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| Formula | C29H40O3 |
| Molar mass | 436.636 g·mol−1 |
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Lixosicone (AEF0117,3β-(4-methoxybenzyloxy)pregn-5-en-20-one) is a compound derived frompregnenolone by Aelis Farma, which acts as a biasedallosteric modulator of thecannabinoidCB1receptor, representing a new class of compounds referred to as CB1-selective signalling-specific inhibitors (CB1-SSi). It binds to an allosteric site on the CB1 receptor and modifies the downstream signalling produced as a result of CB1 activation, preventing CB1 mediated changes tomitogen-activated protein kinase (MAPK) phosphorylation but without affecting the signalling mediated bycyclic AMP. Unlike pregnenolone, AEF0117 is specific for the CB1-SSi activity and lacks theneurosteroid action typical of many structurally related compounds.[1]
In Phase II humanclinical trials in patients diagnosed withcannabis use disorder, AEF0117 was found to partly but not completely block the effects ofTHC, and reduced cannabis self-administration but without producing an acutewithdrawal syndrome and with relatively mild side effects. It is hoped that compounds of this type may be useful either as medications for the treatment of cannabinoid dependence, or could be used alongsidemedicinal cannabis to reduce unwanted side effects while retaining therapeutic efficacy.[2]
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