874902-19-9

874902-19-9 structure

Name: LY2183240
Chemical Name: N,N-dimethyl-5-[(4-phenylphenyl)methyl]tetrazole-1-carboxamide
CAS Number: 874902-19-9
Molecular Formula: C₁₇H₁₇N₅O
Molecular Weight: 307.350
Catalog: Signaling Pathways Metabolic Enzyme/Protease FAAH
Create Date: 2018-12-31 12:47:06
Modify Date: 2025-08-25 20:18:50
LY2183240 is a novel and highly potent blocker of anandamide uptake (IC50 = 270 pM). LY2183240 inhibits fatty acid amide hydrolase (FAAH) activity (IC50 = 12.4 nM). IC50: 270 pM (anandamide uptake); 12.4 nM (FAAH)Target: FAAH; Anandamide uptakeFollowing i.p. administration in rats, LY2183240 increases brain anandamide concentration and exerts antinociceptive effects in formalin model of pain.

Name	N,N-dimethyl-5-[(4-phenylphenyl)methyl]tetrazole-1-carboxamide
Synonyms	5-(4-Biphenylylmethyl)-N,N-dimethyl-1H-tetrazole-1-carboxamide LY-2183240 HMS3269E15 1H-Tetrazole-1-carboxamide 1H-Tetrazole-1-carboxamide, 5-([1,1'-biphenyl]-4-ylmethyl)-N,N-dimethyl- 5-(Biphenyl-4-ylmethyl)-N,N-dimethyl-1H-tetrazole-1-carboxamide LY2183240

Description	LY2183240 is a novel and highly potent blocker of anandamide uptake (IC50 = 270 pM). LY2183240 inhibits fatty acid amide hydrolase (FAAH) activity (IC50 = 12.4 nM). IC50: 270 pM (anandamide uptake); 12.4 nM (FAAH)Target: FAAH; Anandamide uptakeFollowing i.p. administration in rats, LY2183240 increases brain anandamide concentration and exerts antinociceptive effects in formalin model of pain.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> FAAH Signaling Pathways >> Neuronal Signaling >> FAAH Research Areas >> Neurological Disease
References	[1]. Dickason-Chesterfield AK, et al. Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors. Cell Mol Neurobiol. 2006 Jul-Aug;26(4-6):407-23. [2]. Alexander JP, Cravatt BF. The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases. J Am Chem Soc. 2006 Aug 2;128(30):9699-704. [3]. Maione S, et al. Antinociceptive effects of tetrazole inhibitors of endocannabinoid inactivation: cannabinoid and non-cannabinoid receptor-mediated mechanisms. Br J Pharmacol. 2008 Nov;155(5):775-82. [4]. Pelorosso FG, et al. The endocannabinoid anandamide inhibits kinin B1 receptor sensitization through cannabinoid CB1 receptor stimulation in human umbilical vein. Eur J Pharmacol. 2009 Jan 5;602(1):176-9. [5]. Powers MS, et al. Effects of the novel endocannabinoid uptake inhibitor, LY2183240, on fear-potentiated startle and alcohol-seeking behaviors in mice selectively bred for high alcohol preference. Psychopharmacology (Berl). 2010 Dec;212(4):571-83. [6]. Sun L, et al. Endocannabinoid activation of CB1 receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. Eur J Pain. 2017 May;21(5):804-814.

Density	1.2±0.1 g/cm3
Boiling Point	506.1±53.0 °C at 760 mmHg
Melting Point	87-88ºC
Molecular Formula	C₁₇H₁₇N₅O
Molecular Weight	307.350
Flash Point	259.9±30.9 °C
Exact Mass	307.143311
PSA	63.91000
LogP	2.15
Vapour Pressure	0.0±1.3 mmHg at 25°C
Index of Refraction	1.640
Storage condition	2-8℃

Risk Phrases	22

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