The unfortunate French clinical trial disaster in which the FAAH inhibitor BIA 10-2747 (ligand ID 9001) left one participant dead and several others with serious neurological adverse events, occurred back in January 2016. However, the primary publication that describes the properties…
Blog Archives
Hot topic: (but in this case, stale beer) the long overdue primary pharmacological characterisation of BIA 10-2747
Posted in Hot Topics
Hot topic: Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor
In this multi-author, multi-centre publication [1] lead by Denise Wootten and Patrick Sexton from the Monash Institute of Pharmacological Sciences, there is reported a 3.3 Angstrom structure of one of the more unusual G protein-coupled receptors. The CGRP receptor is…
Posted in Hot Topics
Hot Topic: β-Subunit of the voltage-gated Ca2+ channel Cav1.2 drives signaling to the nucleus via H-Ras
This paper [1] extends previous studies demonstrating a key role of voltage-gated L-type Ca2+ channels in the modulation of activity-dependent gene transcription. Earlier work in cultured neurons had already shown that L-type channel activity is required to activate gene expression…
Posted in Hot Topics
July 2018 News, Updates and Hot Topics
July 2018 News, Updates and Hot Topics Database release 2018.3: Our third database release of the year, 2018.3, is now available. This update contains the following new features and content changes: Updates across several target classes. The existing Antimalarial targets…
Hot topic: Direct activation of neuronal KV7 channels by GABA and gabapentin – a novel mechanism for reducing neuronal excitability
The potassium channels KV7.2-KV7.5 (KCNQ2-5; GtoPdb target IDs 561-564) regulate neuronal excitability in the mammalian nervous system. The best characterised neuronal KV7 channels give rise to the M current (1) and are mediated predominantly by hetero-tetramers of KV7.2 and KV7.3…
Posted in Hot Topics
Hot topic: New pharmacological tools reiterate lack of direct connection between Angiotensin 1–7 and the MAS1 GPCR
A new type of deorphanization conundrum confronted in pairing the GPCR, MAS1 with the hormonal peptide angiotensin 1–7 (Ang1-7) was emphasised in recent IUPHAR reviews (1, 2). More evidence for disconnection between Ang1-7 and MAS1 is presented in the recent…
Posted in Hot Topics
Hot Topic: Structural details for coupling of the agonist-occupied µ opioid receptor (amongst others) to the Gi protein
Every few years in the field of receptor pharmacology, a technological advance occurs that drives the field forward in terms of insight and understanding. Over the past couple of years, the cryo-EM technique (the development of which won the 2017…
