Search results for "Receptor"

Metabotropic glutamate receptors activate phospholipase D in astrocytes through a protein kinase C-dependent and Rho-independent pathway.

2003

Metabotropic glutamate receptors (mGluRs) are G protein-coupled receptors that mediate phospholipase D (PLD) activation in brain, but the mechanism underlying this response remains unclear. Here we used primary cultures of astrocytes as a cell model to explore the mechanism that links mGluRs to PLD. Glutamate activated both phospholipase C (PLC) and PLD with equal potency and this effect was mimicked by L-cysteinesulfinic acid, a putative neurotransmitter previously shown to activate mGluRs coupled to PLD, but not PLC, in adult brain. PLD activation by glutamate was dependent on Ca(2+) mobilization and fully blocked by both protein kinase C (PKC) inhibitors and PKC down-regulation, suggesti…

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 …

Ces molécules qui éveillent nos papilles

2017

The sense of taste is a chemical sense and one of the most ancestral sensory modalities. It allows detectingand appreciating taste molecules present in our food. Beyond our vital needs, the pleasure elicited from whatwe eat can drive our feeding behaviors sometimes up to excess. Food intake involves several sensorysystems, mainly smell and taste. The underlying molecular mechanisms are relatively complex. This articlefocuses on the extent of the chemical space associated with the five primary tastes (sour, salty, sweet, bitterand umami), and details the fundamental role of gustatory receptors in the perception of taste as well aswithin interindividual variabilities.

Mucin 1 deficiency mediates corticosteroid insensitivity in asthma

2019

BACKGROUND: The loss of corticosteroid efficacy is an important issue in severe asthma management and may lead to poor asthma control and deterioration of airflow. Recent data indicate that Mucin 1 (MUC1) membrane mucin can mediate corticosteroid efficacy in chronic rhinosinusitis, but the role of MUC1 in uncontrolled severe asthma is unknown. The objective was to analyze the previously unexplored role of MUC1 on corticosteroid efficacy in asthma. METHODS: Mucin 1 expression was evaluated by real-time PCR in human bronchial epithelial cells (HBEC) and blood neutrophils from uncontrolled severe asthma (n=27), controlled mild asthma (n=16), and healthy subjects (n=13). IL-8, MMP9, and GM-CSF …

Identification of new ligands for sigma receptors. Design and synthesis of a beta-aminoketonic drug discovery library

2009

Dolor y recaída en el alcoholismo: alteraciones en la función moduladora del sistema opioide endógeno sobre el sistema dopaminérgico mesocorticolímbi…

2020

Durant els últims anys, múltiples estudis clínics i epidemiològics han revelat que la presència de dolor crònic està estretament relacionada amb el trastorn per consum d'alcohol (AUD). De fet, el dolor crònic sembla augmentar el risc de patir AUD i predir el consum excessiu d'alcohol i la recaiguda en aquells pacients amb antecedents d'abús d'alcohol. A més, s'ha informat que el dolor té un impacte negatiu en el processament motivacional i de recompensa, ja que altera la funció de sistema mesocorticolímbic (MCLS). Els receptors opioides mu (MOR) són components clau del MCLS i són essencials per al processament de recompenses tant d'estímuls naturals com de drogues d'abús, inclòs l'alcohol. …

Analysis of the molecular mechanisms that mediate the therapeutic actions of glucocorticoids in skin

2017

Tesis doctoral 189 páginas, 53 figuras, 1 tabla como material suplementario

Graves’ disease

2017

Diazepāma ļoti mazu devu ietekme uz telpisko iemācīšanos un atmiņu alcheimera slimības streptozocīna modeļa žurkām

2018

Šī daba mērķis bija pētīt diazepāma (DZP) iespējamo pozitīvo ietekmi uz telpisko iemācīšanos un atmiņu Alcheimera slimības (AD) streptozocīna (STZ) modeļa žurkām, rezultātus iegūstot Morisa ūdens labirinta testā. Iegūtie rezultāti rāda, ka diazepāms gan ļoti mazā devā (0,05 mg/kg), gan vidējā devā (1 mg/kg) būtiski uzlaboja AD modeļa žurku telpisko iemācīšanos un atmiņu. STZ izraisītajā AD modelī iegūtie dati varētu norādīt, ka diazepāma mazu un vidējo devu īstermiņa terapeitiska lietošana varētu būt labvēlīga atmiņas traucējumu novēršanai agrīnajā AD fāzē. Tomēr ir nepieciešami tālāki, padziļināti pētījumi, lai izskaidrotu šajā pētījumā iegūtos efektus.

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 …