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. 2017 Jan 29;32(1):588–599. doi: 10.1080/14756366.2017.1279156

Table 3.

General pharmacological screening of compound 7b and milrinone (M).

Test Dose (mg/kg) or Conc. (μg/mL) Considered parameter Significant criterion 7b M Additional reference druga
MTD and Irwin testb p.o. 300 Number animals (died/treated)   3/3 nt  
  100     3/3 3/3 (48h)  
  30     0/3 3/3 (48h)  
  i.p. 100     3/3 3/3  
  50     nt 3/3 (24h)  
  30     0/3 3/3 (48h)  
Blood pressure p.o. 30 Δ% after 1 and 4 h >10% −4/0 nt  
  10       −13/13  
  5       −3/−3  
Heart rate p.o. 30 Δ% after 1 and 4 h >20% +3/+5 +7/+8  
CHCl3 arrhythmia i.p. 30 N° protected animals/treated   1/3   Lidocaine: 3/3
  5   >1/3   0/3 Quinidine (100 mg/kg): 3/3
Inotropismc (in vitro) 10 Δ% >40% +56 +72 Trequinsin: +48
  3     +31 +60  
  0.5       +45
Chronotropism (in vitro) 10 Δ% >10 −23 nt Quinidine: −20; mecamylamine: −14
  5       +11  
  3     −10    
  2.5       +7  
  1     −3    
Saluresis p.o. 30 Urine Na+ μeq treated/control >2 4.5   Furosemide (5 mg/kg): 3.0
Triamterene (2.5 mg/kg): 2.6
  10     4.1 0.5  
  3     3.4    
Diuresis p.o. 30 Urine vol. treated/control >1.5 2.2 nt Amiloride (20 mg/kg): 1.6
Hydroflumethiazide (2.5 mg/kg): 1.7
  10     2.0 0.4  
  3     1.8    
Tracheal contractile tension (in vitro) 100 Relaxation (%) >50% nt 100  
  30     16 nt Theophylline: 60
  1.0     nt 50  
  0.5     nt 23  
Anti-inflammatory (paw edema) p.o. 100 Inhibition (%) >30% 42 nt Aspirin (150 mg/kg): 40
Phenylbutazone (50 mg/kg): 33
Hydrocortisone (25 mg/kg): 32
  30     34 nt  
  10     0 20  
Phenylquinone writhing p.o. 300 Writhing inhibition (%) >50% nt 42 Aspirin (50 mg/kg): 68
  30     60 nt  
  10     20 nt  
Formalin algesia p.o. 30 Licking time reduction (%) >50% 89 ntd  
  10     27    

nt: not tested.

a

When not otherwise specified, the drug reference dosage corresponds to that of column 2.

b

MTD: maximal tolerated dose; neither significant motor stimulation nor behavioral depression were observed.

c

Not blocked by propranolol.

d

Only compounds active in the writhing test were assayed.