J. Barrett, B. Canning, Joseph Coulson, Erin Dombrowsky, S. Douglas, T. Fong, C. Heyward, S. Leeman, Pranela Remeshwar
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引用次数: 0
摘要
速激肽受体(NC-IUPHAR推荐的临时命名[91])被内源性肽物质P (SP)、神经激肽A (NKA;以前称为物质K,神经激肽α,神经质素L),神经激肽B (NKB;神经激肽(A和B)是速激肽家族的哺乳动物成员,它包括哺乳动物和非哺乳动物起源的肽,包含一致的序列:ph -x- gly - leu - met。在非肽配体的背景下,这三种受体在体外药理学上存在显著的物种差异。拮抗剂如阿瑞吡坦和fosaprepitant已被FDA和EMA批准与其他止吐药物联合使用,用于预防呕吐性癌症化疗相关的恶心和呕吐。
Tachykinin receptors (provisional nomenclature as recommended by NC-IUPHAR [91]) are activated by the endogenous peptides substance P (SP), neurokinin A (NKA; previously known as substance K, neurokinin α, neuromedin L), neurokinin B (NKB; previously known as neurokinin β, neuromedin K), neuropeptide K and neuropeptide γ (N-terminally extended forms of neurokinin A). The neurokinins (A and B) are mammalian members of the tachykinin family, which includes peptides of mammalian and nonmammalian origin containing the consensus sequence: Phe-x-Gly-Leu-Met. Marked species differences in in vitro pharmacology exist for all three receptors, in the context of nonpeptide ligands. Antagonists such as aprepitant and fosaprepitant were approved by FDA and EMA, in combination with other antiemetic agents, for the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy.