Loading…

Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors

A series of novel and potent 6-heteroaryl-pyrrolidino-tetrahydroisoquinolines with dual histamine H(3) antagonist/serotonin transporter inhibitor activity is described. In vitro and in vivo data are discussed.

Saved in:

Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters 2007-08, Vol.17 (15), p.4374-4377
Main Authors:	KEITH, John M, GOMEZ, Leslie A, BARBIER, Ann J, WILSON, Sandy J, BOGGS, Jamin D, LORD, Brian, MAZUR, Curt, ALUISIO, Leah, LOVENBERG, Timothy W, CARRUTHERS, Nicholas I
Format:	Article
Language:	English
Subjects:	Animals Biological and medical sciences Blood-Brain Barrier Histamine H1 Antagonists - chemistry Histamine H1 Antagonists - pharmacology Medical sciences Mice Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Pyrrolidines - chemistry Pyrrolidines - pharmacology Receptors, Histamine H3 - drug effects Serotonin Plasma Membrane Transport Proteins - drug effects Serotoninergic system Structure-Activity Relationship Tetrahydroisoquinolines - chemistry Tetrahydroisoquinolines - pharmacology
Citations:	Items that this one cites Items that cite this one
Online Access:	Get full text
Tags:	Add Tag No Tags, Be the first to tag this record!

