N6-Cyclopentyladenosine

N6-Cyclopentyladenosine (CPA) is a selective Adenosine A₁ receptor agonist, with K_i values of 2.3 nM, 790 nM and 43 nM for human A₁, A_2A and A₃ receptors, respectively. N6-cyclopentyladenosine increases Apoptosis. N6-Cyclopentyladenosine has antitumor activity against leukemia. N6-cyclopentyladenosine improves 5-fluorouracil (HY-90006)-induced hematopoietic damage, regulates sleep, and delays Aminophylline-induced clonic epileptic seizures^{[1][2][3][4][5][6][7][8][9]}. IC50 & Target:Ki: 2.3 nM (A₁), 790 nM (A_2A), 43 nM(A₃)^[1]. In Vitro:N6-Cyclopentyladenosine (100 μM, 12-24 h) decreases viability of HL-60 cells and increases the number of apoptotic HL-60 cells^[3].
In Vivo:N6-Cyclopentyladenosine (200 nmol/kg; i.p.; single dose; 22 h before 5-fluorouracil administration) protects the hematopoietic progenitor cells (CFC-GM) in the bone marrow from the cytotoxic damage of 5-fluorouracil (HY-90006) in the 5-fluorouracil-induced hematopoietic damage model of B10CBAF₁ mice^[4]. N6-Cyclopentyladenosine (1 mg/kg; i.p.) suppresses rapid eye movement (REM) sleep and enhances electroencephalographic slow wave activity during non-rapid eye movement (NREM) sleep in rats^[5]. N6-Cyclopentyladenosine (0.15-2.25 μmol/kg; i.p.; single dose; 30 min before training) impairs the memory retention of passive avoidance tasks in mice in a dose-dependent manner in the mouse passive avoidance behavior experiment^[6]. N6-Cyclopentyladenosine (2-4 mg/kg; i.p.; single dose; 15 min before aminophylline administration) delays the onset of aminophylline-induced clonic convulsions in the mouse model of aminophylline-induced recurrent generalized seizures, but cannot prevent the death of mice within 24 h^[9].