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5F-SDB-005 is a drug that acts as a potent agonist for the cannabinoid receptors, with an EC₅₀ of 50 nM for human CB₁ receptors, and 123 nM for human CB₂ receptors. It was discovered during research into the related compound APICA which had been sold illicitly as “2NE1”. Wikipedia
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Abstract
Synthetic cannabinoid receptor agonists (SCRAs) represent the most rapidly expanding class of new psychoactive substances (NPSs). Despite the prevalence and potency of recent chiral indole-3-carboxamide SCRAs, few pharmacological data are available regarding the enantiomeric bias of these NPSs toward human CB1 and CB2 receptors. A series of homochiral indole-3-carboxamides derived from (S)- and (R)-α-methylbenzylamine and featuring variation of the 1-alkyl substituent were prepared, pharmacologically evaluated, and compared to related achiral congeners derived from cumyl- and benzylamine. Competitive binding assays demonstrated that all analogues derived from either enantiomer of α-methylbenzylamine (14–17) showed affinities for CB1 (Ki = 47.9–813 nM) and CB2 (Ki = 47.9–347 nM) that were intermediate to that of the corresponding benzylic (10–13, CB1 Ki = 550 nM to >10 μM; CB2 Ki = 61.7 nM to >10 μM) and cumyl derivatives (6–9, CB1 Ki = 12.6–21.4 nM; CB2 Ki = 2.95–24.5 nM). In a fluorometric membrane potential assay, all α-methylbenzyl analogues (excluding 17) were potent, efficacious agonists of CB1 (EC50 = 32–464 nM; Emax = 89–104%) and low efficacy agonists of CB2 (EC50 = 54–500 nM; Emax = 52–77%), with comparable or greater potency than the benzyl analogues and much lower potency than the cumyl derivatives, consistent with binding trends. The relatively greater affinity and potency of (S)-14–17 compared to (R)-14–17 analogues at CB1 highlighted an enantiomeric bias for this series of SCRAs. Molecular dynamics simulations provided a conformational basis for the observed differences in agonist potency at CB1 pending benzylic substitution.
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| Formula | C21H23FN2O |
| Molar mass | 338.426 g·mol−1 |
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5F-SDB-005 is a drug that acts as a potent agonist for the cannabinoid receptors, with an EC50 of 50 nM for human CB1 receptors, and 123 nM for human CB2 receptors.[1] It was discovered during research into the related compound APICA which had been sold illicitly as “2NE1”.[2] 5F-SDB-006 is the terminally fluorinated analog of SDB-006, just as STS-135 is the terminally fluorinated analog of APICA. Given the known metabolic liberation (and presence as an impurity) of amantadine in the related compound APINACA, it is suspected that metabolic hydrolysis of the amide group of 5F-SDB-006 may release benzylamine.
See also[edit]
References[edit]
- ^ Banister SD, Stuart J, Kevin RC, Edington A, Longworth M, Wilkinson SM, et al. (August 2015). “Effects of bioisosteric fluorine in synthetic cannabinoid designer drugs JWH-018, AM-2201, UR-144, XLR-11, PB-22, 5F-PB-22, APICA, and STS-135”. ACS Chemical Neuroscience. 6 (8): 1445–58. doi:10.1021/acschemneuro.5b00107. PMID 25921407.
- ^ Banister SD, Wilkinson SM, Longworth M, Stuart J, Apetz N, English K, et al. (July 2013). “The synthesis and pharmacological evaluation of adamantane-derived indoles: cannabimimetic drugs of abuse”. ACS Chemical Neuroscience. 4 (7): 1081–92. doi:10.1021/cn400035r. PMC 3715837. PMID 23551277.
KEYWORDS:
Name: 5F-SDB-005
CasNo: 695213-59-3
Molecular Formula: C21H24N2O
IUPAC:N-benzyl-1-(5-fluoropentyl)-1H-indole-3-carboxamide
Molecular weight: 382.2
Appearance: White powder
Application: For chemical research
DeliveryTime: 24 hours
PackAge: 1kg/Aluminum foil bag or according to clent’s request.
Port: HongKong
Production Capacity: 500 Kilogram/Month
Purity: 99.7%
Storage: Kept in a cool,dry and ventilated place
Transportation: TNT, UPS, DHL, FEDEX, EMS and Client’s requests
LimitNum: 10 Gram
Moisture Content: <0.3%
Impurity: <0.3%
Origin: China
100% SAFE AND FAST DELIVERY GUARANTEED
5F-SDB- 006 is one of most popular powder cannabinoid with similar similar effect to SDB-006, the IUPAC name is N-benzyl-1-(5-fluoropentyl)-1H-indole-3-carboxamide, and the Molecular Formula is C21H24N2O with a Molecular weight of 382.2, the purity of our 5F-SDB-006 is above 99.5%, 5F-SDB- 006 is hot sale cannabinoid with good properties. 5F-SDB- 006 is a research compound and should only be used in scientific or forensic facilities and for research purposes only. 5F-SDB- 006 is NOT intended for human consumption.
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