Compounds with activity at serotonin (5‐hydroxytryptamine) 5‐HT₂ and α₁ adrenergic receptors have potential for the treatment of central nervous system disorders, drug addiction or overdose. Isolaureline, dicentrine and glaucine enantiomers were synthesized, and their in vitro functional activities at human 5‐HT₂ and adrenergic α₁ receptor subtypes were evaluated. The enantiomers of isolaureline and dicentrine acted as antagonists at 5‐HT₂ and α₁ receptors with (R)‐isolaureline showing the greatest potency (pK_b = 8.14 at the 5‐HT_2C receptor). Both (R)‐ and (S)‐glaucine also antagonized α₁ receptors, but they behaved very differently to the other compounds at 5‐HT₂ receptors: (S)‐glaucine acted as a partial agonist at all three 5‐HT₂ receptor subtypes, whereas (R)‐glaucine appeared to act as a positive allosteric modulator at the 5‐HT_2A receptor.

中文翻译：

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异烟酰胺，双百里碱和青霉素对映体在5-HT2和α1受体的体外功能评估

与血清素（5-羟色胺）活性的化合物5-HT ₂和α _1个肾上腺素能受体有中枢神经系统障碍，药物成瘾或过量的治疗潜力。Isolaureline，荷包牡丹碱和对映体海罂粟碱合成，并且在人的它们的体外功能活性的5-HT ₂和肾上腺素能α ₁受体亚型进行了评价。isolaureline和荷包牡丹碱中的5-HT充当拮抗剂对映异构体₂和α ₁受体与（[R）-isolaureline显示最大效力（对ķ _b  = 8.14在5-HT _2C受体）。（R）‐和（小号）-glaucine还拮抗α _1种受体，但它们表现得非常不同，以其它化合物在5-HT _2个受体：（小号）-glaucine充当部分激动剂在所有三个5-HT ₂受体亚型，而（[R ）甘草酸似乎在5-HT _2A受体上起正变构调节剂的作用。