2,2-dimethylpropionic acid 3- (2- chloro- 6- methylaminopurin- 9- yl)- 2- (2,2- dimethylpropionyloxymethyl)propyl ester

a P2Y12 receptor antagonist

Also Known As:

MRS 2395; MRS-2395; MRS2395

Networked: 7 relevant articles (1 outcomes, 0 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Purines: 651
      - Adenine: 2120
        2,2-dimethylpropionic acid 3-(2-chloro-6-methylaminopurin-9-yl)-2-(2,2-dimethylpropionyloxymethyl)propyl ester: 7
Organic Chemicals: 133
- Carboxylic Acids: 973
  - Acyclic Acids
    - Valerates: 135
      - 2,2-dimethylpropionic acid 3-(2-chloro-6-methylaminopurin-9-yl)-2-(2,2-dimethylpropionyloxymethyl)propyl ester: 7
Lipids: 114793
- Fatty Acids: 27405
  - Volatile Fatty Acids: 3052
    - Valerates: 135
      - 2,2-dimethylpropionic acid 3-(2-chloro-6-methylaminopurin-9-yl)-2-(2,2-dimethylpropionyloxymethyl)propyl ester: 7

Experts

1.	Yao, Ming: 3 articles (01/2017 - 10/2012)
2.	Huang, Bing: 2 articles (01/2017 - 10/2012)
3.	Lian, Qingquan: 2 articles (01/2017 - 08/2014)
4.	Liu, Mingjuan: 2 articles (01/2017 - 08/2014)
5.	Ni, Huadong: 2 articles (01/2017 - 08/2014)
6.	Wang, Hanqi: 2 articles (01/2017 - 08/2014)
7.	Xu, Longsheng: 2 articles (01/2017 - 08/2014)
8.	Xu, Shijie: 2 articles (01/2017 - 08/2014)
9.	Chen, Lixue: 1 article (11/2019)
10.	He, Wei: 1 article (11/2019)

