Characterization of 5‐HT3 and ‘atypical’ 5‐HT receptors mediating guinea‐pig ileal contractions in vitro
1 Neuronal 5‐hydroxytryptamine (5‐HT) receptors mediating contraction of guinea‐pig ileal segments have been characterized in vitro by the use of methysergide to block 5‐HT1‐like and 5‐HT2 receptors. Concentration‐response curves to 5‐HT were biphasic (first phase, defined as those responses occurri...
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| Veröffentlicht in: | British journal of pharmacology 1990-11, Vol.101 (3), p.513-520 |
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| creator | Eglen, R.M. Swank, S.R. Walsh, L.K.M. Whiting, R.L. |
| description | 1
Neuronal 5‐hydroxytryptamine (5‐HT) receptors mediating contraction of guinea‐pig ileal segments have been characterized in vitro by the use of methysergide to block 5‐HT1‐like and 5‐HT2 receptors. Concentration‐response curves to 5‐HT were biphasic (first phase, defined as those responses occurring between 1 nm and 0.32 μm 5‐HT, –log EC50 = 7.15 ± 0.08; second phase, defined as these responses occurring between 0.32 μm and 32 μm 5‐HT, –log EC50 = 5.32 ± 0.03) but monophasic to 5‐methoxytryptamine (−log EC50 = 7.0 ± 0.08) and 2 methyl 5‐HT (−log EC50 = 5.2 ± 0.13). The maximal response of the first phase to 5‐HT and the maximal response to 5‐methoxytryptamine were 30 ± 4% and 35 ± 5% respectively of the maximum response to the second phase of the 5‐HT concentration‐effect curve (set at 100%). In contrast, the maximal response to 2‐methyl‐5‐HT equalled that obtained with 5‐HT (second phase).
2
The responses comprising the second phase of the concentration‐effect curve to 5‐HT were antagonized by 1 μm ICS 205–930, ondansetron, granisetron, quipazine, N‐methyl‐quipazine and (R,S)‐zacopride and the following pKB values, with 5‐HT as the agonist, were obtained at the 5‐HT3 receptor: ICS 205–930 7.61 ± 0.05, ondansetron 6.90 ± 0.04, granisetron 7.90 ± 0.04, (S)‐zacopride 8.11 ± 0.06, (R,S)‐zacopride 7.64 ± 0.11, and (R)‐zacopride 7.27 ± 0.06.
3
Under conditions of 5‐HT1‐like, 5‐HT2 and 5‐HT3 receptor blockade, the following rank order of agonism was observed: 5‐HT > 5‐methoxytryptamine = renzapride > (S)‐zacopride > (R,S)‐zacopride > 5‐carboxamidotryptamine > BRL 24682 > (R)‐zacopride > metoclopramide > 2‐methyl‐5‐HT ≫ sulpiride. 8‐Dihydroxydiphenylaminotetralin (8‐OHDPAT), GR 43175, N,N‐dipropyl‐5‐carboxamidotryptamine, ondansetron, ICS 205–930, granisetron, quipazine and N‐methyl‐quipazine were inactive as agonists and antagonists. Relative to 5‐HT, (R,S)‐zacopride acted as a partial agonist (intrinsic activity, α = 0.80; –log EC50 = 6.3 ± 0.12; –log KA = 6.1 ± 0.03) as did (R)‐zacopride (α = 0.4, –log EC50 5.7 ± 0.08, –log KA = 5.5 ± 0.11). (S)‐zacopride acted as a full agonist (−log EC50 = 6.9 ± 0.03). ICS 205–930 (3 μm) antagonized competitively responses to 5‐HT, 5 methoxytryptamine, (R,S)‐ and (S)‐zacopride and 5‐carboxamidotryptamine yielding –log KB estimates ranging from 6.1–6.5.
