Last update 01 Nov 2024

P2X1 receptor x P2X3 receptor

Last update 01 Nov 2024

Basic Info

Related Targets

P2X1 receptorP2X3 receptor

Drugs associated with P2X1 receptor x P2X3 receptor

Aurintricarboxylic

Target

P2X1 receptor x P2X3 receptor

Mechanism

P2X1 receptor antagonists [+1]

Active Org.

RWTH Aachen University

Originator Org.

RWTH Aachen University

Active Indication

Chronic cough [+1]

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with P2X1 receptor x P2X3 receptor

100 Translational Medicine associated with P2X1 receptor x P2X3 receptor

0 Patents (Medical) associated with P2X1 receptor x P2X3 receptor

125

Literatures (Medical) associated with P2X1 receptor x P2X3 receptor

01 Jan 2024·Molecular Pain

Acute pulpitis promotes purinergic signaling to induce pain in rats via P38MAPK/NF-κB signaling pathway

Article

Author: Qi, Fang ; Zhang, Tiejun ; Hu, Jun ; Wang, Li ; Kang, Yiqun ; Chen, Yangxi

Toothache is one of the most common types of pain, but the mechanisms underlying pulpitis-induced pain remain unknown. The ionotropic purinergic receptor family (P2X) is reported to mediate nociception in the nervous system. This study aims to investigate the involvement of P2X3 in the sensitisation of the trigeminal ganglion (TG) and the inflammation caused by acute pulpitis. An acute tooth inflammation model was established by applying LPS to the pulp of SD rats. We found that the increased expression of P2X3 was induced by acute pulpitis. A selective P2X3 inhibitor (A-317491) reduced pain-like behavior in the maxillofacial region of rats and depressed the activation of neurons in the trigeminal ganglion induced by pulpitis. The upregulated MAPK signaling (p-p38, p-ERK1/2) expression in the ipsilateral TG induced by pulpitis could also be depressed by the application of the P2X3 inhibitor. Furthermore, the expression of markers of inflammatory processes, such as NF-κB, TNF-α and IL-1β, could be induced by acute pulpitis and deduced by the intraperitoneal injection of P2X3 antagonists. Our findings demonstrate that purinergic P2X3 receptor signaling in TG neurons contributes to pulpitis-induced pain in rats and that P2X3 signaling may be a potential therapeutic target for tooth pain.

01 Sep 2023·Purinergic signalling

DT-0111: a novel P2X3 receptor antagonist.

Article

Author: Mahadevan, Anu ; Rolland, Jean-Francois ; Sirtori, Elena ; Pelleg, Amir

Extracellular ATP (ATP) acts as an autocrine and paracrine agent, the actions of which on affected cells are mediated by P2 receptors (P2R), which include trans cell-membrane cationic channels (P2XRs), and G protein coupled receptors (P2YRs).The mammalian P2X receptors form homotrimeric or heterotrimeric cationic channels, each of which contains three ATP-binding sites.There are seven homotrimeric P2X receptors (P2X1-7) and three heteromeric (P2X2/P2X3, P2X4/P2X6, P2X1/P2X5).In the lungs and airways, ATP activates P2X3 and P2X2/3 receptors (P2X3R, P2X2/3R, resp.) localized on vagal sensory nerve terminals resulting in bronchoconstriction, and cough, and probably also localized release of pro-inflammatory neuropeptides via the axon reflex.Currently, several P2X3R and P2X2/3R antagonists are being developed as drug-candidates for the treatment of chronic cough.This report presents the receptor affinity data of a novel water-soluble small mol., DT-0111, that acts as a selective P2X3R antagonist.

01 Mar 2023·Purinergic SignallingQ3 · MEDICINE

MicroRNA: Crucial modulator in purinergic signalling involved diseases

Q3 · MEDICINE

Review

Author: Yu, Shu-Guang ; Yin, Hai-Yan ; Tang, Jin-Fan ; He, Zhao-Xuan ; Li, Yi-Fan ; Yang, Peng ; Guo, Jing

AbstractBoth microRNAs (miRNAs) and purinergic signalling are widely and respectively expressed in various tissues of different organisms and play vital roles in a variety of physiological and pathological processes. Here, we reviewed the current publications contributed to the relationship of miRNAs and purinergic signalling in cardiovascular diseases, gastrointestinal diseases, neurological diseases, and ophthalmic diseases. We tried to decode the miRNAs-purinergic signalling network of purinergic signalling involved diseases. The evidence indicated that more than 30 miRNAs (miR-22, miR-30, miR-146, miR-150, miR-155, miR-187, etc.) directly or indirectly modulate P1 receptors (A1, A2A, A2B, A3), P2 receptors (P2X1, P2X3, P2X4, P2X7, P2Y2, P2Y6, P2Y12), and ecto-enzymes (CD39, CD73, ADA2); P2X7 and CD73 could be modulated by multiple miRNAs (P2X7: miR-21, miR-22, miR-30, miR-135a, miR-150, miR-186, miR-187, miR-216b; CD73: miR-141, miR-101, miR-193b, miR-340, miR-187, miR-30, miR-422a); miR-187 would be the common miRNA to modulate P2X7 and CD73.

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