436847-09-5
Chemical Structure
MRS2365
- CAS 番号: 436847-09-5
- Formula:C13H19N5O9P2S
- Molecular Weight:483.33
IUPAC Name: ((1R,2R,3S,4R,5S)-4-(6-amino-2-(methylthio)-9H-purin-9-yl)-2,3-dihydroxybicyclo[3.1.0]hexan-1-yl)methyl trihydrogen diphosphate
InChIKey: WJDVSMBTIILRAJ-XEMBYONJSA-N
SMILES: O=P(O)(OP(O)(O)=O)OC[C@]12[C@@H](O)[C@@H](O)[C@H](N3C=NC4=C(N)N=C(SC)N=C34)[C@@]1([H])C2
Biological Activity: MRS2365 is a potent and selective P2Y1 receptor (EC50=0.4 nM) /[35S]GTPγS binding/β-arrestin 2 recruitment agonist with an EC50 of 0.4 nM. MRS2365 relieves mechanical allodynia and increases mechanical sensitivity. MRS2365 shows little agonist or antagonist activity at the P2Y12 or P2Y13 receptors[1][2][3][4].
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MRS2365 | MRS2365 is a potent and selective P2Y1 receptor (EC50=0.4 nM) /[35S]GTPγS binding/β-arrestin 2 recruitment agonist with an EC50 of 0.4 nM. MRS2365 relieves mechanical allodynia and increases mechanical sensitivity. MRS2365 shows little agonist or antagonist activity at the P2Y12 or P2Y13 receptors. | |||||||||||||||||||||
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- [1]. Mariya Chhatriwala, et al. Induction of novel agonist selectivity for the ADP-activated P2Y1 receptor versus the ADP-activated P2Y12 and P2Y13 receptors by conformational constraint of an ADP analog. J Pharmacol Exp Ther. 2004 Dec;311(3):1038-43. [Content Brief]
- [2]. D M Bourdon, et al. (N)-methanocarba-2MeSADP (MRS2365) is a subtype-specific agonist that induces rapid desensitization of the P2Y1 receptor of human platelets. J Thromb Haemost. 2006 Apr;4(4):861-8. [Content Brief]
- [3]. Andó RD, et al. A comparative analysis of the activity of ligands acting at P2X and P2Y receptor subtypes in models of neuropathic, acute and inflammatory pain. Br J Pharmacol. 2010 Mar;159(5):1106-17. [Content Brief]
- [4]. Gao ZG, et al. Distinct Signaling Patterns of Allosteric Antagonism at the P2Y1 Receptor. Mol Pharmacol. 2017 Nov;92(5):613-626. [Content Brief]
Keywords
