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Lu AF27139

P2X7 receptor antagonist

Also Known As:

N-((2S)-2-(4-chlorophenyl)-2-morpholin-4-ylethyl)-2-pyrimidin-2-yl-4-(trifluoromethyl)-1,3-thiazole-5-carboxamide

Networked: 3 relevant articles (0 outcomes, 0 trials/studies)

Bio-Agent Context: Research Results

Experts

1.	Cajina, Manuel: 2 articles (01/2022 - 01/2021)
2.	Chandrasena, Gamini: 2 articles (01/2022 - 01/2021)
3.	Gandhi, Adarsh: 2 articles (01/2022 - 01/2021)
4.	Hopper, Allen T: 2 articles (01/2022 - 01/2021)
5.	Khayrullina, Tanzilya: 2 articles (01/2022 - 01/2021)
6.	Möller, Thomas: 2 articles (01/2022 - 01/2021)
7.	Nattini, Megan E: 2 articles (01/2022 - 01/2021)
8.	Staal, Roland: 2 articles (01/2022 - 01/2021)
9.	Zorn, Stevin H: 2 articles (01/2022 - 01/2021)
10.	Breysse, Nathalie: 1 article (01/2022)

Related Diseases

1.	Pain (Aches) 01/01/2022 - "Lu AF27139 blocked several pain-relevant pathways downstream of P2X7 receptors in vitro. " 12/01/2022 - "Lu AF27139 was well tolerated as revealed by a lack of significant effect on rotarod motor function and coordination at all doses tested up to 300 mg/kg. Thus, P2X7 receptor antagonism is efficacious in a rat model of visceral pain, via a mechanism which potentially involves attenuation of microglial function within spinal and/or supraspinal pain circuits, albeit a peripheral site of action cannot be excluded."
2.	Visceral Pain 12/01/2022 - "Lu AF27139 was well tolerated as revealed by a lack of significant effect on rotarod motor function and coordination at all doses tested up to 300 mg/kg. Thus, P2X7 receptor antagonism is efficacious in a rat model of visceral pain, via a mechanism which potentially involves attenuation of microglial function within spinal and/or supraspinal pain circuits, albeit a peripheral site of action cannot be excluded." 12/01/2022 - "Inhibition of P2X7 receptors by Lu AF27139 diminishes colonic hypersensitivity and CNS prostanoid levels in a rat model of visceral pain."
3.	Hypersensitivity (Allergy) 12/01/2022 - "We have used the selective and CNS penetrant P2X7 receptor antagonist Lu AF27139 to explore this receptor's role in distinct rat models of inflammatory and visceral hypersensitivity. " 12/01/2022 - "Inhibition of P2X7 receptors by Lu AF27139 diminishes colonic hypersensitivity and CNS prostanoid levels in a rat model of visceral pain." 12/01/2022 - "Colonic hypersensitivity was also reversed by Lu AF27139 (10-100 mg/kg) and by the κ-opioid receptor agonist U-50,488H (3 mg/kg, s.c.). "
4.	Central Nervous System Diseases (CNS Diseases) 01/01/2021 - "Based on these properties, we believe Lu AF27139 will be a valuable tool for probing the role of the P2X7 receptor in rodent models of CNS diseases."

Related Drugs and Biologics

1.	Purinergic P2X7 Receptors
2.	(trans)-Isomer 3,4- Dichloro- N- methyl- N- (2- (1- pyrrolidinyl)- cyclohexyl)- benzeneacetamide
3.	Opioid Receptors (Opioid Receptor)
4.	Prostaglandins