Results 171 to 180 of about 19,325 (262)

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Positive allosteric modulator of GLT-1 reduces methamphetamine hyperlocomotion, sensitization and conditioned place preference in mice. [PDF]

Neurosci Res
Mokkarala P, Wiah S, Unterwald EM, Shi X, Stern DR, Fontana ACK, Salvino JM, Rawls SM.   +7 more
europepmc   +1 more source

The relationship between the cannabinoids and cardiac remodelling: A comprehensive review of pivotal mechanisms and emerging evidence

British Journal of Pharmacology, EarlyView.
Cardiac remodelling and fibrosis after myocardial infarction or during chronic diseases, such as arterial and pulmonary hypertension or diabetes mellitus, continue to be the more important prognostic factors in determining survival, and so the search for effective anti‐fibrotic interventions is an important target for research and therapy in cardiology.
Anna Krzyżewska, Marta Baranowska‐Kuczko, Hanna Kozłowska   +2 more
wiley   +1 more source

Discovery of VU0467319: an M₁ Positive Allosteric Modulator Candidate That Advanced into Clinical Trials. [PDF]

ACS Chem Neurosci
Poslunsey MS, Wood MR, Han C, Stauffer SR, Panarese JD, Melancon BJ, Engers JL, Dickerson JW, Peng W, Noetzel MJ, Cho HP, Rodriguez AL, Hopkins CR, Morrison R, Crouch RD, Bridges TM, Blobaum AL, Boutaud O, Daniels JS, Kates MJ, Castelhano A, Rook JM, Niswender CM, Jones CK, Conn PJ, Lindsley CW.   +25 more
europepmc   +1 more source

Comprehensive transduceromic profiling of NOP receptor ligands at different Gα subunits

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose The nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) is an opioid receptor family member with distinct pharmacology and broad therapeutic potential. NOP receptors regulate functions such as nociception, stress reactivity, reward, mood, autonomic tone, immunity and sleep/wake cycle.
Davide Malfacini, Riccardo Camilotto, Michele Maritan, Erika Morrone, Stephen Afriyie Boateng, Anna Vacilotto, Salvatore Pacifico, Remo Guerrini, Nurulain T. Zaveri, Girolamo Calo'   +9 more
wiley   +1 more source

Enhancing Tetrahydrocannabinol's Therapeutic Efficacy in Inflammatory Bowel Disease: The Roles of Cannabidiol and the Cannabinoid 1 Receptor Allosteric Modulator ZCZ011. [PDF]

Pharmaceuticals (Basel)
Thapa D, Patil M, Warne LN, Carlessi R, Falasca M.   +4 more
europepmc   +1 more source

Opening closed inward rectifier potassium channel doors

British Journal of Pharmacology, EarlyView.
Inwardly rectifying potassium (KIR) channels are essential regulators of membrane potential in excitable and non‐excitable tissues. Although KIR channels exhibit a biophysical preference for potassium influx due to voltage‐dependent block of outward current by polyamines and Mg2+, under physiological conditions, they predominantly mediate K+ efflux ...
Anna Stary‐Weinzinger, Fabian Kaiser, Marcel A. G. van der Heyden, Saïd Bendahhou   +3 more
wiley   +1 more source

Preclinical pharmacology of alogabat: a novel GABA_A-α5 positive allosteric modulator targeting neurodevelopmental disorders with impaired GABA_A signaling. [PDF]

Front Pharmacol
Cecere G, Ballard TM, Knoflach F, Honer M, Hipp JF, Garces P, Mueggler T, Künnecke B, Bruns A, Prinssen EP, Schoenenberger P, Janz P, Redondo R, Biemans B, Knust H, Olivares-Morales A, Brigo A, Schulz JM, Bertrand D, Saxe M, O'Connor EC, Hernandez MC.   +21 more
europepmc   +1 more source