Comenic acid decreases the impulse frequency of the nociceptive neuron membrane

2015 ◽  
Vol 462 (1) ◽  
pp. 155-157 ◽  
Author(s):  
O. E. Dick ◽  
T. N. Shelykh ◽  
V. B. Plakhova ◽  
A. D. Nozdrachev ◽  
B. V. Krylov
2019 ◽  
Vol 89 (3) ◽  
pp. 465
Author(s):  
О.Е. Дик

AbstractA bifurcation analysis of a nociceptive neuron model was performed to study how the firing activity pattern changes when an antinociceptive response to damaging pain stimulation arises in rat dorsal ganglia. Ectopic train activity was found to arise in the model. Suppression of train activity was demonstrated to proceed solely through modification of the activation gating structure of the Na _ V 1.8 slow sodium channel in response to comenic acid, which exerts an analgesic effect and is an active ingredient of the new nonopioid analgesic Anoceptin.


Author(s):  
Ilya V. Rogachevskii ◽  
Vera B. Plakhova ◽  
Valentina A. Penniyaynen ◽  
Stanislav G. Terekhin ◽  
Svetlana A. Podzorova ◽  
...  

A gamma-pyrone derivative, comenic acid, activates the opioid-like receptor-mediated signaling pathway that modulates the NaV1.8 channels in the primary sensory neuron membrane. These channels are responsible for generation of the nociceptive signal; gamma-pyrones can therefore have a great therapeutic potential as analgesics, and this effect deserves a deeper understanding. The novelty of our approach to the design of a medicinal substance is based on a combination of the data obtained on living neurons using very sensitive physiological methods and the results of quantum-chemical calculations. This approach allows to correlate the molecular structure of gamma-pyrones with their ability to evoke a physiological response of the neuron. Comenic acid can bind two calcium cations. One of them is chelated by the carbonyl and the hydroxyl functional groups, while another one forms the salt bond with the carboxylate anion. Calcium-bound gamma-pyrones are fundamentally different in electrostatic properties from the free gamma-pyrone molecules. These two calcium ions are the key elements involved in ligand-receptor binding. It is very likely ion-ionic interactions between these cations and anionic functional groups of the opioid-like receptor that activate the latter. The calculated intercationic distance of 9.5 Å is a structural criterion for effective ligand-receptor binding of calcium-bound gamma-pyrones.


2016 ◽  
Vol 466 (1) ◽  
pp. 77-80
Author(s):  
T. N. Shelykh ◽  
I. V. Rogachevsky ◽  
A. D. Nozdrachev ◽  
O. S. Veselkina ◽  
S. A. Podzorova ◽  
...  

Author(s):  
Xiang Zhou ◽  
Jixing Guo ◽  
Mingxia Zhang ◽  
Chunxiu Bai ◽  
Zheng Wang ◽  
...  

Abstract Crematogaster rogenhoferi (Hymenoptera: Formicidae), an omnivorous ant, is one of the dominant predatory natural enemies of a soft scale pest, Parasaissetia nigra Nietner (Homoptera: Coccidae), and can effectively control P. nigra populations in rubber forests. Olfaction plays a vital role in the process of predation. However, the information about the molecular mechanism of olfaction-evoked behaviour in C. rogenhoferi is limited. In this study, we conducted antennal transcriptome analysis to identify candidate olfactory genes. We obtained 53,892 unigenes, 16,185 of which were annotated. Based on annotations, we identified 49 unigenes related to chemoreception, including four odourant-binding proteins, three chemosensory proteins, 37 odourant receptors, two odourant ionotropic receptors and three sensory neuron membrane proteins. This is the first report on the molecular basis of the chemosensory system of C. rogenhoferi. The findings provide a basis for elucidating the molecular mechanisms of the olfactory-related behaviours of C. rogenhoferi, which would facilitate a better application of C. rogenhoferi as a biological control agent.


1991 ◽  
Vol 260 (5) ◽  
pp. H1522-H1530 ◽  
Author(s):  
T. E. Pisarri ◽  
A. Jonzon ◽  
H. M. Coleridge ◽  
J. C. Coleridge

Intravenous injection of hypertonic NaCl solution evokes reflex bradycardia and hypotension, effects thought to result from stimulation of afferent vagal endings in the lungs. To identify the afferents responsible for these effects, we recorded vagal impulses arising from endings in the lungs and lower airways of anesthetized dogs and examined the response to injection of hypertonic solutions into the pulmonary circulation. Injection of 4,800 mmol/l NaCl solution (1 ml/kg) stimulated 39 of 49 pulmonary C-fibers, their impulse frequency increasing 35-fold. Stimulation was concentration dependent, the minimum effective concentration being between 1,200 and 4,800 mmol/l. Rapidly adapting receptors were also stimulated in a concentration-dependent manner, 35 of 41 receptors being stimulated by 4,800 mmol/l NaCl solution, firing increasing fivefold. Bronchial C-fibers were not stimulated by injection into the pulmonary circulation but were by injection into the bronchial artery. Hypertonic urea solutions had qualitatively similar but smaller effects on pulmonary C-fibers and rapidly adapting receptors. The results suggest that the reflex effects of intravenous injection of hypertonic solutions result principally from stimulation of pulmonary C-fibers.


Author(s):  
Lorena Benedetti ◽  
Anna Ghilardi ◽  
Laura Prosperi ◽  
Maura Francolini ◽  
Luca Del Giacco

1967 ◽  
Vol 46 (1) ◽  
pp. 63-84
Author(s):  
K. M. CHAPMAN ◽  
J. H. PANKHURST

1. Conduction velocities of individual afferent nerve fibres from tactile spines and proprioceptive campaniform sensilla have been measured in situ over the temperature range 5-42° C., in leg preparations of the cockroach Periplaneta americana. 2. Conduction velocities at 20° C. (u20) averaged 3.3±1.4 m./sec., ranging from 1.6 to 11.0 m./sec. 3. Temperature coefficients, expressed as Q10 for the interval 20-30° C., averaged 1.7±0.24, ranging from 1.3 to 2.6. 4. The length of the propagated disturbance is about 2-3 mm., and is nearly temperature-independent. 5. Fibre diameters, estimated from conduction velocity, must be about 10 µ. 6. There is no correlation between conduction velocity and distance from the sensillum to the thoracic ganglion. Conduction delays in fibres conducting within one standard deviation of mean u20 range from about 2 to 15 msec., from the most proximal to the most distal tactile spines. 7. The effect of conduction delay on temporal and spatial sensory encoding is probably unimportant from a behavioural point of view. It contributes a factor of the form exp(-sd/u) to the sensory transfer function, and may be appreciable at upper physiological frequencies of impulse frequency modulation.


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