4
It is concluded that two different 5‐HT receptors mediate excitatory neuronal responses in the guinea‐pig ileum. 5‐HT3 receptors mediate the second phase of the biphasic c |
| doi_str_mv | 10.1111/j.1476-5381.1990.tb14113.x |
| format | Article |
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Neuronal 5‐hydroxytryptamine (5‐HT) receptors mediating contraction of guinea‐pig ileal segments have been characterized in vitro by the use of methysergide to block 5‐HT1‐like and 5‐HT2 receptors. Concentration‐response curves to 5‐HT were biphasic (first phase, defined as those responses occurring between 1 nm and 0.32 μm 5‐HT, –log EC50 = 7.15 ± 0.08; second phase, defined as these responses occurring between 0.32 μm and 32 μm 5‐HT, –log EC50 = 5.32 ± 0.03) but monophasic to 5‐methoxytryptamine (−log EC50 = 7.0 ± 0.08) and 2 methyl 5‐HT (−log EC50 = 5.2 ± 0.13). The maximal response of the first phase to 5‐HT and the maximal response to 5‐methoxytryptamine were 30 ± 4% and 35 ± 5% respectively of the maximum response to the second phase of the 5‐HT concentration‐effect curve (set at 100%). In contrast, the maximal response to 2‐methyl‐5‐HT equalled that obtained with 5‐HT (second phase).
2
The responses comprising the second phase of the concentration‐effect curve to 5‐HT were antagonized by 1 μm ICS 205–930, ondansetron, granisetron, quipazine, N‐methyl‐quipazine and (R,S)‐zacopride and the following pKB values, with 5‐HT as the agonist, were obtained at the 5‐HT3 receptor: ICS 205–930 7.61 ± 0.05, ondansetron 6.90 ± 0.04, granisetron 7.90 ± 0.04, (S)‐zacopride 8.11 ± 0.06, (R,S)‐zacopride 7.64 ± 0.11, and (R)‐zacopride 7.27 ± 0.06.
3
Under conditions of 5‐HT1‐like, 5‐HT2 and 5‐HT3 receptor blockade, the following rank order of agonism was observed: 5‐HT > 5‐methoxytryptamine = renzapride > (S)‐zacopride > (R,S)‐zacopride > 5‐carboxamidotryptamine > BRL 24682 > (R)‐zacopride > metoclopramide > 2‐methyl‐5‐HT ≫ sulpiride. 8‐Dihydroxydiphenylaminotetralin (8‐OHDPAT), GR 43175, N,N‐dipropyl‐5‐carboxamidotryptamine, ondansetron, ICS 205–930, granisetron, quipazine and N‐methyl‐quipazine were inactive as agonists and antagonists. Relative to 5‐HT, (R,S)‐zacopride acted as a partial agonist (intrinsic activity, α = 0.80; –log EC50 = 6.3 ± 0.12; –log KA = 6.1 ± 0.03) as did (R)‐zacopride (α = 0.4, –log EC50 5.7 ± 0.08, –log KA = 5.5 ± 0.11). (S)‐zacopride acted as a full agonist (−log EC50 = 6.9 ± 0.03). ICS 205–930 (3 μm) antagonized competitively responses to 5‐HT, 5 methoxytryptamine, (R,S)‐ and (S)‐zacopride and 5‐carboxamidotryptamine yielding –log KB estimates ranging from 6.1–6.5.
4
It is concluded that two different 5‐HT receptors mediate excitatory neuronal responses in the guinea‐pig ileum. 5‐HT3 receptors mediate the second phase of the biphasic concentration‐response curve, whereas a receptor with properties distinct from the 5‐HT1‐like, 5‐HT2 and 5‐HT3 subtypes mediates the initial phase of the concentration‐response curve. This receptor, which exhibits a close similarity to the 5‐HT4 subtype is: (1) stimulated by 5‐methoxytryptamine but not 2‐methyl‐5‐HT; (2) stimulated selectively by certain substituted benzamides; (3) recognizes the optical isomers of zacopride and (4) is blocked by relatively high concentrations ICS 205–930 (pKB = 6.0–6.5) but not ondansetron, granisetron, quipazine or N‐methyl‐quipazine.