Interaction of Orally Administered 5-{3-[((25)-1,4-Benzodioxan-2-ylmethyl)amino]propoxy}-1,3-benzodioxole (MKC-242) with 5-HT1A Receptors in Rat Brain
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Effects of a benzodioxan derivative MKC-242 on the firing activity of the dorsal hippocampus CA1 pyramidal neurons in awake and urethane- anaesthetized rats: in vivo electrophysiological evidence for a 5-HT 1A agonistic property.
The aim of the present in vivo study was to determine whether a benzodioxan derivative MKC-242, (S)-5-[3-[(1,4-benzodioxan-2-ylmethyl)amino]propoxy]-1,3-benzodioxole hydrochloride, possesses an agonistic activity at postsynaptic serotonin (5-HT)1A receptors in the rat hippocampus when administered systemically. We examined the effects of acute administrations of MKC-242 on the firing activities...
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The aim of this work was to improve the oral bioavailability of a recently discovered, novel structural class of 5-HT1A receptor agonists: aryl-{[4-(6-R-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1 -yl-metha none. Incorporation of a fluorine atom in the beta-position to the amino function in the side chain led to analogues that exhibited, in general, enhanced and long-lasting 5-HT1A agonist a...
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BACKGROUND Intrathecal administration of 5-hydroxytryptamine (5-HT) is antinociceptive to noxious heat and electrical stimuli. The contributions of different receptor subtypes to the antinociceptive effects of 5-HT are controversial. The main reasons for this are the poor receptor subtype selectivity of some agonist drugs and the difficulty of restricting drug action to the spinal cord in some ...
متن کاملN′-(2-Hydroxy-3-methoxybenzylidene)-1,3-benzodioxole-5-carbohydrazide monohydrate
Single crystals of the title compound, C(16)H(14)N(2)O(5)·H(2)O, were obtained from a condensation reaction of 1,3-benzodioxole-5-carbohydrazide and 3-methoxy-salicylaldehyde in a 95% ethanol solution. The asymmetric unit consists of a Schiff base mol-ecule, which assumes an E configuration with respect to the C=N bond, and a water mol-ecule of crystallization. The dihedral angle between the tw...
متن کاملNative rat hippocampal 5-HT1A receptors show constitutive activity.
Previous studies have shown that human 5-hydroxytryptamine (5-HT)1A receptors stably expressed in transfected cell lines show constitutive G-protein activity, as revealed by the inhibitory effect of inverse agonists, such as spiperone, on basal guanosine-5'-O-(3-[35S]thio)-triphosphate ([35S]GTPgammaS) binding. In the present study, we evaluated the constitutive activity of native rat 5-HT1A re...
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ژورنال
عنوان ژورنال: Japanese Journal of Pharmacology
سال: 1997
ISSN: 0021-5198
DOI: 10.1016/s0021-5198(19)31428-3