摘要:
Pharmaceutical compositions containing a cocktail of inhibitors of central stress nuclei are provided. The pharmaceutical compositions are useful for the prevention and treatment of a variety of conditions in mammals including humans, including anxiety and mood disorders such as depression.
摘要:
Disclosed herein are methods for quickly obtaining crude membranes from cells, including animal and plant cells. The methods include incubating cells in a buffer and forcing the cells through a filter that causes rupture of the cells, and then separating the resulting crude membranes from most cytosolic proteins.
摘要:
A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen, —OH, —O—C1-6 alkyl, ═O, or halogen; R2 is hydrogen, C(O)OR8, C6H5C(O)OR8, (CH2)1-2OH, CR9R10OH, C(O)O(CH2)0-2 aryl, C(O)NR9R10, C(O)SO2NR9R10, C6H5OR9, W—C(O)OR8, W—OR9, Y, or P(O)(OR9)(ORlO); R3 is hydrogen or —C1-6 alkyl; R4 is hydrogen, —OH or —C(O)OR9; R5 is hydrogen or deuterium; R6 and R7 are independently —C1-6 alkyl, fluoro-substituted —C1-6 alkyl, deutero-substituted —C1-6 alkyl or —(CH2)1-2R11, wherein any carbon atom of the fluoro-substituted —C1-6 alkyl is mono- or di-substituted with fluoro, and any carbon atom of the deutero-substituted —C1-6 alkyl is mono- or di-substituted with fluoro; R8, in each instance in which it occurs, is independently hydrogen, —C1-6 alkyl, or —(CH2)2N+(CH3)3; R9 and R10, in each instance in which they occur, are independently —C1-6 alkyl; R11 is —OH, —O—C1-6 alkyl, -0CD3, —OC(O)OC1-6 alkyl, —NH2, —C6H5, —N3, or W; W is an unsubslituted 5- or 6-raembered heteroaryl ring having 1, 2, or 3 nitrogen atoms, or a substituted 5- or 6-membered heteroaryl ring having 1, 2, or 3 nitrogen atoms that is mono- or di-substituted at any carbon atom with R6 or R7; Y is a 5- or 6-membered heterocyclic ring having 1, 2, 3 or 4 heteroatoms which are N, O, or S or stereoisomers thereof, or pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts of stereoisomers thereof, and methods of using the compounds for treating hypertension.
摘要:
A compound having the structure formula (I) or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
摘要:
The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.
摘要:
The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.
摘要:
An automatic packaging system is provided. The automatic packaging system includes a user interface, a selection-controlling module, an alarm-controlling module, and a package module. The user interface is for receiving user input. The selection-controlling module is for enabling and controlling a vibrating plate to select parts according to the user input, and generating a detection signal. The alarm-controlling module is for generating a package signal according to the detection signal and the user input. The package module is for packaging the parts according to the package signal.
摘要:
A test fixture for a printed circuit board (PCB) assembly (6) includes lower and upper units (2, 4). The PCB assembly includes a PCB (60) defining two spaced positioning holes (62), and a reinforcing plate (64) defining a plurality of openings (65). The lower unit includes a fixed base (20) and an adjustable support plate (21) defining a plurality of through holes (27). The upper unit includes a movable base (40), and a test plate (41) having two rows of identical columns (44) for engaging with the support plate. The support plate includes first and second positioning members (24, 25) supporting the PCB assembly. Support posts (272) are arranged on the fixed base for supporting a bottom of the PCB. The test plate includes two positioning pins (45) engaging in the positioning holes of the PCB, and a plurality of pressing posts (46) for pressing a top of the PCB.
摘要:
The present disclosure provides conjugates that comprise an insulin molecule conjugated via a conjugate framework to two or more separate ligands that each include a saccharide, wherein the framework, ligand, saccharide and insulin molecule optionally comprise a fatty chain (e.g., a C8-30 fatty chain), wherein when said insulin molecule is conjugated both to a C8-30 fatty chain and one or more separate ligands that each include a saccharide, said C8-30 fatty chain is linked to insulin molecule only, and wherein when the framework or ligand comprises a fatty chain the insulin molecule is conjugated to two or more separate ligands. In certain embodiments, a conjugate is characterized in that, when the conjugate is administered to a mammal, at least one pharmacokinetic (PK) and/or pharmacodynamic (PD) property of the conjugate is sensitive to serum concentration of a second saccharide. In certain embodiments, a conjugate is also characterized by having a protracted PK profile. Exemplary conjugates and sustained release formulations are provided in addition to methods of use and preparation.
摘要:
Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.
摘要翻译:胰岛素缀合物包含共价连接到具有两个臂的至少一个双齿连接体的胰岛素分子,每个臂独立地连接到包含糖的配体,并且其中至少一个连接体的配体是岩藻糖。 胰岛素缀合物显示药代动力学(PK)和/或药效学(PD)谱,其对糖类如葡萄糖或α-甲基甘露糖的全身浓度有反应,即使在不存在外源多价的情况下施用于有需要的受试者时 糖结合分子如Con A.