</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1111/j.1476-5381.1990.tb14113.x</identifier><identifier>PMID: 2076474</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>Animals ; Guinea Pigs ; Ileum - drug effects ; Ileum - physiology ; In Vitro Techniques ; Male ; Muscle Contraction - drug effects ; Muscle Contraction - physiology ; Phenoxybenzamine - pharmacology ; Receptors, Serotonin - classification ; Receptors, Serotonin - drug effects ; Receptors, Serotonin - physiology ; Serotonin - pharmacology ; Serotonin Antagonists - pharmacology ; Tetrodotoxin - pharmacology</subject><ispartof>British journal of pharmacology, 1990-11, Vol.101 (3), p.513-520</ispartof><rights>1990 British Pharmacological Society</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1917750/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1917750/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,727,780,784,885,27924,27925,53791,53793</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2076474$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Eglen, R.M.</creatorcontrib><creatorcontrib>Swank, S.R.</creatorcontrib><creatorcontrib>Walsh, L.K.M.</creatorcontrib><creatorcontrib>Whiting, R.L.</creatorcontrib><title>Characterization of 5‐HT3 and ‘atypical’ 5‐HT receptors mediating guinea‐pig ileal contractions in vitro</title><title>British journal of pharmacology</title><addtitle>Br J Pharmacol</addtitle><description>1
Neuronal 5‐hydroxytryptamine (5‐HT) receptors mediating contraction of guinea‐pig ileal segments have been characterized in vitro by the use of methysergide to block 5‐HT1‐like and 5‐HT2 receptors. Concentration‐response curves to 5‐HT were biphasic (first phase, defined as those responses occurring between 1 nm and 0.32 μm 5‐HT, –log EC50 = 7.15 ± 0.08; second phase, defined as these responses occurring between 0.32 μm and 32 μm 5‐HT, –log EC50 = 5.32 ± 0.03) but monophasic to 5‐methoxytryptamine (−log EC50 = 7.0 ± 0.08) and 2 methyl 5‐HT (−log EC50 = 5.2 ± 0.13). The maximal response of the first phase to 5‐HT and the maximal response to 5‐methoxytryptamine were 30 ± 4% and 35 ± 5% respectively of the maximum response to the second phase of the 5‐HT concentration‐effect curve (set at 100%). In contrast, the maximal response to 2‐methyl‐5‐HT equalled that obtained with 5‐HT (second phase).
2
The responses comprising the second phase of the concentration‐effect curve to 5‐HT were antagonized by 1 μm ICS 205–930, ondansetron, granisetron, quipazine, N‐methyl‐quipazine and (R,S)‐zacopride and the following pKB values, with 5‐HT as the agonist, were obtained at the 5‐HT3 receptor: ICS 205–930 7.61 ± 0.05, ondansetron 6.90 ± 0.04, granisetron 7.90 ± 0.04, (S)‐zacopride 8.11 ± 0.06, (R,S)‐zacopride 7.64 ± 0.11, and (R)‐zacopride 7.27 ± 0.06.
3
Under conditions of 5‐HT1‐like, 5‐HT2 and 5‐HT3 receptor blockade, the following rank order of agonism was observed: 5‐HT > 5‐methoxytryptamine = renzapride > (S)‐zacopride > (R,S)‐zacopride > 5‐carboxamidotryptamine > BRL 24682 > (R)‐zacopride > metoclopramide > 2‐methyl‐5‐HT ≫ sulpiride. 8‐Dihydroxydiphenylaminotetralin (8‐OHDPAT), GR 43175, N,N‐dipropyl‐5‐carboxamidotryptamine, ondansetron, ICS 205–930, granisetron, quipazine and N‐methyl‐quipazine were inactive as agonists and antagonists. Relative to 5‐HT, (R,S)‐zacopride acted as a partial agonist (intrinsic activity, α = 0.80; –log EC50 = 6.3 ± 0.12; –log KA = 6.1 ± 0.03) as did (R)‐zacopride (α = 0.4, –log EC50 5.7 ± 0.08, –log KA = 5.5 ± 0.11). (S)‐zacopride acted as a full agonist (−log EC50 = 6.9 ± 0.03). ICS 205–930 (3 μm) antagonized competitively responses to 5‐HT, 5 methoxytryptamine, (R,S)‐ and (S)‐zacopride and 5‐carboxamidotryptamine yielding –log KB estimates ranging from 6.1–6.5.
