Human α-calcitonin gene-related peptide-(8–37) alone (up to doses of 30 nmol kg−1 min−1) had no significant effects on blood pressure, heart rate or common or internal carotid haemodynamics, although it caused significant, reversible, inhibition of the hypotensive, tachycardic, and common and ...

Axonal flow of motoneurones was blocked in the sciatic nerve by the application of vinblastine at a low concentration (100 μM) not considered likely to cause axonal degeneration. The number of motoneurons expressing α-calcitonin gene-related peptide (CGRP) mRNA was significantly increased by v...

Kainic acid (KA) is an excitatory and neurotoxic substance. The role of α-calcitonin gene-related peptide (α-CGRP) in the regulation of KA-induced hippocampal neuronal cell death was investigated in the present study. The intracerebroventricular (i.c.v.) administration with KA (0.07 μg) incre...

Human alpha-CGRP(8-37), a 30 amino acid peptide, is a selective antagonist of the calcitonin gene-related peptide receptor. CGRP is a 37-amino acid peptide that exists in two forms, denoted alpha- and beta-CGRP. Human alpha-CGRP is widely distributed throughout the peripheral and central nervous...

In this study we have analysed the expression of the genes for both α-type and β-type calcitonin gene-related peptide (CGRP) during postnatal development of the rat brain and compared it with the expression of CGRP-like immunoreactivity. At birth both α-type and β-type CGRP messenger RNA wer...

Spinal and cranial motoneurons express alpha- and beta-calcitonin gene-related peptide (CGRP) mRNAs constitutively at variable ratios, and these two mRNAs are differentially regulated following axotomy in spinal, facial, and hypoglossal motoneurons. The purpose of this study was to investigate t...

The neuropeptide, α-calcitonin gene-related peptide (α-CGRP), is expressed from sensory nerves that innervate fat. However, how α-CGRP may act in adipose tissue is unclear. Using 3T3-L1 adipocytes we observed that rat α-CGRP (rα-CGRP) evoked either a biphasic or monophasic reduction in intr...

An efficient and convenient synthesis of both enantiomers of pipecolic acid has been developed using the intramolecular cyclization of 2-amino-6-bromohexanoic acid under mild conditions.

Piperazic acid, a non-proteinogenic amino acid, found in complex secondary metabolites and peptide natural substances, has shown down regulation of Gli1 expression in Hedgehog signaling pathway in cell based assays. Further structure activity relationship study indicated that amide derivatives o...

A simple and rapid gas chromatographic method is described for the simultaneous determination of protein and non-protein amino acids present in aqueous samples. The amino acids were converted into their N(O,S)-isobutoxycarbonyl methyl ester derivatives and measured by gas chromatography7 equippe...

Background: Ramosetron, a new specific 5-hydroxytryptamine3 (5HT3)-receptor antagonist, is 58 times more potent than granisetron, and its antiemetic effect lasts 10.7 times longer than that of granisetron in ferrets treated with cisplatin.Objective: This study was undertaken to compare the durat...

ObjectiveThyroidectomy is associated with a high incidence of postoperative nausea and vomiting (PONV), ranging from 60% to 84%. We conducted this study to compare the antiemetic effects and safety of granisetron 20 μg/kg and ramosetron 4 μg/kg in patients undergoing elective thyroidectomy und...

We examined the effect of ramosetron, a potent serotonin (5-HT)3-receptor antagonist for irritable bowel syndrome with diarrhea, on conditioned fear stress (CFS)-induced defecation and normal (non-stressed) defecation in rats and compared ramosetron with the antidiarrheal agent loperamide and th...

We examined the pharmacological profile of ramosetron, a 5-HT3-receptor antagonist for irritable bowel syndrome with diarrhea, comparing it with those of other 5-HT3-receptor antagonists, alosetron and cilansetron, and the anti-diarrheal agent loperamide. Ramosetron showed high affinity for clon...

Background: Chemotherapeutic drugs used to treat cancer may cause nausea and emesis by inducing the release of 5-hydroxytryptamine (5-HT) in the small intestine. Blockage of 5-HT3 receptors in the small intestine by 5-HT3-receptor antagonists might prevent the nausea and vomiting associated with...

Irritable bowel syndrome (IBS) and functional dyspepsia (FD) are both functional gastrointestinal disorders and frequently co-occur in patients. While one cause of FD appears to be gastric hypersensitivity, whether the hypersensitivity is affected by IBS treatments remains unclear, given the lac...

Background & AimsPrevious studies have indicated that serotonin-3–receptor antagonists might have a sex-specific effect in patients with irritable bowel syndrome with diarrhea (IBS-D). Alosetron has been approved for the treatment of only women, and ramosetron has been approved for the treatmen...

Background & AimsRamosetron, a serotonin (5-hydroxytryptamine)-3 receptor antagonist with high selectivity, reduced stress-induced diarrhea and defecation caused by corticotropin-releasing hormone in rats. However, there have been no clinical trials of its effect in patients with diarrhea and ir...

Suppositories are the preferable dosage form for patients at home or experiencing nausea. Serotonin (5-HT3)-receptor antagonists are used to treat vomiting in intravenous or oral administration but not suppository form. Ramosetron hydrochloride (RAM) is a new 5-HT3 antagonist which effectively i...

Excited state spectral properties like fluorescence quantum yield, emission maxima and lifetime of 2-((7,8-dimethyl-1-oxo-2,3,4,9-tetrahydro-1H-carbazol-6-yl)oxy) acetic acid (DOTHCA) are markedly sensitive to polarity and the H-bonding ability of its immediate local environment. Inspired by the...