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N-Alkyldeoxynojirimycin derivatives with novel terminal tertiary amide substitution for treatment of bovine viral diarrhea virus (BVDV), Dengue, and Tacaribe virus infections.
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Novel N-alkyldeoxynojirimycins (NADNJs) with two hydrophobic groups attached to a nitrogen linker on the alkyl chain were designed. A novel NADNJ containing a terminal tertiary carboxamide moiety was discovered that was a potent inhibitor against BVDV. Further optimization resulted in a structurally
Rationale for the use of nicotinic acid and its amide in non-pellagrous diarrhea and psychoneurosis.
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Erucamide as a modulator of water balance: new function of a fatty acid amide.
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The aim of this study was to isolate a compound from blood plasma that inhibits intestinal diarrhea and that appears also to regulate fluid volumes in other organs. The isolation procedure included lipid extraction, liquid chromatography, and gas chromatography. The active substance was identified
Targeting fatty acid amide hydrolase and transient receptor potential vanilloid-1 simultaneously to modulate colonic motility and visceral sensation in the mouse: A pharmacological intervention with N-arachidonoyl-serotonin (AA-5-HT).
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BACKGROUND
Endocannabinoid anandamide (AEA) inhibits intestinal motility and visceral pain, but it may also be proalgesic through transient receptor potential vanilloid-1 (TRPV1). AEA is degraded by fatty acid amide hydrolase (FAAH). This study explored whether dual inhibition of FAAH and TRPV1
Optimization of benzoxazole-based inhibitors of Cryptosporidium parvum inosine 5'-monophosphate dehydrogenase.
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Cryptosporidium parvum is an enteric protozoan parasite that has emerged as a major cause of diarrhea, malnutrition, and gastroenteritis and poses a potential bioterrorism threat. C. parvum synthesizes guanine nucleotides from host adenosine in a streamlined pathway that relies on inosine
Nicotinamide inhibits HIV-1 in both acute and chronic in vitro infection.
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HIV-1 infected patients can manifest a number of poorly understood conditions including dermatitis, dementia, and diarrhea. These conditions are in some ways suggestive of pellagra, the syndrome associated with niacin depletion. We demonstrate here that nicotinamide, the amide form of niacin,
A phase 2 study of the cytotoxic immunoconjugate CMB-401 (hCTM01-calicheamicin) in patients with platinum-sensitive recurrent epithelial ovarian carcinoma.
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The compound CMB-401 is an immunoconjugate consisting of the monoclonal antibody (MAb) hCTM01 directed against polymorphic epithelial mucin covalently bound to the cytotoxic antibiotic calicheamicin by an amide linker. We evaluated CMB-401 as monotherapy for the treatment of recurrent
Genetic variation in endocannabinoid metabolism, gastrointestinal motility, and sensation.
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Cannabinoid agonist inhibits gastrointestinal motility. The endocannabinoid, anandamide, is inactivated by fatty acid amide hydrolase (FAAH). A single nucleotide polymorphism in the human FAAH gene (C385A) reduces FAAH expression. Our aim was to evaluate associations between FAAH genotype variation
Simultaneous erythema nodosum and erythema multiforme after local lidocaine injection.
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OBJECTIVE
To report a case of simultaneous erythema nodosum and erythema multiforme after local lidocaine injection.
METHODS
A 33-year-old female experienced coexisting erythema nodosum and erythema multiforme after lidocaine spray was used for upper gastrointestinal endoscopy. The reaction was
NUTRITIONAL CYTOPENIA IN MONKEYS RECEIVING THE GOLDBERGER DIET.
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Experiments are reported upon young rhesus monkeys which were given a diet essentially the same as the Goldberger black tongue-producing diet, supplemented in various ways. Those receiving the unsupplemented diet developed the syndrome characterized by leucopenia, anemia, gingivitis, diarrhea, and
Pre-treatment with a PKC or PKA inhibitor prevents the development of morphine tolerance but not physical dependence in mice.
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We previously demonstrated that intracerebroventricular (i.c.v.) administration of protein kinase C (PKC) or protein kinase A (PKA) inhibitors reversed morphine antinociceptive tolerance in 3-day morphine-pelleted mice. The present study aimed at evaluating whether pre-treating mice with a PKC or
Exploration of the GM1 receptor-binding site of heat-labile enterotoxin and cholera toxin by phenyl-ring-containing galactose derivatives.
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Cholera toxin (CT) and the closely related heat-labile enterotoxin of Escherichia coli (LT) are responsible for numerous cases of diarrhea worldwide, leading to considerable morbidity and mortality. The B subunits of these heterohexameric AB(5) toxins form a pentameric arrangement which is
Is glucagon-like peptide 1 an incretin hormone?
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Glucagon-like peptide-1 (GLP-1) was predicted, based on the proglucagon gene sequence. It is synthesised by specific post-translational processing in L cells (lower intestine) and secreted mainly as "truncated" GLP-1 [7-36 amide] in response to nutrient ingestion. Glucagon-like peptide-1 stimulates
Effect of dinitolmide intercalated into Montmorillonite on E. tenella infection in chickens.
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To enhance the anti-coccidial effect of dinitolmide and reduce its residual, the dinitolmide/MMT compounds were synthesized by the method of solution intercalation via dinitolmide intercalated into Na + -montmorillonite (Na + -MMT). The structure of compounds was characterized by X-ray diffraction
THE NATURAL OCCURRENCE OF RIBOFLAVIN DEFICIENCY IN THE EYES OF DOGS.
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In four dogs, the diarrhea, increased salivation and mucous membrane lesions characteristic of blacktongue were relieved within 24 hours following the administration of 150 mgs nicotinic amide, whereas the lacrimation, photophobia and extreme injection of the eye vessels did not diminish. These
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