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Capsazepine partially inhibits neurally mediated gastric mucus secretion following activation of protease-activated receptor 2. 2002

Atsufumi Kawabata, and Mitsuhiro Kinoshita, and Ryotaro Kuroda, and Kazuaki Kakehi
Faculty of Pharmaceutical Sciences, Kinki University, Higashi-Osaka, Japan. kawabata@phar.kindai.ac.jp

1. Protease-activated receptor 2 (PAR2), present in capsaicin-sensitive sensory neurons, induces gastric mucus secretion and mucosal cytoprotection. 2. We studied the possible cross-talk between PAR2 and vanilloid receptor 1 (VR1). The VR1 antagonist capsazepine partially inhibited the PAR2-mediated increase in gastric mucus secretion. 3. Thus, activation of VR1 is responsible, at least in part, for the neurally mediated mucosal cytoprotection following activation of PAR2.

UI MeSH Term Description Entries
D008297 Male Males
D009433 Neural Inhibition The function of opposing or restraining the excitation of neurons or their target excitable cells. Inhibition, Neural
D009475 Neurons, Afferent Neurons which conduct NERVE IMPULSES to the CENTRAL NERVOUS SYSTEM. Afferent Neurons,Afferent Neuron,Neuron, Afferent
D011955 Receptors, Drug Proteins that bind specific drugs with high affinity and trigger intracellular changes influencing the behavior of cells. Drug receptors are generally thought to be receptors for some endogenous substance not otherwise specified. Drug Receptors,Drug Receptor,Receptor, Drug
D002211 Capsaicin An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS. 8-Methyl-N-Vanillyl-6-Nonenamide,Antiphlogistine Rub A-535 Capsaicin,Axsain,Capsaicine,Capsicum Farmaya,Capsidol,Capsin,Capzasin,Gelcen,Katrum,NGX-4010,Zacin,Zostrix,8 Methyl N Vanillyl 6 Nonenamide,NGX 4010,NGX4010
D005753 Gastric Mucosa Lining of the STOMACH, consisting of an inner EPITHELIUM, a middle LAMINA PROPRIA, and an outer MUSCULARIS MUCOSAE. The surface cells produce MUCUS that protects the stomach from attack by digestive acid and enzymes. When the epithelium invaginates into the LAMINA PROPRIA at various region of the stomach (CARDIA; GASTRIC FUNDUS; and PYLORUS), different tubular gastric glands are formed. These glands consist of cells that secrete mucus, enzymes, HYDROCHLORIC ACID, or hormones. Cardiac Glands,Gastric Glands,Pyloric Glands,Cardiac Gland,Gastric Gland,Gastric Mucosas,Gland, Cardiac,Gland, Gastric,Gland, Pyloric,Glands, Cardiac,Glands, Gastric,Glands, Pyloric,Mucosa, Gastric,Mucosas, Gastric,Pyloric Gland
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D017208 Rats, Wistar A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain. Wistar Rat,Rat, Wistar,Wistar Rats
D044464 Receptor, PAR-2 A G-protein-coupled, proteinase-activated receptor that is expressed in a variety of tissues including ENDOTHELIUM; LEUKOCYTES; and the GASTROINTESTINAL TRACT. The receptor is activated by TRYPSIN, which cleaves off the N-terminal peptide from the receptor. The new N-terminal peptide is a cryptic ligand for the receptor. The uncleaved receptor can also be activated by the N-terminal peptide present on the activated THROMBIN RECEPTOR and by small synthetic peptides that contain the unmasked N-terminal sequence. PAR-2 Receptor,Proteinase Activated Receptor 2,PAR2 Receptor,Protease-Activated Receptor 2,Receptor, Trypsin,Trypsin Receptor,Trypsin Receptors,PAR 2 Receptor,Protease Activated Receptor 2,Receptor 2, Protease-Activated,Receptor, PAR 2,Receptor, PAR2,Receptors, Trypsin
D050916 TRPV Cation Channels A subgroup of TRP cation channels named after the vanilloid receptor. They are very sensitive to TEMPERATURE; hot spicy food, and CAPSAICIN. They contain a TRP domain (a five-turn amphipathic helix with an invariant TRYPTOPHAN) and ANKYRIN repeats. Selectivity for CALCIUM over SODIUM ranges from 3 to 100 fold. Capsaicin Receptor,Vanilloid Receptor,Capsaicin Receptors,Vanilloid Receptors,Cation Channels, TRPV,Channels, TRPV Cation,Receptor, Capsaicin,Receptor, Vanilloid,Receptors, Capsaicin,Receptors, Vanilloid

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