(+,-)-Octopamine HCl, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. As a neurohormone, (+,-)-Octopamine HCl induces mobilization of lipids and carbohydrates; as a neuromodulator, (+,-)-Octopamine HCl regulates desensitization of sensory inputs, arousal, initiation, and maintenance of various rhythmic behaviors and complex behaviors such as learning and memory; and as a neurotransmitter, (+,-)-Octopamine HCl regulates endocrine gland activity. (+,-)-Octopamine HCl exerts its function by binding to specific proteins belonging to the G protein-coupled receptor superfamily, which share a common structural feature of seven transmembrane domains. Activation of the octopamine (OA) receptor couples with various second messenger pathways, including activation and inhibition of adenylate cyclase, activation of phospholipase C, and coupling with chloride channels, depending on species, tissue origin, receptor type, and the cell line used to express the clonal receptor[1][2][3].
In vitro, (+,-)-Octopamine HCl (5-40μM) showed no effect on 3T3-L1 cell viability after 24h and on the differentiation of preadipocytes into mature adipocytes after 8 days[4].
In vivo, treatment with (+,-)-Octopamine HCl (81μmol/kg; i.p.; 4 weeks) reduced body weight gain by 19% and decreased elevated plasma insulin levels in obese Zucker rats[5].
References:
[1] Roeder T. Octopamine in invertebrates. Prog Neurobiol. 1999;59(5):533-561.
[2] Farooqui T. Octopamine-mediated neuromodulation of insect senses. Neurochem Res. 2007;32(9):1511-1529.
[3] Axelrod J, Saavedra JM. Octopamine. Nature. 1977;265(5594):501-504.
[4] Lee D, Lee JH, Kim BH, Lee S, Kim DW, Kang KS. Phytochemical Combination (p-Synephrine, p-Octopamine Hydrochloride, and Hispidulin) for Improving Obesity in Obese Mice Induced by High-Fat Diet. Nutrients. 2022;14(10):2164.
[5] Bour S, Visentin V, Prévot D, Carpéné C. Moderate weight-lowering effect of octopamine treatment in obese Zucker rats. J Physiol Biochem. 2003;59(3):175-182.
(+,-)-Octopamine HCl是一种与去甲肾上腺素结构相似的生物性单胺类物质，在无脊椎动物体内充当神经激素、神经调节剂和神经递质的角色。作为神经激素，它能够促使脂质和碳水化合物的动员；作为神经调节剂，它能够调节感觉输入的脱敏、觉醒、行为的启动和维持，以及各种节律性行为和复杂行为（如学习和记忆）的进行；作为神经递质，它能够调节内分泌腺的活动。(+,-)-Octopamine HCl通过与属于G蛋白偶联受体超家族的特定蛋白质结合发挥作用，这些蛋白质具有七个跨膜结构域的共同结构特征。Octopamine（OA）受体的激活会与不同的第二信使通路相耦合，包括腺苷酸环化酶的激活与抑制、磷脂酶C的激活以及与氯离子通道的耦合，具体取决于物种、组织来源、受体类型以及用于表达克隆受体的细胞系[1][2][3]。
体外实验中，(+,-)-Octopamine HCl（5-40μM）在孵育24小时后对3T3-L1细胞活力无影响，在孵育8天后不影响前脂肪细胞向成熟脂肪细胞的分化[4]。
体内实验中，(+,-)-Octopamine HCl（81μmol/kg，腹腔注射，持续4周）的治疗可使肥胖Zucker大鼠的体重增加减少19%并降低升高的血浆胰岛素水平[5]。