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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 …
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 …
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 …
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
Peripheral mediators can contribute to the development and maintenance of inflammatory
and neuropathic pain and its concomitants (hyperalgesia and allodynia) via two …
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 …
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 …
effects are likely mediated by the activation of two G‐protein‐coupled receptors: B1 and B2 …
TRPA1 antagonists as potential analgesic drugs
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 …
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
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 …
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
Bradykinin potentiates synaptic glutamate release and action in the spinal cord via
presynaptic and postsynaptic B2 receptors, contributing thereby to activity-dependent central …
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 …
synaptic transmission at the first sensory synapse formed between primary afferent dorsal …