TY - JOUR
T1 - Anti-anxiety and sedative profile evaluation of imidazo[1,2-a]pyridine derivatives
AU - López-Martínez, Margarita
AU - Salgado-Zamora, Héctor
AU - San-Juan, Eduardo Ramírez
AU - Zamudio, Sergio
AU - Picazo, Ofir
AU - Campos, Maria Elena
AU - Naranjo-Rodriguez, Elia B.
PY - 2010/9
Y1 - 2010/9
N2 - (Table Presented) Three imidazo[1,2-a]pyridine-3-nitrosated (L-1, L-2, L-3) and a 3-formyl imidazo[1,2-a]-pyridine thiosemicarbazone (L-4) were synthesized and evaluated for their effects in the elevated plus maze, burying behavior test, rotarod performance, the horizontal wire test, and locomotor activity. L-2 and L-3 increased the percent time spent in the open arms of the plus maze at doses of 1 and 2 mg/kg without modifying the number of total entries. In addition, L-2 and L-3 (1 mg/kg) increased the number of open arm entries indicating anxiolytic-like activity at this dose. In the burying behavioral test, L-1 (2-8mg/kg), L-2 (8mg/kg), and L-3 (4 and 8mg/kg), induced a clear reduction in cumulative burying behavior, without modifying burying behavior latency, thus reducing experimental anxiety. In the rotarod test, L-1 and L-2 impaired rotarod performance only at the highest evaluated dose (64mg/kg) at which reduction of motor activity was observed and thereby no conclusions about myorelaxant effects can be proposed. All compounds showed a clear sedative effect and corresponding ED50 values were obtained. Results indicate that compounds L-1, L-2, and L-3 show a sedative and an anxiolytic profile.
AB - (Table Presented) Three imidazo[1,2-a]pyridine-3-nitrosated (L-1, L-2, L-3) and a 3-formyl imidazo[1,2-a]-pyridine thiosemicarbazone (L-4) were synthesized and evaluated for their effects in the elevated plus maze, burying behavior test, rotarod performance, the horizontal wire test, and locomotor activity. L-2 and L-3 increased the percent time spent in the open arms of the plus maze at doses of 1 and 2 mg/kg without modifying the number of total entries. In addition, L-2 and L-3 (1 mg/kg) increased the number of open arm entries indicating anxiolytic-like activity at this dose. In the burying behavioral test, L-1 (2-8mg/kg), L-2 (8mg/kg), and L-3 (4 and 8mg/kg), induced a clear reduction in cumulative burying behavior, without modifying burying behavior latency, thus reducing experimental anxiety. In the rotarod test, L-1 and L-2 impaired rotarod performance only at the highest evaluated dose (64mg/kg) at which reduction of motor activity was observed and thereby no conclusions about myorelaxant effects can be proposed. All compounds showed a clear sedative effect and corresponding ED50 values were obtained. Results indicate that compounds L-1, L-2, and L-3 show a sedative and an anxiolytic profile.
KW - Anxiety
KW - Behavioral tests
KW - Imidazo[1,2-a]pyridines
KW - Sedation
UR - http://www.scopus.com/inward/record.url?scp=77957198848&partnerID=8YFLogxK
U2 - 10.1002/ddr.20382
DO - 10.1002/ddr.20382
M3 - Artículo
SN - 0272-4391
VL - 71
SP - 371
EP - 381
JO - Drug Development Research
JF - Drug Development Research
IS - 6
ER -