Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists.

Furan-2-carbohydrazides were found as orally active glucagon receptor antagonists. Starting from the hit compound 5, we successfully determined the structure activity relationships of a series of derivatives obtained by modifying the acidity of the phenol. We identified the ortho-nitrophenol as a good scaffold for glucagon receptor inhibitory activity.

Relationship between orthodontic expertise and perception of need for orthodontic treatment for mandibular protrusion in Japan.

The aims of this study were to investigate how the Peer Assessment Rating (PAR index) predicts the perceived need for orthodontic treatment of mandibular protrusion in Japanese subjects, and to elucidate whether the perceived need for treatment was affected by the raters' orthodontic expertise. The subjects were 110 dental students and 32 orthodontists. We showed them casts of 10 untreated mandibular protrusion cases and gave them a questionnaire in which they had to describe their perceptions of the orthodontic treatment needs using a 10-point visual analog scale (VAS).

Clinical effect of CO(2) laser in reducing pain in orthodontics.

Objective: To test the hypothesis that there is no difference in the pain associated with orthodontic force application after the application of local CO(2) laser irradiation to the teeth involved.

Materials And Methods: Separation modules were placed at the distal contacts of the maxillary first molars in 90 patients in this single-blinded study. In 60 of these patients (42 females and 18 males; mean age = 19.

Development of inhibitory synaptic transmission to the superior salivatory nucleus in rats.

The primary parasympathetic center of the submandibular and sublingual salivary glands is the superior salivatory (SS) nucleus, neurons of which receive excitatory (glutamatergic) and inhibitory (GABAergic and glycinergic) synaptic transmissions in rats. In the present study, to examine postnatal neural development, we focused on inhibitory transmission to the SS neurons in neonatal rats from postnatal day 2 (P2) to P14. Conventional and gramicidin-perforated whole-cell patch-clamp techniques were applied to the neurons in brainstem slices.

Stereospecific recognition of a spirosuccinimide type aldose reductase inhibitor (AS-3201) by plasma proteins: a significant role of specific binding by serum albumin in the improved potency and stability.

AS-3201 [(3R)-2'-(4-bromo-2-fluorobenzyl)spiro[pyrrolidine-3,4'(1'H)-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetrone] is a structurally novel and stereospecifically potent aldose reductase (AKR1B; EC 1.1.1.

Salivary flow rates during relaxing, clenching, and chewing-like movement with maxillary occlusal splints.

The purpose of this study was to test the hypothesis that the application of occlusal splints increases the diurnal salivary flow rate both in bruxism patients and in normal subjects. Salivary flow rates in 16 adult volunteers (8 bruxism patients and 8 sex- and age-matched control subjects) were measured with the spitting method. There was no significant difference in the salivary flow rate with or without splints between the control and bruxism groups.

Association between nocturnal bruxism and gastroesophageal reflux.

Study Objective: To examine the relationship between nocturnal bruxism and gastroesophageal reflux.

Design: Controlled descriptive study and double-blind, placebo-controlled, clinical study.

Setting: Portable pH monitoring, electromyography, and audio-video recordings were conducted during the night in the subjects' home.