Fluorescent H Receptor Squaramide-Type Antagonists: Synthesis, Characterization, and Applications.

Fluorescence labeled ligands have been gaining importance as molecular tools, enabling receptor-ligand-binding studies by various fluorescence-based techniques. Aiming at red-emitting fluorescent ligands for the hHR, a series of squaramides labeled with pyridinium or cyanine fluorophores (-) was synthesized and characterized. The highest hHR affinities in radioligand competition binding assays were obtained in the case of pyridinium labeled antagonists - (p : 7.

Descriptive Cost-Effectiveness Analysis of a Counseling and Coordination Model in Psychosocial Care. Integration of Health Care and Social Rehabilitation.

Introduction: A psychosocial outreach clinic was established to offer counseling and coordination of healthcare and complementary services for persons with psychosocial and mental problems. The cost-effectiveness of these services was measured based on a pre-post comparison.

Methods: A prospective observational study was conducted with clients of the outreach clinic.

Cost evaluation of an innovative outreach clinic across social insurance codes in rural Northern Germany - A routine data analysis.

A community outreach clinic was established in 2013 in a rural part of Germany to counsel and better integrate patients with mental health disorders or clients with psychosocial problems into the healthcare and complementary social assistance system. In a pilot study, we aimed to evaluate the costs of the integration assistance system after the outreach clinic was opened, the number of visits and the trend in the costs of the social assistance system of the federal state. Anonymised secondary cost data were used to evaluate the costs associated with the integration assistance receivers before (2010-2012) and after the establishment of the outreach clinic (2013-2015).

[(3) H]UR-DE257: development of a tritium-labeled squaramide-type selective histamine H2 receptor antagonist.

A series of new piperidinomethylphenoxypropylamine-type histamine H2 receptor (H2 R) antagonists with different substituted "urea equivalents" was synthesized and characterized in functional in vitro assays. Based on these data as selection criteria, radiosynthesis of N-[6-(3,4-dioxo-2-{3-[3-(piperidin-1-ylmethyl)phenoxy]propylamino}cyclobut-1-enylamino)hexyl]-(2,3-(3) H2 )propionic amide ([(3) H]UR-DE257) was performed. The radioligand (specific activity: 63 Ci mmol(-1) ) had high affinity for human, rat, and guinea pig H2 R (hH2 R, Sf9 cells: Kd , saturation binding: 31 nM, kinetic studies: 20 nM).

Red-fluorescent argininamide-type NPY Y1 receptor antagonists as pharmacological tools.

Fluorescently labelled NPY Y(1) receptor (Y(1)R) ligands were synthesized by connecting pyrylium and cyanine dyes with the argininamide-type Y(1)R antagonist core structure by linkers, covering a wide variety in length and chemical nature, attached to the guanidine group. The most promising fluorescent probes had Y(1)R affinities (radioligand binding) and antagonistic activities (calcium assay) in the one- to two-digit nanomolar range. These compounds turned out to be stable under assay conditions and to be appropriate for the detection of Y(1)Rs by confocal microscopy in live cells.