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Biological Activity:
Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI).
in vitro: Efavirenz is a potent inhibitor of the wild-type HIV-1 RT (Ki = 2.93 nM) and exhibited a 95% inhibitory concentration of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture. Efavirenz inhibited synthesis using an RNA PPT-primed substrate with an IC50 of 17 nM. In contrast to L-697661 and nevirapine, efavirenz also inhibited synthesis with the DNA PPT-primed substrate. However, with an IC50 of 345 nM, the activity of efavirenz was more than 20-fold less potent as an inhibitor of DNA PPT-primed synthesis compared with reactions in which an RNA PPT primer was used. in vivo: Efavirenz occasions drug-lever responding in rats discriminating LSD from saline, and this effect is abolished by selective blockade of the 5-HT(2A) receptor. Similar to LSD, efavirenz induces head-twitch responses in wild-type, but not in 5-HT(2A)-knockout, mice. The rats in the treatment group received 600mg/70kg bogy weight of efavirenz dissolved in distilled water daily for 30days through the orogastric tube. Chronic administration of efavirenz may have an adverse effect on the visual sensibilities by affecting the microanatomy of the lateral geniculate body of adult Wistar rats.
References:
1. Grobler, J.A., et al., HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro. J Biol Chem, 2007. 282(11): p. 8005-10.
2. Gatch, M.B., et al., The HIV antiretroviral drug efavirenz has LSD-like properties. Neuropsychopharmacology, 2013. 38(12): p. 2373-84.
3. Adjene, J.O., P.S. Igbigbi, and E.U. Nwose, Histological effects of chronic administration of efavirenz on lateral geniculate body of adult Wistar rats. N Am J Med Sci, 2010. 2(1): p. 1-4.
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C13602 Efavirenz (154598-52-4)