FAAH inhibitor 1 - CAS 326866-17-5
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Not Intended for Therapeutic Use. For research use only.
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Time-dependent preincubation study of FAAH inhibitor 1 was consistent with it being a reversible inhibitor. Activity-based protein-profiling (ABPP) evaluation of FAAH inhibitors 1 in rat tissues revealed that it had exceptional selectivity and no off-target activity with respect to other serine hydrolases. Molecular shape overlay of FAAH inhibitor 1 with a known FAAH inhibitor indicated that these compounds might act as transitionstate analogues, forming putative hydrogen bonds with catalytic residues and mimicking the charge distribution of the tetrahedral transition state. FAAH inhibitors 1 was exclusively specific against FAAH in rat brain and had no missing protein bands in all the other tissues that were tested.
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FAAH inhibitor 1
1.FAAH inhibitor OL-135 disrupts contextual, but not auditory, fear conditioning in rats.
Burman MA1, Szolusha K2, Bind R3, Kerney K3, Boger DL4, Bilsky EJ5. Behav Brain Res. 2016 Apr 13;308:1-5. doi: 10.1016/j.bbr.2016.04.014. [Epub ahead of print]
Anxiety disorders are among the most prevalent psychological disorders, have significant negative impacts on quality of life and the healthcare system, and yet effective treatments remain elusive. Manipulating the endocannabinoid system has demonstrated potential for treating anxiety, although the side effects of direct manipulations of cannabinoid receptors keeps them from widespread clinical use. Disrupting the degradation enzyme fatty acid amide hydrolase (FAAH) enhances endogenous signaling and may produce similar efficacy without the side effects. The current experiments examine the effects of low (5.6mg/kg) or moderate (10.0mg/kg) doses of OL-135, a FAAH inhibitor, on the acquisition and consolidation of classical fear conditioning, a common model of trauma-induced anxiety. The acquisition of contextual, but not auditory, fear conditioning was disrupted by both doses of OL-135. Shock reactivity was not affected. Due to the additional neural circuitry required for contextual, but not auditory, fear conditioning, these data suggest that endocannabinoid signaling outside the amygdala may be critical for a subset of fearful memories.
2.Safety, Tolerability and Pharmacokinetics of FAAH Inhibitor V158866: A Double-Blind, Randomised, Placebo-Controlled Phase I Study in Healthy Volunteers.
Pawsey S1,2, Wood M3, Browne H1, Donaldson K4, Christie M5, Warrington S6. Drugs R D. 2016 Mar 17. [Epub ahead of print]
BACKGROUND AND OBJECTIVE: The inhibition of fatty acid amide hydrolase 1 (FAAH) has been proposed as a novel mechanism for treating pain syndromes by increasing the levels of endogenous cannabinoids (ECs). This study describes the safety, tolerability, pharmacokinetics and pharmacodynamics of V158866, a reversible FAAH inhibitor, after first administration to man.
3.Systemic and spinal administration of FAAH, MAGL inhibitors and dual FAAH/MAGL inhibitors produce antipruritic effect in mice.
Yesilyurt O1, Cayirli M2, Sakin YS3, Seyrek M4, Akar A5, Dogrul A4. Arch Dermatol Res. 2016 Apr 28. [Epub ahead of print]
The increase of endocannabinoid tonus by inhibiting fatty acid amide hydrolase (FAAH) or monoacylglycerol lipase (MAGL) represents a promising therapeutic approach in a variety of disease to overcome serious central side effects of exocannabinoids. Recent studies reported that systemic administration of FAAH and MAGL inhibitors produce antipruritic action. Dual FAAH/MAGL inhibitors have also been described to get enhanced endocannabinoid therapeutic effect. In this study, we examined and compared dose-related antipruritic effects of systemic (intraperitoneal; ip) or intrathecal (it) administration of selective FAAH inhibitor PF-3845 (5, 10, and 20 mg/kg, i.p.; 1, 5, and 10 µg, i.t.), MAGL inhibitor JZL184 (4, 20, and 40 mg/kg, i.p.; 1, 5, and 10 µg, i.t.) and dual FAAH/MAGL inhibitor JZL195 (2, 5, and 20 mg/kg, i.p.; 1, 5, and 10 µg, i.t.) on serotonin (5-HT)-induced scratching model. Serotonin (25 μg) was injected intradermally in a volume of 50 μl into the rostral part of skin on the back of male Balb-C mice.
4.Self-administration of the anandamide transport inhibitor AM404 by squirrel monkeys.
Schindler CW1, Scherma M2, Redhi GH3, Vadivel SK4, Makriyannis A5, Goldberg SR3, Justinova Z3. Psychopharmacology (Berl). 2016 May;233(10):1867-77. doi: 10.1007/s00213-016-4211-3. Epub 2016 Jan 23.
RATIONALE: N-(4-hydroxyphenyl)-arachidonamide (AM404) is an anandamide transport inhibitor shown to reduce rewarding and relapse-inducing effects of nicotine in several animal models of tobacco dependence. However, the reinforcing/rewarding effects of AM404 are not clear.
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CAS 326866-17-5 FAAH inhibitor 1

FAAH inhibitor 1
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Time-dependent preincubation study of FAAH inhibitor 1 was consistent with it being a reversible inhibitor. Activity-based protein-profiling (ABPP) evaluation o...

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CAS 326866-17-5 FAAH inhibitor 1

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