Comparative Evaluation of Exocrine Muscarinic Receptor Binding Characteristics and Inhibition of Salivation of Solifenacin in Mice(Pharmacology)

スポンサーリンク

概要

• 論文の詳細を見る

• Anticholinergic agents such as oxybutynin are clinically useful in the treatment of overactive bladder. However, oral administration of oxybutynin is frequently accompanied by side effects such as dry mouth, and novel bladder-selective anticholinergic agents such as solifenacin and tolterodine are now under development. The aim of the present study was to characterize the suppression of cholinergic salivation and exocrine muscarinic receptor binding of solifenacin on oral administration to mice in comparison with those of oxybutynin. Results showed that both drugs produced a significant increase in K_d values for specific [N-Methyl-^3H] scopolamine methyl chloride ([^3H]NMS) binding in the mouse submaxillary gland, compared with control values. However, this enhancement in K_d values was significantly smaller with solifenacin than with oxybutynin. Moreover, the inhibitory effect of solifenacin on pilocarpine-induced salivary secretion was significantly weaker than that of oxybutynin. Solifenacin dissociated more readily from muscarinic receptors in the mouse submaxillary gland than oxybutynin. In conclusion, the present study indicates that the weak suppression of cholinergic salivation by solifenacin compared with oxybutynin may be partially attributed to its relatively fast dissociation kinetics from exocrine muscarinic receptors.

• 社団法人日本薬学会の論文
• 2006-07-01

著者

• YAMADA Shizuo

  Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence (COE) Program, S

• Yamada Shizuo

  静岡県立大学 薬物動態学

• OKI Tomomi

  Department of Pharmacokinetics and Pharmacodynamics and COE Program in the 21st Century, School of P

• TAKEUCHI Chihiro

  Department of Pharmacokinetics and Pharmacodynamics and COE Program in the 21st Century, School of P

• Yamada S

  School Of Pharmaceutical Sciences And Coe21 University Of Shizuoka

• Yamada Shizuo

  Department Of Biophamacy School Of Pharmaceutical Sciences University Of Shizuoka

• Oki Tomomi

  Department Of Pharmacokinetics And Pharmacodynamics And Coe Program In The 21st Century School Of Ph

• Takeuchi Chihiro

  Department Of Chemical Engineering Nara National College Of Technology

• Takeuchi Chihiro

  Department Of Pharmacokinetics And Pharmacodynamics And Coe Program In The 21st Century School Of Ph

• Oki Tomomi

  Department of Biopharmacy, School of Pharmaceutical Sciences, University of Shizuoka