cited_by	cdi_FETCH-LOGICAL-c246t-58e14c0df769be2aea73b12f23253596c2c49579e84ed615d3f0d8bdd3aede9c3
cites	cdi_FETCH-LOGICAL-c246t-58e14c0df769be2aea73b12f23253596c2c49579e84ed615d3f0d8bdd3aede9c3
container_end_page	4377
container_issue	15
container_start_page	4374
container_title	Bioorganic & medicinal chemistry letters
container_volume	17
creator	KEITH, John M GOMEZ, Leslie A BARBIER, Ann J WILSON, Sandy J BOGGS, Jamin D LORD, Brian MAZUR, Curt ALUISIO, Leah LOVENBERG, Timothy W CARRUTHERS, Nicholas I
description	A series of novel and potent 6-heteroaryl-pyrrolidino-tetrahydroisoquinolines with dual histamine H(3) antagonist/serotonin transporter inhibitor activity is described. In vitro and in vivo data are discussed.
doi_str_mv	10.1016/j.bmcl.2007.03.043
format	article
fullrecord	<record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_70700036</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>70700036</sourcerecordid><originalsourceid>FETCH-LOGICAL-c246t-58e14c0df769be2aea73b12f23253596c2c49579e84ed615d3f0d8bdd3aede9c3</originalsourceid><addsrcrecordid>eNpFkL1uHCEURlEUK944eYEUEU3SzeQywPyUkeXEliw5hS2lQwzc8bJiYQJssa2fPKy8kivgcr5PuoeQLwxaBqz_sWvnvfFtBzC0wFsQ_B3ZMNGLhguQ78kGph6acRJ_L8nHnHcATIAQH8glG-TIJYgNeflzTCl6Z12ITcGS9PZoU3Q5_jvUkXcBM51RJxee6YrB6lDoFgumaI7G10-d6RoL1rE9aE9vOa2Ifo7B5VKvlubKlvoMtLaHvMZU09SFrZtdiSl_IheL9hk_n88r8vTr5vH6trl_-H13_fO-MZ3oSyNHZMKAXYZ-mrHTqAc-s27peCe5nHrTGTHJYcJRoO2ZtHwBO87Wco0WJ8OvyPfX3jXV5TAXtXfZoPc6YDxkNcAAALyvYPcKmhRzTrioNbm9TkfFQJ3Mq506mVcn8wq4quZr6Ou5_TDv0b5Fzqor8O0M6Gy0X6oL4_IbN04wMZD8P_4Wkjo</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>70700036</pqid></control><display><type>article</type><title>Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors</title><source>ScienceDirect Journals</source><creator>KEITH, John M ; GOMEZ, Leslie A ; BARBIER, Ann J ; WILSON, Sandy J ; BOGGS, Jamin D ; LORD, Brian ; MAZUR, Curt ; ALUISIO, Leah ; LOVENBERG, Timothy W ; CARRUTHERS, Nicholas I</creator><creatorcontrib>KEITH, John M ; GOMEZ, Leslie A ; BARBIER, Ann J ; WILSON, Sandy J ; BOGGS, Jamin D ; LORD, Brian ; MAZUR, Curt ; ALUISIO, Leah ; LOVENBERG, Timothy W ; CARRUTHERS, Nicholas I</creatorcontrib><description>A series of novel and potent 6-heteroaryl-pyrrolidino-tetrahydroisoquinolines with dual histamine H(3) antagonist/serotonin transporter inhibitor activity is described. In vitro and in vivo data are discussed.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2007.03.043</identifier><identifier>PMID: 17583504</identifier><language>eng</language><publisher>Oxford: Elsevier</publisher><subject>Animals ; Biological and medical sciences ; Blood-Brain Barrier ; Histamine H1 Antagonists - chemistry ; Histamine H1 Antagonists - pharmacology ; Medical sciences ; Mice ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Pharmacology. Drug treatments ; Pyrrolidines - chemistry ; Pyrrolidines - pharmacology ; Receptors, Histamine H3 - drug effects ; Serotonin Plasma Membrane Transport Proteins - drug effects ; Serotoninergic system ; Structure-Activity Relationship ; Tetrahydroisoquinolines - chemistry ; Tetrahydroisoquinolines - pharmacology</subject><ispartof>Bioorganic & medicinal chemistry letters, 2007-08, Vol.17 (15), p.4374-4377</ispartof><rights>2008 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c246t-58e14c0df769be2aea73b12f23253596c2c49579e84ed615d3f0d8bdd3aede9c3</citedby><cites>FETCH-LOGICAL-c246t-58e14c0df769be2aea73b12f23253596c2c49579e84ed615d3f0d8bdd3aede9c3</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=18909105$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17583504$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>KEITH, John M</creatorcontrib><creatorcontrib>GOMEZ, Leslie A</creatorcontrib><creatorcontrib>BARBIER, Ann J</creatorcontrib><creatorcontrib>WILSON, Sandy J</creatorcontrib><creatorcontrib>BOGGS, Jamin D</creatorcontrib><creatorcontrib>LORD, Brian</creatorcontrib><creatorcontrib>MAZUR, Curt</creatorcontrib><creatorcontrib>ALUISIO, Leah</creatorcontrib><creatorcontrib>LOVENBERG, Timothy W</creatorcontrib><creatorcontrib>CARRUTHERS, Nicholas I</creatorcontrib><title>Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>A series of novel and potent 6-heteroaryl-pyrrolidino-tetrahydroisoquinolines with dual histamine H(3) antagonist/serotonin transporter inhibitor activity is described. In vitro and in vivo data are discussed.