Name

N,N-dimethyl-5-[(4-phenylphenyl)methyl]tetrazole-1-carboxamide

Synonym

More Synonyms

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.

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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

Risk Phrases

22

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