Neuroleptic properties of Y-20024, a new benzofurancarboxamide derivative
N-[(1-butyl-2-pyrrolidinyl) methyl]-2-methyl-5-sulfamoyl-2, 3-dihydrobenzofuran-7-carboxamide hydrochloride (Y-20024) was synthesized in our laboratories in anticipation of developing a new psychotropic drug. In the present study, the pharmacological properties of Y-20024 were compared with those of...
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| Veröffentlicht in: | Folia Pharmacologica Japonica 1989, Vol.94(5), pp.269-280 |
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| container_title | Folia Pharmacologica Japonica |
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| creator | FUKUDA, Takemi MORIMOTO, Yasuto MORIMOTO, Toshihiko SHOJI, Hidenori MURAKAMI, Shu TAHARA, Tetsuya SETOGUCHI, Michihide |
| description | N-[(1-butyl-2-pyrrolidinyl) methyl]-2-methyl-5-sulfamoyl-2, 3-dihydrobenzofuran-7-carboxamide hydrochloride (Y-20024) was synthesized in our laboratories in anticipation of developing a new psychotropic drug. In the present study, the pharmacological properties of Y-20024 were compared with those of sulpiride (SPR) and haloperidol (HPD). Administered orally, Y-20024 was 10 times stronger than SPR in inhibiting apomorphine (0.5 mg/kg, s.c.) -induced hyperactivity in mice; administered intravenously or intracerebroventricularly, it was 2 times or one third as strong, respectively. Y-20024 was almost equipotent to SPR in antagonizing apomorphine (0.1 mg/kg, s.c.)-induced vomiting in dogs. Combined with methamphetamine (5 mg/kg, i.p.), Y-20024 and SPR induced mortality dose-dependently in rats, but HPD did not. The mammotropic activity of Y-20024 administered orally once a day for 5 days was almost equipotent to that of SPR. From these results, Y-20024, pharmacologically similar to SPR, but superior in bioavailability and penetration through the blood brain barrier, may have potential usefulness as an antipsychotic drug. |
| doi_str_mv | 10.1254/fpj.94.269 |
| format | Article |
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In the present study, the pharmacological properties of Y-20024 were compared with those of sulpiride (SPR) and haloperidol (HPD). Administered orally, Y-20024 was 10 times stronger than SPR in inhibiting apomorphine (0.5 mg/kg, s.c.) -induced hyperactivity in mice; administered intravenously or intracerebroventricularly, it was 2 times or one third as strong, respectively. Y-20024 was almost equipotent to SPR in antagonizing apomorphine (0.1 mg/kg, s.c.)-induced vomiting in dogs. Combined with methamphetamine (5 mg/kg, i.p.), Y-20024 and SPR induced mortality dose-dependently in rats, but HPD did not. The mammotropic activity of Y-20024 administered orally once a day for 5 days was almost equipotent to that of SPR. From these results, Y-20024, pharmacologically similar to SPR, but superior in bioavailability and penetration through the blood brain barrier, may have potential usefulness as an antipsychotic drug.</description><identifier>ISSN: 0015-5691</identifier><identifier>EISSN: 1347-8397</identifier><identifier>DOI: 10.1254/fpj.94.269</identifier><identifier>PMID: 2575566</identifier><language>jpn</language><publisher>Japan: The Japanese Pharmacological Society</publisher><subject>Animals ; Antipsychotic Agents - administration & dosage ; Antipsychotic Agents - pharmacology ; Apomorphine - antagonists & inhibitors ; Benzofurans - administration & dosage ; Benzofurans - pharmacology ; Body Temperature - drug effects ; Catalepsy - drug therapy ; Dogs ; Dose-Response Relationship, Drug ; Drug Synergism ; Female ; Male ; Methamphetamine - antagonists & inhibitors ; Methamphetamine - toxicity ; Mice ; Motor Activity - drug effects ; Prolactin - metabolism ; Pyrrolidines - administration & dosage ; Pyrrolidines - pharmacology ; Rats ; Rats, Inbred Strains ; Self Stimulation - drug effects</subject><ispartof>Folia Pharmacologica Japonica, 1989, Vol.94(5), pp.269-280</ispartof><rights>The Japanese