A series of 13 2,2-disubstituted 3-(3,5-di-t-butyl-4-hydroxyphenyl)propan-1-ol derivatives have been prepared for evaluation as allosteric modulators of GABAB receptors. The activity (EC50, 4–7 μM) was greatest for the cyclohexyl and cyclopentyl analogues.
The pharmacological actions of 2,6-di-tert-butyl-4-(3-hydroxy-2-spiropentylpropyl)-phenol (BSPP), a putative presynaptic GABA(B) receptor modulator, were examined in electrically stimulated rat neocortical brain slices preloaded with [3H]-GABA or [3H]-glutamic acid. At 10 mmol/L, BSPP inhibited the release of [3H]-GABA in the presence of baclofen, but not that of [3H]-glutamic acid. This effect was sensitive to the GABA(B) receptor antagonist (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid (Sch 50911). Alone, BSPP had no effect on the release of [3H]-GABA or [3H]-glutamic acid. It is concluded that BSPP selectively potentiates the action of baclofen at GABA(B) autoreceptors, but not heteroreceptors and may be a useful ligand to discriminate between presynaptic GABA(B) receptor subtypes.
Introduction: Condylomata acuminata (CA) is human papillomavirus (HPV) infection, and one of the most common sexually transmitted disease, characterized with papul or papillomatous nodule in genital, perineum and anal, this disease can be asymptomatic as well. Some study proved sexually transmitted infection increases the incidence of Human immunodeficiency virus (HIV)/ acquired immunodeficiency syndrome (AIDS), and vice versa. Management of CA is Trichloroacetic acid (TCA), Tincture Podophyllin, and Electrocautery. This study aims to determine profile of condyloma acuminata in Dermatovenereology Outpatient Polyclinic Sanglah General Hospital Denpasar Bali period 2015-2017. A retrospective study during three years (2015-2017).Method: Data was obtained from medical record in Dermatovenereology Outpatient Polyclinic Sanglah General Hospital Denpasar Bali period 2015- 2017.Result: Total patient condyloma acuminata is 260 patients (5.48%), male is dominant 70 patients (67.31%), range age 12-35 years old (123%), there was 59 patient who infected with HIV (22.31%), with five pregnancy (1.92%). Most therapy is given trichloroacetic acid (TCA) (79.62%).Conclusion: Men suffered from condyloma acuminata more commonly than women, the most common treatment for this condition is trichloroacetic acid (TCA)
A series of 15 analogues of fendiline, and 34 derivatives of N-(3-phenylpropyl)-1-arylethylamine have been prepared for evaluation as positive allosteric modulators of GABAB receptors. The most active (EC50, 10 nM) was N-(3,3-diphenylpropyl)-1-(3-chloro-4-methoxyphenyl)ethylamine 6g.
Leprosy cases were still a common problem in Indonesia. Even though Bali was not considered as a high epidemic region in Indonesia, new cases of multibacillary leprosy continuously appeared. Vitamin D and its receptor, Vitamin D Receptor (VDR) has a role in modulation of immune system against M. leprae. This study aimed to find correlation between blood VDR serum level with bacterial index of multibacillary leprosy patients. Study design using cross-sectional model conducted in Sanglah General Hospital involving 47 multibacillary leprosy patients taken consecutively from July-October 2017. The level of VDR was examined by ELISA method. Characteristic of study participant is 29 (61.7%) male patients and 18 (38.3%) female patients. The mean age of the patient was 38.83 years. The mean VDR level was 27.80 pg/dl. Spearman correlation test found that there is a strong negative correlation (r = - 0.954; p < 0.001) between plasma level of VDR with bacterial index in multibacillary patients. This result suggests that the lower the VDR level, the higher bacterial index in leprosy patients. This study emphasizes more the role of Vitamin D and its receptor in immunomodulation especially in leprosy infection.
Gelatin is a biopolymer that can be generated from partially hydrolysis of collagen tissue. Extraction of gelatin consists of pretreatment and thermal extraction steps. Pretreatment process used sodium hydroxide to remove non collagen protein in matrix sample, sulfuric acid to demineralize, and citric acid to hydrolyse. The aim of this research was to study the effect of variation in concentrations of citric acid used in hydrolysis process on the gel strength and protein profile of gelatin products extracted from broiler chicken skin. The variation of the concentration citric acid used was 0.7 % (GA); 1.5% (GB); and 3.0% b/v (GC) respectively. The gel strength was measured using CT3 Texture Analyzer and protein profile of gelatin product was analyzed by SDS-PAGE method. The result showed that variation in concentration of citric acid used in the pretreatment process affected the gel strength and protein profile of gelatin product. Increasing the concentration of citric acid used in pretreatment process decreased the gel strength and molecular weight of gelatin product. Gel strength of each gelatin product was 265.81 g bloom for GA ; 196.05 g bloom for GB (1.5%), and 35.32 g bloom for GC (3.0 %) respectively. The electropherogram of both GA (0.7%) and GB (1.5%) revealed similar pattern of protein bands but the thickness of each bands was different. On the other hands, GC (3.0%) did not show any protein bands on the eletropherogram. The best gelatin product obtained in this experiment was found by using 0.7 % b/v citric acid (GA) in the pretreatment process. The gelatin product (GA) had characteristics as follows: yield 15.73%; moisture 7.30%; ash 0.51%; protein content 97.95%; fat content 0.62%; gel strength 265. 81 g bloom and thicker protein bands than others.
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