LY255582 是一种具有选择性的中枢活性阿片受体拮抗剂，对 mu、delta 和 kappa 受体具有高亲和力 ，Ki 分别为 0.4 nM、5.2、2.0 nM。LY255582 可以抑制饮食相关的中脑边缘多巴胺水平的增加，并减少食物摄入的消耗。LY255582 常用于对肥胖的研究。LY255582是用于阿片受体介导的细胞信号传导研究的潜在化合物。

Nociceptin (1-13), amide 是一种 ORL1 (OP4) 受体激动剂，与大鼠前脑膜结合的 Ki 为 0.75 nM，对小鼠输精管的 pEC50 为 7.9。

Adrenorphin (Metorphamide) 是一种 μ 阿片受体激动剂，Ki 值为 12 nM。

Ro 64-6198 is a nonpeptide, high-affinity, and brain penetration N/OFQ receptor (NOP) agonist (EC50: 25.6 nM). Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors.

Acetyl tetrapeptide-15 targets neuro sensitive skin which by decreasing the release of pro-inflammatory mediators.

Porcine dynorphin A (1-13) is a potent, endogenous κ-opioid receptor agonist that exhibits antinociceptive effects at physiological concentrations. Exposure to dynorphin A (1-13) causes acute increases in [Ca2+]i in individual neurons, similar to increases observed with acute exposure to other agents.

ADL-5859 HCl is a delta-opioid receptor agonist.

AZD7268 is a potent, selective, reversible, and orally bioavailable agonist of δ-opioid receptor with CNS penetration.

Acetalin-2, 具有序列 Ac-Arg-Phe-Met-Trp-Met-Arg-NH2 的阿片肽，其选择性地与 [3H]DAMGO 结合，展示出 93.3 nM 的 Ki 值。