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Blood-Brain Barrier</subject><subject>Histamine H1 Antagonists - chemistry</subject><subject>Histamine H1 Antagonists - pharmacology</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Pharmacology. Drug treatments</subject><subject>Pyrrolidines - chemistry</subject><subject>Pyrrolidines - pharmacology</subject><subject>Receptors, Histamine H3 - drug effects</subject><subject>Serotonin Plasma Membrane Transport Proteins - drug effects</subject><subject>Serotoninergic system</subject><subject>Structure-Activity Relationship</subject><subject>Tetrahydroisoquinolines - chemistry</subject><subject>Tetrahydroisoquinolines - pharmacology</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><recordid>eNpFkL1uHCEURlEUK944eYEUEU3SzeQywPyUkeXEliw5hS2lQwzc8bJiYQJssa2fPKy8kivgcr5PuoeQLwxaBqz_sWvnvfFtBzC0wFsQ_B3ZMNGLhguQ78kGph6acRJ_L8nHnHcATIAQH8glG-TIJYgNeflzTCl6Z12ITcGS9PZoU3Q5_jvUkXcBM51RJxee6YrB6lDoFgumaI7G10-d6RoL1rE9aE9vOa2Ifo7B5VKvlubKlvoMtLaHvMZU09SFrZtdiSl_IheL9hk_n88r8vTr5vH6trl_-H13_fO-MZ3oSyNHZMKAXYZ-mrHTqAc-s27peCe5nHrTGTHJYcJRoO2ZtHwBO87Wco0WJ8OvyPfX3jXV5TAXtXfZoPc6YDxkNcAAALyvYPcKmhRzTrioNbm9TkfFQJ3Mq506mVcn8wq4quZr6Ou5_TDv0b5Fzqor8O0M6Gy0X6oL4_IbN04wMZD8P_4Wkjo</recordid><startdate>20070801</startdate><enddate>20070801</enddate><creator>KEITH, John M</creator><creator>GOMEZ, Leslie A</creator><creator>BARBIER, Ann J</creator><creator>WILSON, Sandy J</creator><creator>BOGGS, Jamin D</creator><creator>LORD, Brian</creator><creator>MAZUR, Curt</creator><creator>ALUISIO, Leah</creator><creator>LOVENBERG, Timothy W</creator><creator>CARRUTHERS, Nicholas I</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>20070801</creationdate><title>Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors</title><author>KEITH, John M ; GOMEZ, Leslie A ; BARBIER, Ann J ; WILSON, Sandy J ; BOGGS, Jamin D ; LORD, Brian ; MAZUR, Curt ; ALUISIO, Leah ; LOVENBERG, Timothy W ; CARRUTHERS, Nicholas I</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c246t-58e14c0df769be2aea73b12f23253596c2c49579e84ed615d3f0d8bdd3aede9c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2007</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Blood-Brain Barrier</topic><topic>Histamine H1 Antagonists - chemistry</topic><topic>Histamine H1 Antagonists - pharmacology</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Pharmacology. Drug treatments</topic><topic>Pyrrolidines - chemistry</topic><topic>Pyrrolidines - pharmacology</topic><topic>Receptors, Histamine H3 - drug effects</topic><topic>Serotonin Plasma Membrane Transport Proteins - drug effects</topic><topic>Serotoninergic system</topic><topic>Structure-Activity Relationship</topic><topic>Tetrahydroisoquinolines - chemistry</topic><topic>Tetrahydroisoquinolines - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>KEITH, John M</creatorcontrib><creatorcontrib>GOMEZ, Leslie A</creatorcontrib><creatorcontrib>BARBIER, Ann J</creatorcontrib><creatorcontrib>WILSON, Sandy J</creatorcontrib><creatorcontrib>BOGGS, Jamin D</creatorcontrib><creatorcontrib>LORD, Brian</creatorcontrib><creatorcontrib>MAZUR, Curt</creatorcontrib><creatorcontrib>ALUISIO, Leah</creatorcontrib><creatorcontrib>LOVENBERG, Timothy W</creatorcontrib><creatorcontrib>CARRUTHERS, Nicholas I</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>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>KEITH, John M</au><au>GOMEZ, Leslie A</au><au>BARBIER, Ann J</au><au>WILSON, Sandy J</au><au>BOGGS, Jamin D</au><au>LORD, Brian</au><au>MAZUR, Curt</au><au>ALUISIO, Leah</au><au>LOVENBERG, Timothy W</au><au>CARRUTHERS, Nicholas I</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2007-08-01</date><risdate>2007</risdate><volume>17</volume><issue>15</issue><spage>4374</spage><epage>4377</epage><pages>4374-4377</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>A series of novel and potent 6-heteroaryl-pyrrolidino-tetrahydroisoquinolines with dual histamine H(3) antagonist/serotonin transporter inhibitor activity is described. In vitro and in vivo data are discussed.</abstract><cop>Oxford</cop><pub>Elsevier</pub><pmid>17583504</pmid><doi>10.1016/j.bmcl.2007.03.043</doi><tpages>4</tpages></addata></record>
fulltext	fulltext
identifier	ISSN: 0960-894X
ispartof	Bioorganic & medicinal chemistry letters, 2007-08, Vol.17 (15), p.4374-4377
issn	0960-894X 1464-3405
language	eng
recordid	cdi_proquest_miscellaneous_70700036
source	ScienceDirect Journals
subjects	Animals Biological and medical sciences Blood-Brain Barrier Histamine H1 Antagonists - chemistry Histamine H1 Antagonists - pharmacology Medical sciences Mice Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Pyrrolidines - chemistry Pyrrolidines - pharmacology Receptors, Histamine H3 - drug effects Serotonin Plasma Membrane Transport Proteins - drug effects Serotoninergic system Structure-Activity Relationship Tetrahydroisoquinolines - chemistry Tetrahydroisoquinolines - pharmacology
title	Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors
url	http://sfxeu10.hosted.exlibrisgroup.com/loughborough?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-07T10%3A05%3A11IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Pyrrolidino-tetrahydroisoquinolines%20bearing%20pendant%20heterocycles%20as%20potent%20dual%20H3%20antagonist%20and%20serotonin%20transporter%20inhibitors&rft.jtitle=Bioorganic%20&%20medicinal%20chemistry%20letters&rft.au=KEITH,%20John%20M&rft.date=2007-08-01&rft.volume=17&rft.issue=15&rft.spage=4374&rft.epage=4377&rft.pages=4374-4377&rft.issn=0960-894X&rft.eissn=1464-3405&rft_id=info:doi/10.1016/j.bmcl.2007.03.043&rft_dat=%3Cproquest_cross%3E70700036%3C/proquest_cross%3E%3Cgrp_id%3Ecdi_FETCH-LOGICAL-c246t-58e14c0df769be2aea73b12f23253596c2c49579e84ed615d3f0d8bdd3aede9c3%3C/grp_id%3E%3Coa%3E%3C/oa%3E%3Curl%3E%3C/url%3E&rft_id=info:oai/&rft_pqid=70700036&rft_id=info:pmid/17583504&rfr_iscdi=true