Search results for " receptors"
showing 5 items of 785 documents
Abemaciclib: safety and effectiveness of a unique cyclin-dependent kinase inhibitor
2020
Introduction: The discovery and the clinical availability of novel cyclin-dependent kinases 4 and 6 inhibitors have profoundly changed the therapeutic scenario of metastatic hormone receptor-positive breast carcinoma. Among these inhibitors, abemaciclib can induce potent and sustained cell cycle arrest and immune system stimulation. Areas covered: This review summarizes the safety profile and clinical efficacy data on abemaciclib alone or in combination with aromatase inhibitors or fulvestrant in metastatic hormone receptor-positive breast carcinoma. The management of patients treated with abemaciclib is the object of this paper. Expert opinion: As shown in phase 2 and 3 clinical trials on …
Identification of new ligands for sigma receptors. Design and synthesis of a beta-aminoketonic drug discovery library
2009
Divu diazepāma devu ietekme uz Alcheimera slimības modeļa dzīvnieku sinaptisko plasticitāti un acetilholīna šķelšanu
2018
Šī darba mērķis bija noteikt gamma-aminosviestskābes (GABA) receptora benzodiazepīna saita agonista diazepāma (DZP) ļoti zemas (0,05 mg/kg) un vidējās (1 mg/kg) devas efektus uz Alcheimera slimības (AD) modeļa žurku sinaptisko plasticitāti un acetilholīna šķelšanu. Rezultāti rāda, ka AD modeļa žurku smadzenēs tika būtiski samazināta sinaptofizīna-1 (SYP) ekspresija un būtiski pieauga acetilholīna šķelšanās. Ļoti zema (0,05 mg/kg) diazepāma deva spēja uzlabot sinaptisko plasticitāti, savukārt abas (0,05 mg/kg un 1 mg/kg) diazepāma devas būtiski normalizēja acetilholīna šķelšanos AD modeļa žurku garozā un hipokampā. Iegūtie dati norāda uz ļoti zemas un vidējas devas diazepāma neiroprotektīvo …
Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety
2019
σ1 and/or σ2 receptors play a crucial role in pathological conditions such as pain, neurodegenerative disorders, and cancer. A set of spirocyclic cyclohexanes with diverse O-heterocycles and amino moieties (general structure III) was prepared and pharmacologically evaluated. In structure-activity relationships studies, the σ1 receptor affinity and σ1:σ2 selectivity were correlated with the stereochemistry, the kind and substitution pattern of the O-heterocycle, and the substituents at the exocyclic amino moiety. cis-configured 2-benzopyran cis-11b bearing a methoxy group and a tertiary cyclohexylmethylamino moiety showed the highest σ1 affinity ( Ki = 1.9 nM) of this series of compounds. In…
Targeting the Activin Receptor Signaling to Counteract the Multi-Systemic Complications of Cancer and Its Treatments
2021
Muscle wasting, i.e., cachexia, frequently occurs in cancer and associates with poor prognosis and increased morbidity and mortality. Anticancer treatments have also been shown to contribute to sustainment or exacerbation of cachexia, thus affecting quality of life and overall survival in cancer patients. Pre-clinical studies have shown that blocking activin receptor type 2 (ACVR2) or its ligands and their downstream signaling can preserve muscle mass in rodents bearing experimental cancers, as well as in chemotherapy-treated animals. In tumor-bearing mice, the prevention of skeletal and respiratory muscle wasting was also associated with improved survival. However, the definitive proof tha…