The synthesis of a new series of 2-(aryl)alkylthio derivatives of N-ethylcarboxamido adenosine (NECA) is described, in comparison with the corresponding derivatives of adenosine. Binding studies (A1, A2A, and A3) and adenylyl cyclase activity (A2B) at human adenosine receptor subtypes stably transfected in Chinese hamster ovary (CHO) cells showed that the 2(aryl)alkylthioadenosine derivatives a...

According to the Gα subunit amino acid sequence homology, G proteins divide into four families that can couple to different GPCRs. To investigate the combination of interaction between G proteins (Gs, Gi/Go, q11 and 12/13) and A2A, D2R, or A2A/D2 respectively, Föster resonance energy transfer (FRET) and bimolecular fluorescence complementation (BiFC) assays, with the advantage to analyze protei...

Caffeine is the most widely used stimulant in Western countries. Some people voluntarily reduce caffeine consumption because it impairs the quality of their sleep. Studies in mice revealed that the disruption of sleep after caffeine is mediated by blockade of adenosine A2A receptors. Here we show in humans that (1) habitual caffeine consumption is associated with reduced sleep quality in self-r...

The objective of this study was to estimate the effects of beta-kappa-casein (CN) haplotypes on first-lactation milk production traits. The beta-kappa-CN haplotypes were deduced using information on beta- and kappa-CN genotypes of cows and their sires for 16,973 Finnish Ayrshire cows that had at least nine paternal half sibs. Effects of CN haplotypes on milk production traits were estimated for...

Scislo, Tadeusz J., and Donal S. O’Leary. Differential role of ionotropic glutamatergic mechanisms in responses to NTS P2x and A2a receptor stimulation. Am J Physiol Heart Circ Physiol 278: H2057–H2068, 2000.—Activation of ATP P2x receptors in the subpostremal nucleus tractus solitarii (NTS) via microinjection of a,b-methylene ATP (a,b-MeATP) elicits fast initial depressor and sympathoinhibitor...

The concept that G protein-coupled receptors (GPCRs) function as oligomers has been widely accepted, however, different methodologies often used to study the phenomenon of GPCR interactions do not allow, as yet, for any generalization as to whether di- or oligomers are formed constitutively or are ligand-promoted. Here, we report on the use of three independent biophysical approaches based on t...

METHODS. Isolated arteries from the intraocular part of the porcine ciliary artery were suspended in microvascular myographs for isometric tension recording. The segments were contracted with the a2-adrenoceptor agonists brimonidine, apraclonidine, and oxymetazoline. To determine which subtypes of the a2-adrenoceptor mediate this contraction, antagonists subselective for the different a2-adreno...

BACKGROUND Severe Clostridium difficile toxin-induced enteritis is characterized by exuberant intestinal tissue inflammation, epithelial disruption and diarrhea. Adenosine, through its action on the adenosine A2A receptor, prevents neutrophillic adhesion and oxidative burst and inhibits inflammatory cytokine production. Alanyl-glutamine enhances intestinal mucosal repair and decreases apoptosis...

Behavior is guided by motivation; such motivation includes effort and reward. The striatum plays a central role in integrating value of reward and effort associated with behavior, through converging inputs from multiple areas of the brain. Two antagonistic pathways within the striatum are involved in this process; the direct pathway which executes behavior that is rewarded and the indirect path...

The function of A1- and A2a-adenosine receptors in the control of vascular resistance and in the modulation of light-evoked neuronal activity was investigated in the isolated perfused cat eye. The A1 agonist CCPA, the A1 antagonist CPT, the A2a agonist CGS 21680 and the A2 antagonist DMPX were used. The agents were applied intra-arterially at concentrations in the low nanomolar to micromolar ra...