PharmacologicalSociety</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c399t-130828da701a763359cbdec57564f56d1ac0761c8acf9a073e0ad16d8473fe393</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,4024,27923,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2575566$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>FUKUDA, Takemi</creatorcontrib><creatorcontrib>MORIMOTO, Yasuto</creatorcontrib><creatorcontrib>MORIMOTO, Toshihiko</creatorcontrib><creatorcontrib>SHOJI, Hidenori</creatorcontrib><creatorcontrib>MURAKAMI, Shu</creatorcontrib><creatorcontrib>TAHARA, Tetsuya</creatorcontrib><creatorcontrib>SETOGUCHI, Michihide</creatorcontrib><title>Neuroleptic properties of Y-20024, a new benzofurancarboxamide derivative</title><title>Folia Pharmacologica Japonica</title><addtitle>Nihon Yakurigaku Zasshi</addtitle><description>N-[(1-butyl-2-pyrrolidinyl) methyl]-2-methyl-5-sulfamoyl-2, 3-dihydrobenzofuran-7-carboxamide hydrochloride (Y-20024) was synthesized in our laboratories in anticipation of developing a new psychotropic drug. In the present study, the pharmacological properties of Y-20024 were compared with those of sulpiride (SPR) and haloperidol (HPD). Administered orally, Y-20024 was 10 times stronger than SPR in inhibiting apomorphine (0.5 mg/kg, s.c.) -induced hyperactivity in mice; administered intravenously or intracerebroventricularly, it was 2 times or one third as strong, respectively. Y-20024 was almost equipotent to SPR in antagonizing apomorphine (0.1 mg/kg, s.c.)-induced vomiting in dogs. Combined with methamphetamine (5 mg/kg, i.p.), Y-20024 and SPR induced mortality dose-dependently in rats, but HPD did not. The mammotropic activity of Y-20024 administered orally once a day for 5 days was almost equipotent to that of SPR. From these results, Y-20024, pharmacologically similar to SPR, but superior in bioavailability and penetration through the blood brain barrier, may have potential usefulness as an antipsychotic drug.</description><subject>Animals</subject><subject>Antipsychotic Agents - administration & dosage</subject><subject>Antipsychotic Agents - pharmacology</subject><subject>Apomorphine - antagonists & inhibitors</subject><subject>Benzofurans - administration & dosage</subject><subject>Benzofurans - pharmacology</subject><subject>Body Temperature - drug effects</subject><subject>Catalepsy - drug therapy</subject><subject>Dogs</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug Synergism</subject><subject>Female</subject><subject>Male</subject><subject>Methamphetamine - antagonists & inhibitors</subject><subject>Methamphetamine - toxicity</subject><subject>Mice</subject><subject>Motor Activity - drug effects</subject><subject>Prolactin - metabolism</subject><subject>Pyrrolidines - administration & dosage</subject><subject>Pyrrolidines - pharmacology</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Self Stimulation - drug effects</subject><issn>0015-5691</issn><issn>1347-8397</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1989</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kD1PwzAQhi0EKlXpwo6UGZFix1_xiCoKlSpYYGCKLvYZUrVJ5KTl49fjKlWXu-F99ejuIeSa0RnLpLj37XpmxCxT5oyMGRc6zbnR52RMKZOpVIZdkmnXVSWlUmdacTYio0xqKZUak-UL7kKzwbavbNKGpsXQV9gljU8-0ozSTNwlkNT4nZRY_zV-F6C2EMrmB7aVw8RhqPbQV3u8IhceNh1Oj3tC3hePb_PndPX6tJw_rFLLjelTxmme5Q40ZRCP4dLY0qGN9yjhpXIMLNWK2RysN0A1RwqOKZcLzT1ywyfkduDa0HRdQF-0odpC-C0YLQ5GimikMKKIRmL5Zii3u3KL7lQ9_h_z-ZCvux4-8ZRDtGA3eEAxI8QBJ4cRqafUfkEosOb_uPpzXw</recordid><startdate>1989</startdate><enddate>1989</enddate><creator>FUKUDA, Takemi</creator><creator>MORIMOTO, Yasuto</creator><creator>MORIMOTO, Toshihiko</creator><creator>SHOJI, Hidenori</creator><creator>MURAKAMI, Shu</creator><creator>TAHARA, Tetsuya</creator><creator>SETOGUCHI, Michihide</creator><general>The Japanese Pharmacological Society</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>1989</creationdate><title>Neuroleptic properties of Y-20024, a new benzofurancarboxamide derivative</title><author>FUKUDA, Takemi ; MORIMOTO, Yasuto ; MORIMOTO, Toshihiko ; SHOJI, Hidenori ; MURAKAMI, Shu ; TAHARA, Tetsuya ; SETOGUCHI, Michihide</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c399t-130828da701a763359cbdec57564f56d1ac0761c8acf9a073e0ad16d8473fe393</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>jpn</language><creationdate>1989</creationdate><topic>Animals</topic><topic>Antipsychotic