PMID: 8583392Sep 1, 1995Paper

Pharmacological properties of 403U76, a new chemical class of 5-hydroxytryptamine- and noradrenaline-reuptake inhibitor

The Journal of Pharmacy and Pharmacology
R M FerrisB Cooper

Abstract

403U76 (5-chloro-[[2-[(dimethylamino)methyl]phenyl]thio]benzene- methanol hydrochloride) is a potent, competitive, inhibitor of 5-hydroxytryptamine (5-HT) and noradenaline reuptake into rat brain synaptosomes. Inhibition of 5-HT uptake in-vivo by 403U76 was demonstrated by potentiation of the behavioural effects of 5-hydroxytryptophan in rats and mice and blockade of p-induced depletion of 5-HT in rats. The firing of 5-HT-ergic dorsal raphe neurons in rats was decreased after intravenous administration of low doses of 403U76 as would be predicted for a 5-HT uptake inhibitor. 403U76 antagonized tetrabenazine-induced sedation, an effect associated with inhibitors of noradrenaline uptake, but not with inhibitors of 5-HT uptake. Thus 403U76 affects noradrenergic as well as 5-HT-ergic neurotransmission in-vivo. Potential anxiolytic activity was indicated by reductions in isolation-induced vocalizations in neonates after 403U76 treatment. Low intravenous doses of 403U76 were well tolerated and had no sustained cardiovascular effects. There were no deleterious behavioural side-effects at active doses. Effects observed on isolated tissues or transmitter receptors occurred only at very high concentrations and were pharmacologically unim...Continue Reading

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Oct 13, 2009·European Journal of Nuclear Medicine and Molecular Imaging·Ya-Yao HuangChyng-Yann Shiue
Jun 17, 1999·Il Farmaco·D DjurovićN Majkić-Singh
Feb 8, 2003·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·Grace G ShiueChyng-Yann Shiue
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Apr 3, 2009·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·Ya-Yao HuangChyng-Yann Shiue
Nov 29, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Jeffrey S Stehouwer, Mark M Goodman
Feb 28, 2003·Seminars in Nuclear Medicine·Hank F KungSeok Rye Choi
Oct 19, 2004·Radiologic Clinics of North America·Chyng-Yann Shiue, Michael J Welch
Jul 17, 2013·Nuclear Medicine and Biology·Laetitia LemoineHank F Kung
Dec 13, 2005·Bioorganic & Medicinal Chemistry Letters·Johnny VercouilliePatrick Emond

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