4
It is concluded that two different 5‐HT receptors mediate excitatory neuronal responses in the guinea‐pig ileum. 5‐HT3 receptors mediate the second phase of the biphasic concentration‐response curve, whereas a receptor with properties distinct from the 5‐HT1‐like, 5‐HT2 and 5‐HT3 subtypes mediates the initial phase of the concentration‐response curve. This receptor, which exhibits a close similarity to the 5‐HT4 subtype is: (1) stimulated by 5‐methoxytryptamine but not 2‐methyl‐5‐HT; (2) stimulated selectively by certain substituted benzamides; (3) recognizes the optical isomers of zacopride and (4) is blocked by relatively high concentrations ICS 205–930 (pKB = 6.0–6.5) but not ondansetron, granisetron, quipazine or N‐methyl‐quipazine.</description><subject>Animals</subject><subject>Guinea Pigs</subject><subject>Ileum - drug effects</subject><subject>Ileum - physiology</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Muscle Contraction - drug effects</subject><subject>Muscle Contraction - physiology</subject><subject>Phenoxybenzamine - pharmacology</subject><subject>Receptors, Serotonin - classification</subject><subject>Receptors, Serotonin - drug effects</subject><subject>Receptors, Serotonin - physiology</subject><subject>Serotonin - pharmacology</subject><subject>Serotonin Antagonists - pharmacology</subject><subject>Tetrodotoxin - pharmacology</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1990</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpVkdFKwzAUhoMoc04fQQjetyZNmjY3og51wkAv5nVI07RL6drSdnPzao_gpb7ensTUlaHnJgc-zsfJ-QG4wsjFtq4zF9OAOT4JsYs5R24bYYoxcddHYHhAx2CIEAocjMPwFJw1TYaQhYE_AAMPBYwGdAjq8VzWUrW6Nh-yNWUBywT6u-3nZEagLGK4237JdlMZJfPd9rtHsNZKV21ZN3ChY2MHixSmS1NoaXllUmhyLXOoyqLt7NbbQFPAlWnr8hycJDJv9EX_jsDb48NsPHGmL0_P47upkxEfEwcrGlPlc56ECDPFOVc-lYqSxGMJZxxpL2BhEsskYp6Kolgx7XuIIc1lnKiIjMDN3lstI7ul0t0uuahqs5D1RpTSiP-kMHORliuBObZXQlZw-VdwmOyPZ_ntnr_b324OGCPRpSQy0UUhuihEl5LoUxJrcf86-W3JD2qbjuc</recordid><startdate>199011</startdate><enddate>199011</enddate><creator>Eglen, R.M.</creator><creator>Swank, S.R.</creator><creator>Walsh, L.K.M.</creator><creator>Whiting, R.L.</creator><general>Blackwell Publishing Ltd</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>5PM</scope></search><sort><creationdate>199011</creationdate><title>Characterization of 5‐HT3 and ‘atypical’ 5‐HT receptors mediating guinea‐pig ileal contractions in vitro</title><author>Eglen, R.M. ; Swank, S.R. ; Walsh, L.K.M. ; Whiting, R.L.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-j3513-1c4d4c599f8016c999c54ac43f26f9690e2768fdafb62cbbdc6e52060e9adfcb3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1990</creationdate><topic>Animals</topic><topic>Guinea Pigs</topic><topic>Ileum - drug effects</topic><topic>Ileum - physiology</topic><topic>In Vitro Techniques</topic><topic>Male</topic><topic>Muscle Contraction - drug effects</topic><topic>Muscle Contraction - physiology</topic><topic>Phenoxybenzamine - pharmacology</topic><topic>Receptors, Serotonin - classification</topic><topic>Receptors, Serotonin - drug effects</topic><topic>Receptors, Serotonin - physiology</topic><topic>Serotonin - pharmacology</topic><topic>Serotonin Antagonists - pharmacology</topic><topic>Tetrodotoxin - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Eglen, R.M.</creatorcontrib><creatorcontrib>Swank, S.R.</creatorcontrib><creatorcontrib>Walsh, L.K.M.</creatorcontrib><creatorcontrib>Whiting, R.L.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>British journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Eglen, R.M.</au><au>Swank, S.R.</au><au>Walsh, L.K.M.</au><au>Whiting, R.L.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Characterization of 5‐HT3 and ‘atypical’ 5‐HT receptors mediating guinea‐pig ileal contractions in vitro</atitle><jtitle>British journal of pharmacology</jtitle><addtitle>Br J Pharmacol</addtitle><date>1990-11</date><risdate>1990</risdate><volume>101</volume><issue>3</issue><spage>513</spage><epage>520</epage><pages>513-520</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><abstract>1
Neuronal 5‐hydroxytryptamine (5‐HT) receptors mediating contraction of guinea‐pig ileal segments have been characterized in vitro by the use of methysergide to block 5‐HT1‐like and 5‐HT2 receptors. Concentration‐response curves to 5‐HT were biphasic (first phase, defined as those responses occurring between 1 nm and 0.32 μm 5‐HT, –log EC50 = 7.15 ± 0.08; second phase, defined as these responses occurring between 0.32 μm and 32 μm 5‐HT, –log EC50 = 5.32 ± 0.03) but monophasic to 5‐methoxytryptamine (−log EC50 = 7.0 ± 0.08) and 2 methyl 5‐HT (−log EC50 = 5.2 ± 0.13). The maximal response of the first phase to 5‐HT and the maximal response to 5‐methoxytryptamine were 30 ± 4% and 35 ± 5% respectively of the maximum response to the second phase of the 5‐HT concentration‐effect curve (set at 100%). In contrast, the maximal response to 2‐methyl‐5‐HT equalled that obtained with 5‐HT (second phase).