Agents - administration & dosage</topic><topic>Antipsychotic Agents - pharmacology</topic><topic>Apomorphine - antagonists & inhibitors</topic><topic>Benzofurans - administration & dosage</topic><topic>Benzofurans - pharmacology</topic><topic>Body Temperature - drug effects</topic><topic>Catalepsy - drug therapy</topic><topic>Dogs</topic><topic>Dose-Response Relationship, Drug</topic><topic>Drug Synergism</topic><topic>Female</topic><topic>Male</topic><topic>Methamphetamine - antagonists & inhibitors</topic><topic>Methamphetamine - toxicity</topic><topic>Mice</topic><topic>Motor Activity - drug effects</topic><topic>Prolactin - metabolism</topic><topic>Pyrrolidines - administration & dosage</topic><topic>Pyrrolidines - pharmacology</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Self Stimulation - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>FUKUDA, Takemi</creatorcontrib><creatorcontrib>MORIMOTO, Yasuto</creatorcontrib><creatorcontrib>MORIMOTO, Toshihiko</creatorcontrib><creatorcontrib>SHOJI, Hidenori</creatorcontrib><creatorcontrib>MURAKAMI, Shu</creatorcontrib><creatorcontrib>TAHARA, Tetsuya</creatorcontrib><creatorcontrib>SETOGUCHI, Michihide</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Folia Pharmacologica Japonica</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>FUKUDA, Takemi</au><au>MORIMOTO, Yasuto</au><au>MORIMOTO, Toshihiko</au><au>SHOJI, Hidenori</au><au>MURAKAMI, Shu</au><au>TAHARA, Tetsuya</au><au>SETOGUCHI, Michihide</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Neuroleptic properties of Y-20024, a new benzofurancarboxamide derivative</atitle><jtitle>Folia Pharmacologica Japonica</jtitle><addtitle>Nihon Yakurigaku Zasshi</addtitle><date>1989</date><risdate>1989</risdate><volume>94</volume><issue>5</issue><spage>269</spage><epage>280</epage><pages>269-280</pages><issn>0015-5691</issn><eissn>1347-8397</eissn><abstract>N-[(1-butyl-2-pyrrolidinyl) methyl]-2-methyl-5-sulfamoyl-2, 3-dihydrobenzofuran-7-carboxamide hydrochloride (Y-20024) was synthesized in our laboratories in anticipation of developing a new psychotropic drug. In the present study, the pharmacological properties of Y-20024 were compared with those of sulpiride (SPR) and haloperidol (HPD). Administered orally, Y-20024 was 10 times stronger than SPR in inhibiting apomorphine (0.5 mg/kg, s.c.) -induced hyperactivity in mice; administered intravenously or intracerebroventricularly, it was 2 times or one third as strong, respectively. Y-20024 was almost equipotent to SPR in antagonizing apomorphine (0.1 mg/kg, s.c.)-induced vomiting in dogs. Combined with methamphetamine (5 mg/kg, i.p.), Y-20024 and SPR induced mortality dose-dependently in rats, but HPD did not. The mammotropic activity of Y-20024 administered orally once a day for 5 days was almost equipotent to that of SPR. From these results, Y-20024, pharmacologically similar to SPR, but superior in bioavailability and penetration through the blood brain barrier, may have potential usefulness as an antipsychotic drug.</abstract><cop>Japan</cop><pub>The Japanese Pharmacological Society</pub><pmid>2575566</pmid><doi>10.1254/fpj.94.269</doi><tpages>12</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | Folia Pharmacologica Japonica, 1989, Vol.94(5), pp.269-280 |
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| source | MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals |
| subjects | Animals Antipsychotic Agents - administration & dosage Antipsychotic Agents - pharmacology Apomorphine - antagonists & inhibitors Benzofurans - administration & dosage Benzofurans - pharmacology Body Temperature - drug effects Catalepsy - drug therapy Dogs Dose-Response Relationship, Drug Drug Synergism Female Male Methamphetamine - antagonists & inhibitors Methamphetamine - toxicity Mice Motor Activity - drug effects Prolactin - metabolism Pyrrolidines - administration & dosage Pyrrolidines - pharmacology Rats Rats, Inbred Strains Self Stimulation - drug effects |
| title | Neuroleptic properties of Y-20024, a new benzofurancarboxamide derivative |
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