The “cyclopropyl fragment” is a versatile player that frequently appears in preclinical/clinical drug molecules

TT Talele - Journal of medicinal chemistry, 2016 - ACS Publications
Recently, there has been an increasing use of the cyclopropyl ring in drug development to
transition drug candidates from the preclinical to clinical stage. Important features of the …

Models and mechanisms of hyperalgesia and allodynia

J Sandkuhler - Physiological reviews, 2009 - journals.physiology.org
Hyperalgesia and allodynia are frequent symptoms of disease and may be useful
adaptations to protect vulnerable tissues. Both may, however, also emerge as diseases in …

International union of pharmacology. XLV. Classification of the kinin receptor family: from molecular mechanisms to pathophysiological consequences

LMF Leeb-Lundberg, F Marceau, W Müller-Esterl… - Pharmacological …, 2005 - Elsevier
Kinins are proinflammatory peptides that mediate numerous vascular and pain responses to
tissue injury. Two pharmacologically distinct kinin receptor subtypes have been identified …

Sensory and signaling mechanisms of bradykinin, eicosanoids, platelet-activating factor, and nitric oxide in peripheral nociceptors

G Pethő, PW Reeh - Physiological reviews, 2012 - journals.physiology.org
Peripheral mediators can contribute to the development and maintenance of inflammatory
and neuropathic pain and its concomitants (hyperalgesia and allodynia) via two …

Novel therapeutic strategy to prevent chemotherapy-induced persistent sensory neuropathy by TRPA1 blockade

G Trevisan, S Materazzi, C Fusi, A Altomare… - Cancer …, 2013 - aacrjournals.org
Chemotherapy-induced peripheral neuropathy (CIPN) is a severe and painful adverse
reaction of cancer treatment in patients that is little understood or treated. Cytotoxic drugs …

Kinin B1 receptors: key G‐protein‐coupled receptors and their role in inflammatory and painful processes

JB Calixto, R Medeiros, ES Fernandes… - British journal of …, 2004 - Wiley Online Library
Kinins are a family of peptides implicated in several pathophysiological events. Most of their
effects are likely mediated by the activation of two G‐protein‐coupled receptors: B1 and B2 …

TRPA1 antagonists as potential analgesic drugs

EL Andrade, FC Meotti, JB Calixto - Pharmacology & therapeutics, 2012 - Elsevier
The necessity of safe and effective treatments for chronic pain has intensified the search for
new analgesic drugs. In the last few years, members of a closely-related family of ion …

Bradykinin produces pain hypersensitivity by potentiating spinal cord glutamatergic synaptic transmission

H Wang, T Kohno, F Amaya, GJ Brenner, N Ito… - Journal of …, 2005 - jneurosci.org
Bradykinin, an inflammatory mediator, sensitizes nociceptor peripheral terminals reducing
pain threshold. We now show that the B2 kinin receptor is expressed in rat dorsal horn …

Bradykinin enhances AMPA and NMDA receptor activity in spinal cord dorsal horn neurons by activating multiple kinases to produce pain hypersensitivity

T Kohno, H Wang, F Amaya, GJ Brenner… - Journal of …, 2008 - jneurosci.org
Bradykinin potentiates synaptic glutamate release and action in the spinal cord via
presynaptic and postsynaptic B2 receptors, contributing thereby to activity-dependent central …

Potentiation of glutamatergic synaptic transmission by protein kinase C‐mediated sensitization of TRPV1 at the first sensory synapse

P Sikand, LS Premkumar - The Journal of physiology, 2007 - Wiley Online Library
Sensory input from the periphery to the CNS is critically dependent on the strength of
synaptic transmission at the first sensory synapse formed between primary afferent dorsal …