Psychiatry related information on L 740093

• Locomotor activity induced by subcutaneous administration of MK-801 (0.15 mg/kg) was potentiated by intraperitoneal L-740,093 (0.3, 1 and 3 mg/kg) [1].

High impact information on L 740093

• RESULTS: Gastrin induced degradation of IkappaB-alpha and activation of NFkappaB, which was abolished by the selective gastrin receptor antagonist L-740,093 and the general PKC inhibitor GF109203X [2].
• An ex vivo binding assay in mice was used to investigate the interaction of L-740,093 with central CCK binding sites [3].
• Biological properties of the benzodiazepine amidine derivative L-740,093, a cholecystokinin-B/gastrin receptor antagonist with high affinity in vitro and high potency in vivo [3].
• These studies demonstrate that L-740,093 is the most potent and selective CCK-B antagonist yet described and that it has excellent central nervous system penetration [3].
• Carboxy-terminal extended gastrins induced histamine release which was inhibited by the gastrin/CCK(B) antagonist L-740,093, but had to be given in concentrations 100-fold higher than amidated gastrin-17 to produce comparable effects [4].

Chemical compound and disease context of L 740093

• The cholecystokinin antagonists L-740,093, L-365,260, LY-288513 and CI988, which are all selective for the cholecystokininB receptor subtype, were examined for their ability to modulate locomotor activity induced by the non-competitive N-methyl-D-aspartate receptor antagonists phencyclidine and dizocilpine maleate (MK-801) in habituated rats [1].

Biological context of L 740093

• L-740,093 bound with high affinity to guinea pig gastrin receptors in vitro (IC50 of 0.04 nM) [3].

Anatomical context of L 740093

• L-740,093 exhibited high affinity (IC50 0.49 nM) and selectivity (<50% displacement at CCK-A sites at 1 microM) for the human CCK-B receptor subtype as estimated from [125I]-CCK-8S displacement studies with membranes prepared from hCCK-B.CHO cells [5].
• A stable cell line expressing the human cholecystokinin-B receptor gene (hCCK-B.CHO) has been employed in an evaluation of the recently developed CCK-B receptor antagonist L-740,093 [5].

Associations of L 740093 with other chemical compounds

• 4. The structurally related benzodiazepines L-365,260, L-740,093, and YM022 are selective antagonists of the CCK-B receptor subtype [6].

Gene context of L 740093

• L-740,093, a new antagonist of the CCK-B receptor, potentiates the antinociceptive effect of morphine: electrophysiological and behavioural studies [7].
• Rat gastrin-17I (2.5 nmol/kg/hour) or gastrin-17I plus gastrin receptor antagonist, L-740,093 (2.0 mg/kg/hour), was injected intravenously into male Sprague-Dawley rats [8].
• When tested at 10 nM L-740,093 produced a modest rightward shift in the CCK-4 dose response curve, an effect which was accompanied by a small reduction (13%) in the maximum response to CCK-4 [5].

References