Broad ligament Extraintestinal Gastrointestinal Stromal Tumor (EGIST): Case report and brief overview of EGIST.

•Highly suspicious pelvic mass may require preoperative biopsy for diagnosis.•Neoadjuvant imatinib lowers EGIST tumor burden in extensive disease preoperatively.•EGIST resection aims at complete surgical resection and negative margins.

Synthesis and pharmacological characterization of new neuronal nicotinic acetylcholine receptor ligands derived from Sazetidine-A.

The enantiomers of two analogs of Sazetidine-A as well as several other novel biosteric analogues were synthesized. Their binding affinities at three major nAChRs subtypes and selectivity profiles were determined. Though many (S)-enantiomers of Sazetidine-A analogs have high binding affinities and good subtype selectivities, it is not a general rule that (S)-enantiomers are better than their (R) counterparts.

Effects of the sazetidine-a family of compounds on the body temperature in wildtype, nicotinic receptor β2-/- and α7-/- mice.

Nicotine elicits hypothermic responses in rodents. This effect appears to be related to nicotinic receptor desensitization because sazetidine-A, an α4β2 nicotinic receptor desensitizing agent, produces marked hypothermia and potentiates nicotine-induced hypothermia in mice. To determine the specificity of sazetidine-A induced hypothermia to β2 subunit-containing nicotinic receptors, we tested its efficacy in β2 knockout (β2(-/-)) mice.

Determination of intestinal permeability of rigosertib (ON 01910.Na, Estybon): correlation with systemic exposure.

Objectives: Rigosertib (ON 01910.Na, Estybon) is a novel, anticancer agent undergoing phase 3 clinical trials for a lead indication against myelodysplastic syndromes (MDS). In this research, the permeability of rigosertib was evaluated using the in-situ perfused rat intestine (IPRI) model to support development of an oral formulation for rigosertib for treating cancer patients.

Renal excretion of apricitabine in rats: ex vivo and in vivo studies.

Apricitabine (ATC) is a novel nucleoside reverse transcriptase inhibitor undergoing phase 2/3 clinical development for the treatment of HIV infection. In this investigation, the renal handling of ATC was evaluated in the isolated perfused rat kidney (IPK) model with follow-up in vivo studies. IPK experiments were performed to characterize the renal excretion of ATC, to probe mechanisms of ATC excretion using known inhibitors of organic cation (cimetidine) and organic anion (probenecid) transport systems, and to screen for potential drug-drug interactions between ATC and clinically relevant medications (dapsone, metformin, pentamidine, stavudine, tenofovir and ritonavir).

Basic hair transplantation: 2007.

The most common form of hair loss is androgenic alopecia that affects at least half of the male population by age 50 is speculated to be caused by a change in the balance of androgen hormones. Male hair loss occurs in a characteristic pattern of decreased hair growth where hair becomes progressively finer, less pigmented, ceasing growth completely, and then becoming dislodged from the scalp. Hair loss to some patients is a serious issue that can impart a social and psychologic impact on their life.