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M94A2238.TXT
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1994-10-25
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Document 2238
DOCN M94A2238
TI SDZ SID 791 (JM 3100): a mechanistically unique anti-HIV agent with
potent antiviral activity in vitro and in vivo.
DT 9412
AU Datema R; Sandoz Research Institute, Vienna, Austria.
SO Int Conf AIDS. 1994 Aug 7-12;10(1):35 (abstract no. 113A). Unique
Identifier : AIDSLINE ICA10/94370337
AB OBJECTIVE: To determine whether SID 791 has a potential as an anti-HIV
agent. RESULTS: SID 791 is a bicyclam blocking HIV replication in vitro
(including that of various clinical isolates in primary T-cells and
monocytes) by > 90% at concentrations of 1-10 nM. The in vitro
selectivity index is > 300,000. SID 791 blocks an uncoating/fusion step
in acute infections and--in chronically infected cells--the infectivity
of released particles. Decreased sensitivity of HIV-1, NL4.3, to the
compound develops slowly upon serial passaging in vitro (50 passages for
100-fold increase in IC50). In rats SID 791 has a long terminal
half-life (53h from blood cells) and a large volume of distribution. The
bicyclam binds to plasma proteins, but this does not effect its
antiviral activity. At non-toxic, once-daily, subcutaneous doses of > 1
mg/kg/day, SID 791 suppresses HIV-1 replication in intrathymically
infected SCID-hu (Thy/Liv) mice. CONCLUSION: The properties of SID 791
suggest a potential for antiviral therapy.
DE Animal Antiviral Agents/*PHARMACOLOGY/PHARMACOKINETICS Bicyclo
Compounds/PHARMACOLOGY Half-Life HIV/*DRUG EFFECTS/PHYSIOLOGY
HIV-1/DRUG EFFECTS In Vitro Mice Mice, Inbred Strains Protein
Binding Rats Virus Replication/*DRUG EFFECTS MEETING ABSTRACT
SOURCE: National Library of Medicine. NOTICE: This material may be
protected by Copyright Law (Title 17, U.S.Code).