Muscarinic acetylcholine receptors: mutant mice provide new insights for drug development
Specific mAChR-regulated pathways are identified as potentially novel targets for the treatment of various important disorders including Alzheimer's disease, schizophrenia, pain, obesity and diabetes.
Muscarinic receptor subtypes and smooth muscle function.
Structure and Function of a Novel Voltage-gated, Tetrodotoxin-resistant Sodium Channel Specific to Sensory Neurons (*)
Functional expression in Xenopus oocytes showed that PN3 is a voltage-gated sodium channel with a depolarized activation potential, slow inactivation kinetics, and resistance to high concentrations of tetrodotoxin.
Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo
In urethane‐anaesthetized rats, the cholinergic component of volume‐induced bladder contractions was inhibited by muscarinic antagonists but had marginal effects on pinacidil‐induced, adenosine 3′:5′‐cyclic monophosphate (cyclic AMP)‐independent, relaxation, consistent with a major contribution of M2 receptors in the generation of volume-induced bladdercontractions.
RS-102221: A Novel High Affinity and Selective, 5-HT2C Receptor Antagonist
A comparison of the potential role of the tetrodotoxin-insensitive sodium channels, PN3/SNS and NaN/SNS2, in rat models of chronic pain.
The biophysical properties of the tetrodotoxin-resistant current, mediated, at least in part, by the sodium channel PN3 (SNS), suggests that it may play a specialized, pathophysiological role in the sustained, repetitive firing of the peripheral neuron after injury and suggests that relief from chronic inflammatory or neuropathic pain might be achieved by selective blockade or inhibition of Pn3 expression.
Assessment of the role of α2‐adrenoceptor subtypes in the antinociceptive, sedative and hypothermic action of dexmedetomidine in transgenic mice
1 The role of α2‐adrenoceptor (AR) subtypes in the modulation of acute nociception, motor behaviour and body temperature, has been investigated by determining the activity of the α2AR selective…
Distribution of the Tetrodotoxin-Resistant Sodium Channel PN3 in Rat Sensory Neurons in Normal and Neuropathic Conditions
The specific subcellular redistribution of PN3 after peripheral nerve injury may be an important factor in establishing peripheral nerve hyperexcitability and resultant neuropathic pain.
A Novel Tetrodotoxin-sensitive, Voltage-gated Sodium Channel Expressed in Rat and Human Dorsal Root Ganglia*
Cl cloning from rat, dorsal root ganglia (DRG), cellular expression, and functional analysis of a novel tetrodotoxin-sensitive peripheral sodium channel (PN), PN1 are reported, suggesting that rat Pn1 is an ortholog of the human neuroendocrine channel.