neurokinin receptor antagonist

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  • Antagonism of the Neurokinin-1 Receptor Improves Survival in a Mouse Model of Sepsis by Decreasing Inflammation and Increasing Early Cardiovascular Function.
  • Mella JR1, Chiswick E, Stepien D, Moitra R, Duffy ER, Stucchi A, Remick D.
  • Critical care medicine.Crit Care Med.2017 Feb;45(2):e213-e221. doi: 10.1097/CCM.0000000000002075.
  • OBJECTIVES: Sepsis remains a serious clinical problem despite intensive research efforts and numerous attempts to improve outcome by modifying the inflammatory response. Substance P, the principal ligand for the neurokinin-1 receptor, is a potent proinflammatory mediator that exacerbates inflammator
  • PMID 27632670
  • Pharmacodynamic evaluation of Lys5, MeLeu9, Nle10-NKA(4-10) prokinetic effects on bladder and colon activity in acute spinal cord transected and spinally intact rats.
  • Kullmann FA1, Katofiasc M2, Thor KB2, Marson L3.
  • Naunyn-Schmiedeberg's archives of pharmacology.Naunyn Schmiedebergs Arch Pharmacol.2017 Feb;390(2):163-173. doi: 10.1007/s00210-016-1317-4. Epub 2016 Nov 26.
  • The purpose of this study was to determine feasibility of a novel therapeutic approach to drug-induced voiding after spinal cord injury (SCI) using a well-characterized, peptide, neurokinin 2 receptor (NK2 receptor) agonist, Lys5, MeLeu9, Nle10-NKA(4-10) (LMN-NKA). Cystometry and colorectal pressure
  • PMID 27889808
  • Differential effects of aprepitant, a clinically used neurokinin-1 receptor antagonist on the expression of conditioned psychostimulant versus opioid reward.
  • Mannangatti P1, Sundaramurthy S1, Ramamoorthy S1, Jayanthi LD2.
  • Psychopharmacology.Psychopharmacology (Berl).2017 Feb;234(4):695-705. doi: 10.1007/s00213-016-4504-6. Epub 2016 Dec 24.
  • RATIONALE: Neurokinin-1 receptor (NK1R) signaling modulates behaviors associated with psychostimulants and opioids. Psychostimulants, such as amphetamine (AMPH) and cocaine, bind to monoamine transporters and alter their functions. Both dopamine and norepinephrine transporters are regulated by NK1R
  • PMID 28013351


  • Antiemetic Effects of a Potent and Selective Neurokinin-1 Receptor Antagonist, FK886, on Cisplatin- and Apomorphine-Induced Emesis in Dogs
  • Yoshino Furukawa Takako,Nakayama Hiroe,Kikuchi Aya [他]
  • Biological & pharmaceutical bulletin 36(6), 974-979, 2013-06
  • NAID 40019652671
  • Volume Transmission of Substance P in Striatum Induced by Intraplantar Formalin Injection Attenuates Nociceptive Responses via Activation of the Neurokinin 1 Receptor
  • Nakamura Yoki,Izumi Hiroki,Shimizu Takumi,Hisaoka-Nakashima Kazue,Morioka Norimitsu,Nakata Yoshihiro
  • Journal of Pharmacological Sciences 121(4), 257-271, 2013
  • … A slow-onset but significant increase of SP and neurokinin 1 receptor (NK1R) internalization in the contralateral striatum were observed following the second phase of formalin-induced nociceptive behaviors. … Moreover, these anti-nociceptive effects of SP were completely inhibited by co-treatment with the NK1R antagonist CP96345. …
  • NAID 130003362690


Neurokinin 1 (NK1) receptor antagonists are in a class of drug used to treat nausea and vomiting associated with chemotherapy. Aprepitant, casopitant, and fosaprepitant are NK1 drugs. There is some evidence that fosaprepitant may ...
英語タイトル:Neurokinin 3 (NK3) Receptor Antagonists -Pipeline Insights, 2015 商品コード:DIMRMOA5494 発行会社(調査会社):DelveInsight 発行日:2015年版(※最新版はお問い合わせください) ページ数:25以上 ...





  [★] 拮抗薬

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「a drug that neutralizes or counteracts the effects of another drug」

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「a muscle that relaxes while another contracts; "when bending the elbow the triceps are the antagonist"」

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  [★] 受容体

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「a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response」

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「=sense organ / 受信装置」