Toll Free: (877) 796-6397 -- USA and Canada only -- |
Fax: +1-832-582-8590 Orders: +1-832-582-8158 |
Tech Support: +1-832-582-8158 Ext:3 Please provide your Order Number in the email. |
Formula | C22H21Cl2IN4O |
||||||
Molecular Weight | 555.24 | CAS No. | 183232-66-8 | ||||
Solubility (25°C)* | In vitro | DMSO | 40 mg/mL (72.04 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
|
||||||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. | |
---|---|---|
Targets |
|
|
In vitro | AM251 reduces veratridine-dependent (tetrodotoxin suppressible) release of L-glutamic acid and GABA from synaptosomes with IC50 of 8.5 μM and 9.2 μM, respectively. AM251 increases (by 2.3 times) the Kd of radioligand without altering Bmax. AM251 inhibits equilibrium binding by allosterically accelerating the dissociation of the [3H]-batrachotoxinin A 20-alpha-benzoate:sodium channel complex. [1] AM251 reduces cholesteryl ester synthesis in unstimulated and acetylated LDL-stimulated Raw 264.7 macrophages, CB2+/+ and CB2 −/− peritoneal macrophages. [2] | |
In vivo | AM251 causes a sustained reduction of daily food intake in the rat. [3] AM251 produces food avoidance and behaviors associated with nausea but does not impair feeding efficiency in rats. [4] AM251 disrupts memory consolidation of the inhibitory avoidance task. [5] AM251 has caused a significative decrease in the test step-down latency when compared to the control group, but no differences are detected in the open field habituation task, including the number of crossings, i.e. there are no motor effects. [6] AM251 (4.0 mg/kg) reduces freezing during a conditioned tone cue played within a novel context. [7] | |
Features | A selective cannabinoid 1 blocker. |
Animal Study:[5] |
|
---|
, , Tumour Biol, 2016, DOI: 10.1007/s13277-016-5447-6
Data from [Data independently produced by , , Neuropharmacology, 2018, 133:242-253]
Wwl70-induced ABHD6 inhibition attenuates memory deficits and pathological phenotypes in APPswe/PS1dE9 mice [ Pharmacol Res, 2023, 194:106864] | PubMed: 37480972 |
The endocannabinoid system's involvement in motor development relies on cannabinoid receptors, TRP channels, and Sonic Hedgehog signaling [ Physiol Rep, 2023, 11(1):e15565] | PubMed: 36636759 |
Medium-throughput zebrafish optogenetic platform identifies deficits in subsequent neural activity following brief early exposure to cannabidiol and Δ9-tetrahydrocannabinol [ Sci Rep, 2021, 11(1):11515] | PubMed: 34075141 |
Early suppression of the endocannabinoid degrading enzymes FAAH and MAGL alters locomotor development in zebrafish [ J Exp Biol, 2021, jeb.242635] | PubMed: 34151979 |
Embryonic exposure to cannabidiol disrupts active neural circuits, an effect increased by Δ□-tetrahydrocannabinol and involving CB1R and CB2R in zebrafish [ BioRxiv, 2021, 10.1101/2021.01.04.425279] | PubMed: none |
N-linoleyltyrosine protects PC12 cells against oxidative damage via autophagy: Possible involvement of CB1 receptor regulation [ Int J Mol Med, 2020, 46(5):1827-1837] | PubMed: 33000188 |
Rimonabant suppresses RNA transcription of hepatitis B virus by inhibiting hepatocyte nuclear factor 4α. [ Microbiol Immunol, 2020, 10.1111/1348-0421.12777] | PubMed: 31981244 |
CB1 and CB2 receptors play differential roles in early zebrafish locomotor development. [ J Exp Biol, 2019, 222(Pt 16)] | PubMed: 31253713 |
CB1 and CB2 receptors play differential roles in early zebrafish locomotor development [ J Exp Biol, 2019, 222(Pt 16)jeb206680] | PubMed: 31253713 |
Impaired glucocorticoid-mediated HPA axis negative feedback induced by juvenile social isolation in male rats [Boero G Neuropharmacology, 2018, 133:242-253] | PubMed: 29407214 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.