5-HT Receptor Antagonists with an Unprecedented Selectivity Profile.

Selective leads: In this study, we generated a new series of serotonin 5-HT receptor antagonists. Their synthesis, structure-activity relationships, and selectivity profiles are reported. This series includes 5-HT antagonists with unprecedented high selectivity for the 5-HT receptor, setting the stage for lead optimization of drugs acting on a range of neurological targets.

Qualitative analysis of substance P, NK1-receptor and nerve ingrowth in substance P-treated ruptured rat Achilles tendon.

Substance P has a stimulating effect on fibroblast proliferation, collagen organization, and angiogenesis in ruptured and subsequently sutured rat Achilles tendon. This effect is also reflected in the biomechanical properties of the tendon. The aim of this study was to substantiate the effect of exogenous substance P on endogenous substance P, NK-1 receptor, and nerve ingrowth in an in vivo tendon-healing setting.

Application of BMP-7 to tibial non-unions: a 3-year multicenter experience.

The effective treatment of the often debilitating, longlasting and large-asset-consuming complication of fracture non-unions has been in the centre of scientific interest the last decades. The use of alternative bone substitutes to the gold standard of autologous graft includes the osteoinductive molecules named bone morphogenetic proteins (BMPs). A multicenter registry and database (bmpusergroup.

The effects of substance P on the biomechanic properties of ruptured rat Achilles' tendon.

Objective: To determine whether injection of substance P into the paratendinous region of a ruptured and subsequently sutured rat Achilles' tendon alters the biomechanic properties of the tendon.

Design: Interventional animal study.

Setting: Animal laboratory at a university hospital.

Exogenously administered substance P and neutral endopeptidase inhibitors stimulate fibroblast proliferation, angiogenesis and collagen organization during Achilles tendon healing.

Background: In the last few years much research has been conducted in methods to promote tendon healing. The aim of this study was to determine if the healing process after operative repair of rat Achilles tendons could be stimulated by the paratendinous injection of a sensory peptide, substance P (SP).

Methods: Ninety-six male Sprague-Dawley rats were randomly allocated to four groups: (I) control buffer injections, (II) injections of SP 10(-6) mol/kg body weight combined with a carrier, (III) injections of SP 10(-8) mol/kg BW with the carrier, and (IV) injections with the carrier only (thiorphan 1 micromol/kg BW and captopril 30 micromol/kg BW, both neutral endopeptidase inhibitors).