生物活性

• 描述NECA (5'-N-Ethylcarboxamidoadenosine) is a nonselective adenosine receptor agonist. After the administration of NECA, the mean number of cocaine infusions obtained per session is decreased significantly in a dose-dependent manner. The administration of NECA results in a significant increase in latencies above values obtained for vehicle treatment^[1]. In isolated rat hearts, both NECA and the ERS (endoplasmic reticulum stress) inhibitor TUDCA decreased myocardial infarction, increased GSK-3β phosphorylation, and reversed GRP94 expression at reperfusion, suggesting that NECA protected the heart by inhibiting GSK-3β and ERS. NECA prevents the mPTP opening through inactivation of GSK-3β via ERS inhibition^[2]. Adenosine receptor (AR) stimulation by NECA increased the extravasation of intravascular tracers into the brain and proposed that AR agonism may be an effective method for therapeutic BBB disruption. Elevated blood urea nitrogen levels in mice following NECA treatment suggested that renal function impairment was a probable cause of tracer retention. Rather than inducing BBB disruption, our study demonstrated that NECA increased tracer extravasation into the brain by increasing the concentration gradient of the tracer across the BBB^[3].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01132469	Endoscopic Submucosal Dissecti... more >>on Early Gastric Cancer Multi-center, Single-arm Clinical Trial Historical Control Group Quality of Life and Cost Analysis Collapse <<	Not Applicable	Unknown	June 2017	Korea, Republic of ... more >> Inje University Busan Baik Hospital and 10 other institutes Recruiting Busan, Korea, Republic of, 614-735 Contact: Sang-Yong Seol, M.D.    82-51-890-6158    seolsymd@hanmail.net    Principal Investigator: Sang-Yong Seol, M.D. Collapse <<
  NCT00872066	Rheumatoid Arthritis ... more >> Osteoarthritis Post-traumatic Arthritis Collagen Disorders Avascular Necrosis Traumatic Femoral Fractures Nonunion of Femoral Fractures Congenital Hip Dysplasia Slipped Capital Femoral Epiphysis Collapse <<	Phase 4	Completed	-	Slovakia ... more >> Orthopaedic-traumatology Clinic University Hospital Martin Martin, Slovakia Collapse <<
  NCT02202941	Sepsis	Not Applicable	Completed	-	Korea, Republic of ... more >> Seoul National University Hospital Seoul, Korea, Republic of, 110-744 Samsung Medical Center Seoul, Korea, Republic of, 135-710 Asan Medical Center Seoul, Korea, Republic of Severance Hospital Seoul, Korea, Republic of Collapse <<

• 参考文献

• [1] Knapp CM, Foye MM, Cottam N, Ciraulo DA, Kornetsky C. Adenosine agonists CGS 21680 and NECA inhibit the initiation of cocaine self-administration. Pharmacol Biochem Behav. 2001 Apr;68(4):797-803

  [2] Xing F, Han H, He Y, Zhang Y, Jing L, Xu Z, Xi J. Roles of Endoplasmic Reticulum Stress in NECA-Induced Cardioprotection against Ischemia/Reperfusion Injury. Oxid Med Cell Longev. 2017;2017:2490501

  [3] Cheng CC, Yang YL, Liao KH, Lai TW. Adenosine receptor agonist NECA increases cerebral extravasation of fluorescein and low molecular weight dextran independent of blood-brain barrier modulation. Sci Rep. 2016 Mar 30;6:23882