Radiochemical Synthesis and Binding Characteristics of a New Thioperamide Derivative as a Potent Histamine H3 Antagonist.
نویسندگان
چکیده
منابع مشابه
Thioperamide, antagonist of histamine H3 receptors, increases brain production of kynurenic acid
Brain histamine plays the role of neuromodulator and neurotransmitter in a variety of physiological and pathological processes. Kynurenic acid (KYNA) is an antagonist of the glycine site within the N-methyl-D-aspartate (NMDA) receptor complex, and of nicotinic α7 receptors in the brain of mammals. Here, we report that thioperamide, H3 receptor antagonist/inverse agonist is capable of increasing...
متن کاملPharmacological properties and procognitive effects of ABT-288, a potent and selective histamine H3 receptor antagonist.
Blockade of the histamine H(3) receptor (H(3)R) enhances central neurotransmitter release, making it an attractive target for the treatment of cognitive disorders. Here, we present in vitro and in vivo pharmacological profiles for the H(3)R antagonist 2-[4'-((3aR,6aR)-5-methyl-hexahydro-pyrrolo[3,4-b]pyrrol-1-yl)-biphenyl-4-yl]-2H-pyridazin-3-one (ABT-288). ABT-288 is a competitive antagonist w...
متن کاملNeurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist.
Ciproxifan, i.e., cyclopropyl-(4-(3-1H-imidazol-4-yl)propyloxy) phenyl) ketone, belongs to a novel chemical series of histamine H3-receptor antagonists. In vitro, it behaved as a competitive antagonist at the H3 autoreceptor controlling [3H]histamine release from synaptosomes and displayed similar Ki values (0.5-1.9 nM) at the H3 receptor controlling the electrically-induced contraction of guin...
متن کاملa fundamental study of "histiriographic metafiction", and "literary genres", as introduced in "new historical philosophy", and tracing them in the works of julian barnes.
abstract a fundamental study of “historio-graphic metafiction” and “literary genres”, as introduced in “new historical philosophy”, and tracing them in the works of julian barnes having studied the two novels, the porcupine and arthur & george, by julian barnes, the researcher has applied linda hutcheon’s historio-graphic metafictional theories to them. the thesis is divided into five cha...
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ژورنال
عنوان ژورنال: Japanese Journal of Pharmacology
سال: 1993
ISSN: 0021-5198
DOI: 10.1016/s0021-5198(19)51259-8