2
The responses comprising the second phase of the concentration‐effect curve to 5‐HT were antagonized by 1 μm ICS 205–930, ondansetron, granisetron, quipazine, N‐methyl‐quipazine and (R,S)‐zacopride and the following pKB values, with 5‐HT as the agonist, were obtained at the 5‐HT3 receptor: ICS 205–930 7.61 ± 0.05, ondansetron 6.90 ± 0.04, granisetron 7.90 ± 0.04, (S)‐zacopride 8.11 ± 0.06, (R,S)‐zacopride 7.64 ± 0.11, and (R)‐zacopride 7.27 ± 0.06.
3
Under conditions of 5‐HT1‐like, 5‐HT2 and 5‐HT3 receptor blockade, the following rank order of agonism was observed: 5‐HT > 5‐methoxytryptamine = renzapride > (S)‐zacopride > (R,S)‐zacopride > 5‐carboxamidotryptamine > BRL 24682 > (R)‐zacopride > metoclopramide > 2‐methyl‐5‐HT ≫ sulpiride. 8‐Dihydroxydiphenylaminotetralin (8‐OHDPAT), GR 43175, N,N‐dipropyl‐5‐carboxamidotryptamine, ondansetron, ICS 205–930, granisetron, quipazine and N‐methyl‐quipazine were inactive as agonists and antagonists. Relative to 5‐HT, (R,S)‐zacopride acted as a partial agonist (intrinsic activity, α = 0.80; –log EC50 = 6.3 ± 0.12; –log KA = 6.1 ± 0.03) as did (R)‐zacopride (α = 0.4, –log EC50 5.7 ± 0.08, –log KA = 5.5 ± 0.11). (S)‐zacopride acted as a full agonist (−log EC50 = 6.9 ± 0.03). ICS 205–930 (3 μm) antagonized competitively responses to 5‐HT, 5 methoxytryptamine, (R,S)‐ and (S)‐zacopride and 5‐carboxamidotryptamine yielding –log KB estimates ranging from 6.1–6.5.
4
It is concluded that two different 5‐HT receptors mediate excitatory neuronal responses in the guinea‐pig ileum. 5‐HT3 receptors mediate the second phase of the biphasic concentration‐response curve, whereas a receptor with properties distinct from the 5‐HT1‐like, 5‐HT2 and 5‐HT3 subtypes mediates the initial phase of the concentration‐response curve. This receptor, which exhibits a close similarity to the 5‐HT4 subtype is: (1) stimulated by 5‐methoxytryptamine but not 2‐methyl‐5‐HT; (2) stimulated selectively by certain substituted benzamides; (3) recognizes the optical isomers of zacopride and (4) is blocked by relatively high concentrations ICS 205–930 (pKB = 6.0–6.5) but not ondansetron, granisetron, quipazine or N‐methyl‐quipazine.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>2076474</pmid><doi>10.1111/j.1476-5381.1990.tb14113.x</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Animals Guinea Pigs Ileum - drug effects Ileum - physiology In Vitro Techniques Male Muscle Contraction - drug effects Muscle Contraction - physiology Phenoxybenzamine - pharmacology Receptors, Serotonin - classification Receptors, Serotonin - drug effects Receptors, Serotonin - physiology Serotonin - pharmacology Serotonin Antagonists - pharmacology Tetrodotoxin - pharmacology |
| title | Characterization of 5‐HT3 and ‘atypical’ 5‐HT receptors mediating guinea‐pig ileal contractions in vitro |
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