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. Author manuscript; available in PMC: 2024 Jun 20.
Published in final edited form as: Neuron. 2023 Oct 16;111(24):3926–3940.e10. doi: 10.1016/j.neuron.2023.09.017

Figure 1. Design, synthesis, and in vitro validation of PhOX and PhNX.

Figure 1.

(A) Chemical structures of OXM (1), NLX (2), and the photoactivatable small molecule opioid drugs CNV-NLX (3), PhOX (4), PhNX (5), and DEAC-OXM (6). The light-removable DMNPE and DEAC caging groups are drawn in violet.

(B) Reaction scheme depicting the one-step alkylation procedure used to synthesize PhOX and PhNX.

(C) Reaction scheme depicting ultraviolet-light-driven photorelease of OXM and NLX from PhOX, and PhNX, respectively.

(D) Agonist dose-response curves at the MOR using a cAMP assay. The solid line depicts the best-fit sigmoidal function used to derive the indicated EC50 value. Data were normalized to the response produced by DAMGO (1 μM) and are expressed as mean ± SEM (n = 5 wells per concentration).

(E) Antagonist dose-response curves at the MOR in the presence of DAMGO (100 nM). Data are presented as in (D). See also Figures S1–S3.