Cooper, Samantha L March, Julie Sabbatini, Andrea R Hill, Stephen J Jörg, Manuela Scammells, Peter J Woolard, Jeanette
Published in
British journal of pharmacology
Adenosine is a local mediator that regulates physiological and pathological processes via activation of four G protein-coupled receptors (A1 , A2A , A2B , A3 ). We have investigated the effect of two A1 -receptor selective agonists and the novel A1 -receptor bitopic ligand VCP746 on the rat cardiovascular system. To investigate the effect of these ...
Florence Noble Lenoir, Magalie Marie, Nicolas
Published in
British Journal of Pharmacology
The endogenous opioid system is largely expressed in the brain, and both endogenous opioid peptides and receptors are present in areas associated with reward and motivation. It is well known that this endogenous system plays a key role in many aspects of addictive behaviours. The present review summarizes the modifications of the opioid system indu...
Sykes, David A Riddy, Darren M Stamp, Craig Bradley, Michelle E McGuiness, Neil Sattikar, Afrah Guerini, Danilo Rodrigues, Ines Glaenzel, Albrecht Dowling, Mark R
...
Published in
British Journal of Pharmacology
FTY720-P and S1P activation of the S1P1R results in receptor internalization as a consequence of an efficient recruitment of β-arrestin. The combination of slow off-rate, efficacious β-arrestin recruitment and metabolic stability all contribute to FTY720-P's ability to promote prolonged S1P1R internalization and may be critical factors in its effic...
Macías, A de la Cruz, A Prieto, A Peraza, D A Tamkun, M M González, T Valenzuela, C
Published in
British journal of pharmacology
The finding that the voltage-dependence of inactivation and the pharmacology of Kv 1.5 + Kv β1.3 channels after PKC inhibition resembled that observed in Kv 1.5 channels suggests that both processes are dependent on PKC-mediated phosphorylation. These results may have clinical relevance in diseases that are characterized by alterations in kinase ac...
Datta, Arnab Scotton, Chris J Chambers, Rachel C
Published in
British journal of pharmacology
Pulmonary fibrosis represents the end stage of a number of heterogeneous conditions and is, to a greater or lesser degree, the hallmark of the interstitial lung diseases. It is characterized by the excessive deposition of extracellular matrix proteins within the pulmonary interstitium leading to the obliteration of functional alveolar units and in ...
van der Linde, H J Van Deuren, B Teisman, A Towart, R Gallacher, D J
Published in
British journal of pharmacology
This study shows the importance of correcting QTcV intervals for changes in Tc, to avoid misleading interpretations of apparent QTcV interval changes. We recommend that all ICH S7A, conscious animal safety studies should routinely measure core body temperature and correct QTcV appropriately, if body temperature and heart rate changes are observed.
Bertrand, G Puech, R Maisonnasse, Y Bockaert, J Loubatières-Mariani, M M
Published in
British Journal of Pharmacology
1. The effects of pituitary adenylate cyclase-activating polypeptide (PACAP), vasoactive intestinal peptide (VIP) and secretin on pancreatic endocrine secretions and vascular resistance were investigated and compared in the isolated perfused pancreas of the rat. The PACAP/VIP receptor types involved have been characterized. 2. On insulin secretion,...
Lemmens-Gruber, R Karkhaneh, A Studenik, C Heistracher, P
Published in
British Journal of Pharmacology
1. The cardiotoxic effects of emetine dihydrochloride on mechanical and electrical activity were studied in isolated preparations (papillary muscles, sinoatrial and atrioventricular nodes, ventricular myocytes) of the guinea-pig heart. 2. Force of contraction was measured isometrically, action potentials and maximum rate of rise of the action poten...
