The pharmacology of sibutramine hydrochloride (BTS 54 524), a new antidepressant which induces rapid noradrenergic down-regulation

1. 1. Sibutramine hydrochloride (BTS 54 524) has been evaluated in a range of behavioural and biochemical models predictive of potential antidepressant activity. 2. 2. BTS 54 524 exhibited potent activity in acute behavioural tests for detecting potential antldepressants. 3. 3. BTS 54 524 rapidly an...

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Veröffentlicht in:Progress in neuro-psychopharmacology & biological psychiatry 1988, Vol.12 (5), p.575-584
Hauptverfasser: Buckett, W.Roger, Thomas, Peter C., Luscombe, Graham P.
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Thomas, Peter C.
Luscombe, Graham P.
description 1. 1. Sibutramine hydrochloride (BTS 54 524) has been evaluated in a range of behavioural and biochemical models predictive of potential antidepressant activity. 2. 2. BTS 54 524 exhibited potent activity in acute behavioural tests for detecting potential antldepressants. 3. 3. BTS 54 524 rapidly and potently down-regulated rat cortical β-adrenoceptors, being effective after only three days of oral administration. 4. 4. BTS 54 524 showed very little activity in a range of experiments predictive of side-effect potential. 5. 5. BTS 54 524 possesses a pharmacological profile which suggests that it may be a potent antidepressant with a rapid onset of action, and with a low potential for causing side-effects.
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Sibutramine hydrochloride (BTS 54 524) has been evaluated in a range of behavioural and biochemical models predictive of potential antidepressant activity. 2. 2. BTS 54 524 exhibited potent activity in acute behavioural tests for detecting potential antldepressants. 3. 3. BTS 54 524 rapidly and potently down-regulated rat cortical β-adrenoceptors, being effective after only three days of oral administration. 4. 4. BTS 54 524 showed very little activity in a range of experiments predictive of side-effect potential. 5. 5. 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Sibutramine hydrochloride (BTS 54 524) has been evaluated in a range of behavioural and biochemical models predictive of potential antidepressant activity. 2. 2. BTS 54 524 exhibited potent activity in acute behavioural tests for detecting potential antldepressants. 3. 3. BTS 54 524 rapidly and potently down-regulated rat cortical β-adrenoceptors, being effective after only three days of oral administration. 4. 4. BTS 54 524 showed very little activity in a range of experiments predictive of side-effect potential. 5. 5. BTS 54 524 possesses a pharmacological profile which suggests that it may be a potent antidepressant with a rapid onset of action, and with a low potential for causing side-effects.</description><subject>Adenylyl Cyclases - metabolism</subject><subject>Animals</subject><subject>Antidepressant</subject><subject>Antidepressive Agents, Tricyclic - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Blepharoptosis - drug therapy</subject><subject>Body Temperature Regulation - drug effects</subject><subject>BTS 54 524</subject><subject>Cerebral Cortex - metabolism</subject><subject>Cyclobutanes - pharmacology</subject><subject>Discrimination (Psychology) - drug effects</subject><subject>Female</subject><subject>Helplessness, Learned - physiopathology</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Monoamine Oxidase Inhibitors - pharmacology</subject><subject>Motor Activity - drug effects</subject><subject>Neuropharmacology</subject><subject>noradrenergic down-regulation</subject><subject>Norepinephrine - metabolism</subject><subject>Pharmacology. 