Serotonin 3(5-HT3) receptor antagonist YM060.
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چکیده
منابع مشابه
MDL72222, a serotonin 5-HT3 receptor antagonist, blocks MDMA's ability to establish a conditioned place preference.
Methylenedioxymethamphetamine (MDMA) has previously been shown to produce a positive conditioned place preference (CPP) among rats. Here the effects of doses of a specific 5-HT3 antagonist, MDL72222, on MDMA's ability to produce a CPP were assessed. A dose of MDL72222 (0.03 mg/kg) blocked the establishment of a MDMA CPP. These results support the suggestions that compounds affecting the 5-HT3 r...
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D iabetic diarrhea is a troublesome gastrointestinal complication of diabetes. This condition persists for several weeks to months, and it frequently accompanies fecal incontinence. The cause of diabetic diarrhea is not fully understood, but autonomic neuropathy is thought to be an underlying mechanism (1). Parenteral somatostatin analog octreotide has been shown to be useful in the treatment o...
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YM060, (R)-5-[(1-methyl-3-indolyl)carbonyl]-4,5,6,7-tetrahydro-1H-benzimidazole hydrochloride, is a new serotonin (5HT)3-receptor antagonist. We examined the effects of YM060 on chemotherapeutic agent-, apomorphine- and copper sulfate-induced emesis. Intravenous YM060 potently prevented cisplatin (10 mg/kg, i.v.)-induced emesis with ED50 values of 0.06 (0.05-0.07) micrograms/kg, i.v. in ferrets...
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Our recently solved high-resolution structure of the serotonin 5-HT3 receptor (5-HT3R) delivered the first detailed structural insights for a mammalian pentameric ligand-gated ion channel. Based on this structure, we here performed a total of 2.8-μs all-atom molecular dynamics simulations to unravel at atomic detail how neurotransmitter binding on the extracellular domain induces sequential con...
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Serotonin (5-hydroxytryptamine, 5-HT), next to being an important neurotransmitter, recently gained attention as a key-regulator of pre- and postnatal development in the mammalian central nervous system (CNS). Several receptors for 5-HT are expressed in the developing brain including a ligand-gated ion channel, the 5-HT3 receptor. Over the past years, evidence has been accumulating that 5-HT3 r...
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ژورنال
عنوان ژورنال: Kagaku To Seibutsu
سال: 1993
ISSN: 0453-073X,1883-6852
DOI: 10.1271/kagakutoseibutsu1962.31.49