TY - JOUR
T1 - Ro 5-4864 has a negative inotropic effect on human atrial muscle strips that is not antagonized by PK 11195
AU - Shany, Eilon
AU - Hochhauser, Edith
AU - Halpern, Pinchas
AU - Vidne, Bernardo
AU - Gavish, Moshe
AU - Geller, Eran
AU - Hasharoni, Amir
AU - Barak, Yaakov
AU - Yakirevich, Vladimir
PY - 1994/3/3
Y1 - 1994/3/3
N2 - The effects of Ro 5-4864, a peripheral benzodiazepine receptor agonist (9 × 10-6 M and 9 × 10-5 M) and of PK 11195, a peripheral benzodiazepine receptor antagonist (3 × 10-6 M and 3 × 10-5 M), alone or together, on contraction parameters of human atrial muscle strips were studied. Atrial muscle strips were obtained from patients undergoing cardiac surgery. The strips were suspended in Krebs-Henseleit solution at 36.8±0.2°C, connected to an isometric force transducer and then stimulated at 15 V above threshold and paced at 1.5 Hz. Ro 5-4864 at its higher concentration, alone or mixed with PK 11195 at both concentrations, depressed the contraction amplitude to 80% of the control value (P < 0.05). In conclusion, Ro 5-4864 had a small but significant depressant effect on the contraction amplitude of human atrial strips. Surprisingly, this effect was not reversed by the peripheral benzodiazepine receptor antagonist PK 11195.
AB - The effects of Ro 5-4864, a peripheral benzodiazepine receptor agonist (9 × 10-6 M and 9 × 10-5 M) and of PK 11195, a peripheral benzodiazepine receptor antagonist (3 × 10-6 M and 3 × 10-5 M), alone or together, on contraction parameters of human atrial muscle strips were studied. Atrial muscle strips were obtained from patients undergoing cardiac surgery. The strips were suspended in Krebs-Henseleit solution at 36.8±0.2°C, connected to an isometric force transducer and then stimulated at 15 V above threshold and paced at 1.5 Hz. Ro 5-4864 at its higher concentration, alone or mixed with PK 11195 at both concentrations, depressed the contraction amplitude to 80% of the control value (P < 0.05). In conclusion, Ro 5-4864 had a small but significant depressant effect on the contraction amplitude of human atrial strips. Surprisingly, this effect was not reversed by the peripheral benzodiazepine receptor antagonist PK 11195.
KW - Muscle strip
KW - PK 11195
KW - Peripheral benzodiazepine
KW - Ro 5-4864
KW - human
UR - http://www.scopus.com/inward/record.url?scp=0028269105&partnerID=8YFLogxK
U2 - 10.1016/0014-2999(94)90196-1
DO - 10.1016/0014-2999(94)90196-1
M3 - Article
AN - SCOPUS:0028269105
SN - 0014-2999
VL - 253
SP - 231
EP - 236
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
IS - 3
ER -