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Pharmacology of P2X channels
The recent advancement of drug candidates targeting P2x channels into human trials, confirms the medicinal exploitability of this novel target family and provides hope that safe and effective medicines for the treatment of disorders involving P2X channels may be identified in the near future.
AF‐353, a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist
The current work describes the in vitro pharmacological characteristics of AF‐353, a novel, orally bioavailable, highly potent and selective P2X3/P2X2/3 receptor antagonist.
'Seeing through a glass darkly': casting light on imidazoline 'I' sites.
Muscarinic receptor ligands and their therapeutic potential.
Purinoceptors as therapeutic targets for lower urinary tract dysfunction
It is clearly possible that the development of selective antagonists for these receptors will occur that could lead to therapies offering better relief of sensory and motor symptoms for patients, while minimizing the systemic side effects that limit current medicines.
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
Discovery and optimization of RO-85, a novel drug-like, potent, and selective P2X3 receptor antagonist.
Harmane and harmalan are bioactive components of classical clonidine-displacing substance.
It is proposed that the beta-carbolines harmane and harmalan represent active components of classical CDS and will allow us to establish clear physiological roles for CDS.
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF.
In an effort to develop RAF inhibitors with the appropriate pharmacological properties to treat RAS mutant tumors, RAF709, a compound with potency, selectivity, and in vivo properties, was developed that will allow preclinical therapeutic hypothesis testing, but also provide an excellent probe to further unravel the complexities of RAF kinase signaling.