A-317491

Modify Date: 2024-01-11 12:41:52

A-317491 Structure
A-317491 structure
Common Name A-317491
CAS Number 475205-49-3 Molecular Weight 565.56900
Density N/A Boiling Point N/A
Molecular Formula C33H27NO8 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of A-317491


A-317491 is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors. IC50 value: Target: P2X2/3It is known that P2X3 and P2X2/3 receptors stimulate the pronociceptive effects of ATP upon activation. Studies indicate that the P2X3 receptor is implicated in both neuropathic and inflammatory pain. P2X3 receptor is a promising target for therapeutic intervention in cancer patients for pain management.

 Names

Name 5-[(3-phenoxyphenyl)methyl-[(1S)-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoyl]benzene-1,2,4-tricarboxylic acid
Synonym More Synonyms

 A-317491 Biological Activity

Description A-317491 is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors. IC50 value: Target: P2X2/3It is known that P2X3 and P2X2/3 receptors stimulate the pronociceptive effects of ATP upon activation. Studies indicate that the P2X3 receptor is implicated in both neuropathic and inflammatory pain. P2X3 receptor is a promising target for therapeutic intervention in cancer patients for pain management.
Related Catalog
References

[1]. Hansen RR, Nasser A, Falk S, et al. Chronic administration of the selective P2X3, P2X2/3 receptor antagonist, A-317491, transiently attenuates cancer-induced bone pain in mice. Eur J Pharmacol. 2012 Aug 5;688(1-3):27-34.

[2]. Wu JX, Xu MY, Miao XR, et al. Functional up-regulation of P2X3 receptors in dorsal root ganglion in a rat model of bone cancer pain. Eur J Pain. 2012;16(10):1378-88.

[3]. Xu J, Chu KL, Brederson JD, et al. Spontaneous firing and evoked responses of spinal nociceptive neurons are attenuated by blockade of P2X3 and P2X2/3 receptors in inflamed rats. J Neurosci Res. 2012;90(8):1597-606.

[4]. Yasuda M, Shinoda M, Kiyomoto M, et al. P2X3 receptor mediates ectopic mechanical allodynia with inflamed lower lip in mice. Neurosci Lett. 2012 18;528(1):67-72.

[5]. Maria Cláudia G. Oliveiraa, Adriana Pelegrini-da-Silvaa, et al. Peripheral mechanisms underlying the essential role of P2X3,2/3 receptors in the development of inflammatory hyperalgesia. PAIN. 2009,141(1-2): 127-134.

[6]. Yuan M, et al. Effect of A-317491 delivered by glycolipid-like polymer micelles on endometriosis pain. Int J Nanomedicine. 2017 Nov 9;12:8171-8183.

 Chemical & Physical Properties

Molecular Formula C33H27NO8
Molecular Weight 565.56900
Exact Mass 565.17400
PSA 141.44000
LogP 6.29350
Storage condition -20°C

 Synonyms

cs-1250
A-317491