関連論文

• The Forefront for Novel Therapeutic Agents Based on the Pathophysiology of Lower Urinary Tract Dysfunction: Bladder Selectivity Based on In Vivo Drug–Receptor Binding Characteristics of Antimuscarinic Agents for Treatment of Overactive Bladder
• Pharmacologically Relevant Receptor Binding Characteristics and 5α-Reductase Inhibitory Activity of Free Fatty Acids Contained in Saw Palmetto Extract(Pharmacology)
• Effects of Dietary Ingredients on Function and Expression of P-Glycoprotein in Human Intestinal Epithelial Cells
• Structure-Activity Relationships of Receptor Binding of 1,4-Dihydropyridine Derivatives(Pharmacology)
• PJ-566 Influence of CYP2C9 Genotype on Pharmacokinetics and Pharmacodynamics of Benzbromarone(Cardiovascular pharmacology, basic/clinical-6, The 71st Annual Scientific Meeting of the Japanese Circulation Society)
• Comparative Evaluation of Exocrine Muscarinic Receptor Binding Characteristics and Inhibition of Salivation of Solifenacin in Mice(Pharmacology)
• Isolation and Pharmacological Characterization of Fatty Acids from Saw Palmetto Extract
• Highly Sensitive Measurement of P-Glycoprotein-Mediated Transport Activity in Caco-2 Cells
• Relationship between Development of Nephrotoxicity and Blood Concentration of Cyclosporine A in Bone-Marrow Transplanted Recipients Who Received the Continuous Intravenous Infusion(Pharmacology)
• Enhancement by Grapefruit Juice of Morphine Antinociception(Pharmacology)
• Antinociceptive Effects of St. John's Wort, Harpagophytum Procumbens Extract and Grape Seed Proanthocyanidins Extract in Mice(Pharmacology)
• The 5-HT_2 Receptor Antagonist Reduces Immobility of Mice Treated with the Atypical Antidepressant Mianserin in the Forced Swimming Test
• Development of a New Vasoactive Intestinal Peptide Analogue and Its Topical Administration System, Dry Powder Inhalation
• The Structural Biology of VIP (2) : Biological Activity of VIP is Dependent on its Secondary Structure
• Prediction of α_1-Adrenoceptor Occupancy in the Human Prostate from Plasma Concentrations of Silodosin, Tamsulosin and Terazosin to Treat Urinary Obstruction in Benign Prostatic Hyperplasia(Pharmacology)
• EFFECT OF PIPERIDINE AND RELATED ALICYCLIC AMINES ON NICOTINIC AND MUSCARINIC AGONIST BINDING SITES IN THE MAMMALIAN BRAIN
• P-253 DEVELOPMENT OF POTENT HISTAMINE H_3 AND/OR H_4 RECEPTOR ANTAGONISTS BY THE STEREOCHEMICAL DIVERSITY-ORIENTED CONFORMATIONAL RESTRICTION STRATEGY
• Synthesis of Conformationally Restricted Analogs of Baclofen, a Potent GABA_B Receptor Agonist, by the Introduction of a Cyclopropane Ring
• Low Dosage of Streptozotocin and Fat-diet Reduced Rat Liver Insulin Receptor Activities
• Evaluation on Rat Model of Metabolic Syndrome Induced by Fat-diet and Streptozotocin
• RATIONALE FOR THE USE OF α-BLOCKERS IN THE TREATMENT OF BENIGN PROSTATIC HYPERPLASIA (BPH)
• In Vivo Measurement of 1, 4-Dihydropyridine Receptors in Mesenteric Arteries of Spontaneously Hypertensive Rats and Effect of Nifedipine and Cilnidipine
• Muscarinic Receptor Binding Characteristics in Rat Tissues after Oral Administration of Oxybutynin and Propiverine
• Improvement in the Histopathology of Hearts from Cardiomyopathic BIO TO-2 Hamsters Following Long-Term Administration of Amlodipine and Cilnidipine
• Ex Vivo and in Vivo α_1-Adrenoceptor Binding Characteristics of a Novel α_-Adrenoceptor Antagonist, JTH-601,in Rat Tissues
• Comparative Study on Pharmacokinetics and in Vivoα_1-Adrenoceptor Binding of [^3H]Tamsulosin and [^3H]Prazosin in Rats
• Onset of Clinical Effects and Plasma Concentration of Fluvoxamine in Japanese Patients
• Effects of Cigarette Smoking and Cytochrome P450 2D6 Genotype on Fluvoxamine Concentration in Plasma of Japanese Patients
