agonists.</abstract><cop>Amsterdam</cop><pub>Elsevier</pub><pmid>1425937</pmid><doi>10.1016/0014-2999(92)90841-Q</doi><tpages>9</tpages></addata></record> |
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| subjects | 8-Hydroxy-2-(di-n-propylamino)tetralin - antagonists & inhibitors 8-Hydroxy-2-(di-n-propylamino)tetralin - pharmacology Animals Behavioral psychophysiology Biological and medical sciences Columbidae Discrimination (Psychology) - drug effects Dose-Response Relationship, Drug Fundamental and applied biological sciences. Psychology Indoles - pharmacology Neurotransmission and behavior Pindolol - pharmacology Piperazines - administration & dosage Piperazines - pharmacology Prazosin - pharmacology Psychology. Psychoanalysis. Psychiatry Psychology. Psychophysiology Serotonin Antagonists - pharmacology |
| title | Discriminative stimulus effects of 8-OH-DPAT in pigeons : antagonism studies with the putative 5-HT1A receptor antagonists BMY 7378 and NAN-190 |
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