Abstract：
:Prulifloxacin, a new thiazeto-quinoline derivative with antibiotic properties, was evaluated for cardiac risk both in vitro on the ether-à-go-go-related gene (HERG) K+ channel, and in vivo in the conscious dog monitored by telemetry. HERG current was measured from stably transfected human embryonic kidney (HEK) 293 cells by means of the patch-clamp technique. Application of AF 3013, the active metabolite of prulifloxacin, produced only minor reduction of HERG current amplitude (tail current=-40 mV), producing a maximum blockade of 12.3 +/- 3.3% at the highest concentration tested (335 microM). In comparison, ciprofloxacin also failed to produce a 50% inhibition of HERG current amplitude, although the maximum blockade was greater than that observed with prulifloxacin (47.6 +/- 1.9% at the highest concentration tested (335 microM). In contrast, moxifloxacin blocked HERG current amplitude with an IC50 value of 74.7 microM. Prulifloxacin had no effect on the QTc interval (Fridericia's) following 5 days of repeated oral administration (150 mg/kg/day) in the conscious dog monitored by telemetry. These findings suggest that prulifloxacin is not likely to prolong the QT interval.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Lacroix P,Crumb WJ,Durando L,Ciottoli GBdoi
10.1016/s0014-2999(03)02180-0keywords:
subject
Has Abstractpub_date
2003-09-05 00:00:00pages
69-72issue
1eissn
0014-2999issn
1879-0712pii
S0014299903021800journal_volume
477pub_type
杂志文章abstract：:Results from lesion studies show that selective damage to the temporal cortex or lateral entorhinal cortex impairs visual memory, whereas damage to the hippocampal region does not affect retention of a visual discrimination task. Major input pathways of the above structures use glutamate as neurotransmitter. The gluta...
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journal_title：European journal of pharmacology
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