• Time-Dependent Induction of Hepatic Cytochrome P450 Enzyme Activity and mRNA Expression by Bilobalide in Rats
• Nasal Absorption of Digoxin in Rats
• Comparative Characterization of Lung Muscarinic Receptor Binding After Intratracheal Administration of Tiotropium, Ipratropium, and Glycopyrrolate
• HYPO-ACTIVITY OF LIVER INSULIN RECEPTOR IN GOTO-KAKISAKI RATS IMPROVED BY NATURAL VANADIUM CONTANING WATER(Endocrinology,Abstracts of papers presented at the 74^ Annual Meeting of the Zoological Society of Japan)
• Characterization of Specific[^3H]Nociceptin Binding in Rat Brain and Spinal Cord
• Effects of Repeated Morphine Treatment on the Antinociceptive Effects, Intestinal Absorption, and Efflux from Intestinal Epithelial Cells of Morphine
• THE INFLUENCE OF EXTRACELLULAR Ca2+ CONCENTRATION ON THE INHIBITORY EFFECT OF ADENOSINE IN GUINEA-PIG ILEAL LONGITUDINAL MUSCLES
• Pharmacokinetic and Pharmacodynamic Analysis of Acetylcholinesterase Inhibition by Distigmine Bromide in Rats
• Demonstration of Muscarinic and Nicotinic Receptor Binding Activities of Distigmine to Treat Detrusor Underactivity
• Benzbromarone Pharmacokinetics and Pharmacodynamics in Different Cytochrome P450 2C9 Genotypes
• COMPARATIVE STUDIES ON ANTI-NICOTINIC ACTION OF HEXAMETHONIUM, MECAMYLAMINE AND ADENOSINE IN THE GUINEA PIG ISOLATED ILEUM
• EFFECTS OF SURUGATOXIN ON ADRENERGICALLY INNERVATED TISSUES
• Higher order structure of Mucor miehei lipase and micelle size in cetyltrimethylammonium bromide reverse micellar system
• The Forefront for Novel Therapeutic Agents Based on the Pathophysiology of Lower Urinary Tract Dysfunction : Bladder Selectivity Based on In Vivo Drug-Receptor Binding Characteristics of Antimuscarinic Agents for Treatment of Overactive Bladder
• Comparative Characterization of Lung Muscarinic Receptor Binding After Intratracheal Administration of Tiotropium, Ipratropium, and Glycopyrrolate
• EFFECT OF PICROTOXIN ON ADRENAL CATECHOLAMINE SECRETION
• EFFECTS OF NICOTINIC RECEPTOR AGONISTS AND ANTAGONISTS ON UPTAKE AND EFFLUX OF 45Ca IN PERFUSED BOVINE ADRENAL GLANDS
• Effects of Functional Food Constituents on P-glycoprotein Activity in Caco-2 Cells Determined by a New Method Using Confocal Laser Scanning Microscopy
• Inhibitory Effects of Citrus Polymethoxyflavones, Nobiletin and its Analogues, on Acetylcholinesterase Activity
• A simple method to evaluate reactivity of acylglucuronides optimized for early stage drug discovery
• Beneficial Effects of Gosha-jinki-gan and Green Tea Extract in Rats With Chemical Cystitis
• Plasma Concentration and Occupation of Calcium (Ca2+) Antagonist Receptors of Amlodipine, a Long-acting Ca2+ Antagonist in SHR
• Muscarinic Receptor Binding of the Novel Radioligand, [3H]Imidafenacin in the Human Bladder and Parotid Gland
• Bladder Endothelin-1 Receptor Binding of Bosentan and Ambrisentan
• Alterations in Renal α and β-Adrenoceptors in Stroke-Prone Spontaneously Hypertensive Rats (SHRSP)
• Inhibition by chlorpromazine, metals and I-ascorbic acid of calcium-ATPase and magnesium-ATPase in bovine adrenal medullary microsomes.
• Reduced .ALPHA.2-adrenoceptor binding in lower brainstem of stroke-prone spontaneously hypertensive rats.
• Reciprocal alteration in cardiac and hypothalamic adrenergic receptors in spontaneously hypertensive rats
• Central Acetylcholine Receptors in Spontaneously Hypertensive Rats
• Effect of 2,4,6-trinitrophenol on catecholamine secretion from perfused bovine adrenal glands.
• Determination of the Effects of Green Tea Extract and Fruit Extracts on P-glycoprotein Activity in Caco-2 Cells by Using a New Method Involving Confocal Laser Scanning Microscopy

もっと見る 閉じる

スポンサーリンク