Abstract:
:The blocking action of recently synthesized benzothiazolamine derivative R56865 was compared with that of dihydropyridine (nimodipine) and diphenylalkylamine (flunarizine) on low-voltage-activated and non-inactivating high-voltage-activated Ca2+ currents. The experiments were carried out on freshly isolated Purkinje neurons of rat cerebellum using patch-clamp technique in the whole-cell configuration. Among the substances tested R56865 was found to be the most effective blocker of the Ca2+ current. In the sequence R56865, flunarizine and nimodipine, apparent Kd values for low-voltage-activated current are 0.1, 0.9 and 3.5 microM, and for high-voltage-activated current 3.1, 9.5 and 38 microM, respectively. The current-voltage relationships for both types of currents displayed little or no shift under either flunarizine or R56865 but showed a 10-mV shift in the positive direction under the action of nimodipine. The steady-state inactivation curves for low-voltage-activated calcium currents were shifted under the action of R56865, flunarizine and nimodipine (in concentrations which blocked 50-60% of the current) to more negative membrane potentials for 20, 10 and 6 mV, respectively. In contrast to R56865, flunarizine blocked both types of Ca2+ channel in a use-dependent manner. It is concluded that the order of potency of Ca2+ antagonist for both types of channels studied is R56865 > flunarizine > nimodipine. Strong shift of steady-state inactivation relationship by R56865 can further facilitate its blocking action in in vivo conditions.
journal_name
Neurosciencejournal_title
Neuroscienceauthors
Panchenko VA,Krishtal OA,Tegtmeier F,Tsyndrenko AYadoi
10.1016/0306-4522(93)90230-dsubject
Has Abstractpub_date
1993-06-01 00:00:00pages
587-94issue
3eissn
0306-4522issn
1873-7544pii
0306-4522(93)90230-Djournal_volume
54pub_type
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