Related Diseases

1.	Pain (Aches) 03/01/2010 - "MRS2365 and MRS2395 had a profound, while BBG had a mild effect on inflammatory pain, with a following rank order of mED values: MRS2395 > MRS2365 > BBG. " 10/23/2012 - "These results demonstrate rat bone cancer pain could partially relieved after intrathecal injection of P2Y12 receptor inhibitor MRS2395 through inhibiting the phosphorylation of p38MAPK in spinal dorsal horn." 08/26/2014 - "To explore the roles of P2Y12 receptor (P2Y12R) in bone cancer pain by observing the changes of inflammatory cytokines (IL-1β, IL-6) after intrathecal injection (i.t.) of P2Y12R antagonist MRS2395. " 03/01/2010 - "The effect of the wide spectrum P2 receptor antagonist PPADS, the selective P2X7 receptor antagonist Brilliant Blue G (BBG), the P2X1 receptor antagonist (4,4',4'',4-[carbonylbis(imino-5,1,3-benzenetriyl-bis(carbonylimino))]tetrakis-1,3-benzenedisulfonic acid, octasodium salt (NF449) and (8,8'-[carbonylbis(imino-3,1-phenylenecarbonylimino)]bis-1,3,5-naphthalene-trisulphonic acid, hexasodium salt (NF023), the P2Y12 receptor antagonist (2,2-dimethyl-propionic acid 3-(2-chloro-6-methylaminopurin-9-yl)-2-(2,2-dimethyl-propionyloxymethyl)-propylester (MRS2395), the selective P2Y1 receptor agonist ([[(1R,2R,3S,4R,5S)-4-[6-amino-2-(methylthio)-9H-purin-9-yl]-2,3-dihydroxybicyclo[3.1.0]hex-1-yl]methyl] diphosphoric acid mono ester trisodium salt (MRS2365), the P2Y2/P2Y4 agonist uridine-5'-triphosphate (UTP), and the P2Y4/P2Y6 agonist uridine-5'-diphosphate (UDP) were examined on mechanical allodynia in the Seltzer model of neuropathic pain, on acute thermal nociception, and on the inflammatory pain and oedema induced by complete Freund's adjuvant (CFA). "
2.	Bone Neoplasms (Bone Cancer) 01/01/2017 - "Using the bone cancer model inoculated with Walker 256 tumor cells into the left tibia of Sprague Dawley rat, we blocked spinal P2Y12R through intrathecal administration of its selective antagonist MRS2395 (400 pmol/µL, 15 µL). " 10/23/2012 - "These results demonstrate rat bone cancer pain could partially relieved after intrathecal injection of P2Y12 receptor inhibitor MRS2395 through inhibiting the phosphorylation of p38MAPK in spinal dorsal horn." 08/26/2014 - "An intrathecal injection of MRS2395 may alleviate hyperalgesia and inhibit the up-regulated expression of spinal cord inflammatory cytokines in bone cancer rats. " 08/26/2014 - "To explore the roles of P2Y12 receptor (P2Y12R) in bone cancer pain by observing the changes of inflammatory cytokines (IL-1β, IL-6) after intrathecal injection (i.t.) of P2Y12R antagonist MRS2395. "
3.	Hyperalgesia 11/13/2019 - "MRS2395 and clopidogrel attenuated the development of tactile allodynia and suppressed the expression of CGRP, c-fos, and GTP-RhoA/ROCK2 in the TNC. " 08/26/2014 - "An intrathecal injection of MRS2395 may alleviate hyperalgesia and inhibit the up-regulated expression of spinal cord inflammatory cytokines in bone cancer rats. " 03/01/2010 - "MRS2365, MRS2395 and UTP, but not the other compounds, significantly alleviated mechanical allodynia in the neuropathic pain model, with the following rank order of minimal effective dose (mED) values: MRS2365 > MRS2395 > UTP. " 03/01/2010 - "The effect of the wide spectrum P2 receptor antagonist PPADS, the selective P2X7 receptor antagonist Brilliant Blue G (BBG), the P2X1 receptor antagonist (4,4',4'',4-[carbonylbis(imino-5,1,3-benzenetriyl-bis(carbonylimino))]tetrakis-1,3-benzenedisulfonic acid, octasodium salt (NF449) and (8,8'-[carbonylbis(imino-3,1-phenylenecarbonylimino)]bis-1,3,5-naphthalene-trisulphonic acid, hexasodium salt (NF023), the P2Y12 receptor antagonist (2,2-dimethyl-propionic acid 3-(2-chloro-6-methylaminopurin-9-yl)-2-(2,2-dimethyl-propionyloxymethyl)-propylester (MRS2395), the selective P2Y1 receptor agonist ([[(1R,2R,3S,4R,5S)-4-[6-amino-2-(methylthio)-9H-purin-9-yl]-2,3-dihydroxybicyclo[3.1.0]hex-1-yl]methyl] diphosphoric acid mono ester trisodium salt (MRS2365), the P2Y2/P2Y4 agonist uridine-5'-triphosphate (UTP), and the P2Y4/P2Y6 agonist uridine-5'-diphosphate (UDP) were examined on mechanical allodynia in the Seltzer model of neuropathic pain, on acute thermal nociception, and on the inflammatory pain and oedema induced by complete Freund's adjuvant (CFA). "
4.	Neoplasms (Cancer) 01/01/2017 - "Using the bone cancer model inoculated with Walker 256 tumor cells into the left tibia of Sprague Dawley rat, we blocked spinal P2Y12R through intrathecal administration of its selective antagonist MRS2395 (400 pmol/µL, 15 µL). " 08/26/2014 - "Thirty-two female SD rats were randomly divided into 4 groups (n = 8 each): sham group (group S), MRS2395 group (group M), cancer group (group A) and cancer + MRS2395 group (group MA).Groups S and M received an injection of 10 µl Hank's solution into left tibia medullar cavity while groups A and MA had an injection of Walker 256 mammary cancer cells (10 µl, 2×10(7) cells/ml) into the same place. "
5.	Acute Pain 03/01/2010 - "The rank order of mED values in acute pain was the following: MRS2365 > MRS2395 > NF449 > NF023 > UDP = UTP > PPADS. "

Related Drugs and Biologics

1.	Purinergic P2Y Receptor Antagonists
2.	Purinergic P2X7 Receptors
3.	Purinergic P2X1 Receptors
4.	Purinergic P2Y1 Receptors
5.	Cytokines
6.	Calcitonin Gene-Related Peptide
7.	Uridine Triphosphate (UTP)
8.	Uridine Diphosphate (UDP)
9.	Uridine
10.	Solutions

Related Therapies and Procedures

1.	Spinal Injections