The neuroprotective agent MS-153 stimulates glutamate uptake.

We investigated the effect of (R)-(-)-5-methyl-1-nicotinoyl-2-pyrazoline (MS-153), a novel neuroprotective agent, on L-[3H]glutamate uptake through GLT-1, a Na(+)/K(+)-dependent glial glutamate transporter, expressed in COS-7 cells. MS-153 (1-100 microM) accelerated the L-[3H]glutamate uptake through GLT-1 in a concentration-dependent and time-dependent manner. Eadie-Hofstee analysis revealed that MS-153 significantly decreased the K(m) of the glutamate uptake by COS-7 cells expressing GLT-1.

Antiaggregatory, antithrombotic effects of MS-180, a novel platelet glycoprotein IIb/IIIa receptor antagonist.

The antiaggregatory and antithrombotic effects of (S)-(-)-ethyl[6-[4-(morpholinoformimidoyl)benzamido]-3,4-dihydro-2 H-1-benzo-pyran-3-yl]acetate hydrochloride (MS-180), a novel platelet glycoprotein IIb/IIIa receptor antagonist, were investigated. Ma-HCl, (S)-(-)-[6-[4-(Morpholinoformimidoyl)benzamido]-3,4-dihydro-2H-1-b enzopyran-3-yl]acetic acid hydrochloride, the hydrochloride salt of Ma (active metabolite), inhibited the binding of fibrinogen to immobilized human glycoprotein IIb/III receptor with an IC50 value of 0.12+/-0.

Respiratory effects of halothane and AMPA receptor antagonist synergy in rats.

The influence of N-methyl-D-aspartate (NMDA) or alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA) receptor antagonists in combination with halothane anaesthesia on the respiratory system was investigated. Under 1.5% halothane anaesthesia, respiratory parameters including respiratory rate, minute volume, tidal volume, inspiratory and expiratory duration were measured before and after drug administration in rats.

Inclusion of trithia[5]heterohelicene by various serum albumins. An effective probe for chiral discrimination.

Racemic 2-hydroxymethyltrithia[5]heterohelicene (2-HT), which has a labile helical structure was incorporated into serum albumins of nine species in 1% ethanolic aqueous solution, giving 1:1 complexes which exhibited induced circular dichroism spectra with species specificity. The application of 2-HT to bovine serum as a probe for chiral recognition revealed that the serum itself manifested an apparent chiral discrimination between enantiomers of 2-HT.

Cerebroprotective effects of a novel pyrazoline derivative, MS-153, on focal ischemia in rats.

MS-153 ((R)-(-)-5-methyl-1-nicotinoyl-2-pyrazoline) is a novel pyrazoline compound that has potent cerebroprotective effects in the rat focal cerebral ischemia model. Middle cerebral artery (MCA) occlusion in rats allows detailed assessment of both functional and morphological sequelae of brain infarct. Using this model, we evaluated the cerebroprotective effects of MS-153.