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Psychiatry</subject><subject>Psychopharmacology</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Receptors, Adrenergic, beta - drug effects</subject><subject>Receptors, Adrenergic, beta - metabolism</subject><subject>Reserpine - pharmacology</subject><subject>sibutramine</subject><issn>0278-5846</issn><issn>1878-4216</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1988</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkUGLFDEQhYO4rOPqP1DIQWQXbE06SXf6IqyLusKCB-ceMkllOtKdtEm3w1z95ZtxhjnqKZV6XxXFewi9ouQ9JbT5QOpWVkLy5lrKm44QwqrmCVpRWdq8ps1TtDojz9DznH8WhjLCLtFlLQWVol2hP-se8NTrNGoTh7jd4-hw9ptlTnr0AXC_tymafojJW8DXn9Y_sOBY1PzmHdY4wA7rMBdpSpBzKfGu96bHPtjFQMZJT97iEJO2CQKkrTfYxl2oEmyXQc8-hhfowukhw8vTe4XWXz6v7-6rh-9fv93dPlSGSzZXHBzvJGtdazvaMr4R1HTAa-NqQsunox0YxxhzdFNUDoZ2HISRxjrdOXaF3h7XTin-WiDPavTZwDDoAHHJqpWNkITy_4JUEFFLSQrIj6BJMecETk3JjzrtFSXqEJE6-K8O_isp1d-IVFPGXp_2L5sR7HnolEnR35x0nY0eXNLB-HzGmoaRhtUF-3jEoHj220NS2XgIBqxPYGZlo__3HY-mX63J</recordid><startdate>1988</startdate><enddate>1988</enddate><creator>Buckett, W.Roger</creator><creator>Thomas, Peter C.</creator><creator>Luscombe, Graham P.</creator><general>Elsevier Inc</general><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>7TK</scope><scope>7X8</scope></search><sort><creationdate>1988</creationdate><title>The pharmacology of sibutramine hydrochloride (BTS 54 524), a new antidepressant which induces rapid noradrenergic down-regulation</title><author>Buckett, W.Roger ; Thomas, Peter C. ; Luscombe, Graham P.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c483t-4ef49837f7d91734b51c9e42cf201b51919ecf333f1b34b4ec194e5c8cdfa9f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1988</creationdate><topic>Adenylyl Cyclases - metabolism</topic><topic>Animals</topic><topic>Antidepressant</topic><topic>Antidepressive Agents, Tricyclic - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Blepharoptosis - drug therapy</topic><topic>Body Temperature Regulation - drug effects</topic><topic>BTS 54 524</topic><topic>Cerebral Cortex - metabolism</topic><topic>Cyclobutanes - pharmacology</topic><topic>Discrimination (Psychology) - drug effects</topic><topic>Female</topic><topic>Helplessness, Learned - physiopathology</topic><topic>In Vitro Techniques</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Monoamine Oxidase Inhibitors - pharmacology</topic><topic>Motor Activity - drug effects</topic><topic>Neuropharmacology</topic><topic>noradrenergic down-regulation</topic><topic>Norepinephrine - metabolism</topic><topic>Pharmacology. 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Sibutramine hydrochloride (BTS 54 524) has been evaluated in a range of behavioural and biochemical models predictive of potential antidepressant activity. 2. 2. BTS 54 524 exhibited potent activity in acute behavioural tests for detecting potential antldepressants. 3. 3. BTS 54 524 rapidly and potently down-regulated rat cortical β-adrenoceptors, being effective after only three days of oral administration. 4. 4. BTS 54 524 showed very little activity in a range of experiments predictive of side-effect potential. 5. 5. BTS 54 524 possesses a pharmacological profile which suggests that it may be a potent antidepressant with a rapid onset of action, and with a low potential for causing side-effects.</abstract><cop>Amsterdam</cop><pub>Elsevier Inc</pub><pmid>2851857</pmid><doi>10.1016/0278-5846(88)90003-6</doi><tpages>10</tpages></addata></record>
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1878-4216
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source MEDLINE; Elsevier ScienceDirect Journals Complete
subjects Adenylyl Cyclases - metabolism
Animals
Antidepressant
Antidepressive Agents, Tricyclic - pharmacology
Biological and medical sciences
Blepharoptosis - drug therapy
Body Temperature Regulation - drug effects
BTS 54 524
Cerebral Cortex - metabolism
Cyclobutanes - pharmacology
Discrimination (Psychology) - drug effects
Female
Helplessness, Learned - physiopathology
In Vitro Techniques
Male
Medical sciences
Mice
Monoamine Oxidase Inhibitors - pharmacology
Motor Activity - drug effects
Neuropharmacology
noradrenergic down-regulation
Norepinephrine - metabolism
Pharmacology. Drug treatments
Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
Rats
Rats, Inbred Strains
Receptors, Adrenergic, beta - drug effects
Receptors, Adrenergic, beta - metabolism
Reserpine - pharmacology
sibutramine
title The pharmacology of sibutramine hydrochloride (BTS 54 524), a new antidepressant which induces rapid noradrenergic down-regulation
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