9 Potassium Channel Activators: Pharmacological Methods, Models, and Structure–Activity Relationships

Comparative Studies on the Relaxing Action of Several Adenosine 5'-Triphosphate-Sensitive K+ Channel Openers in Pig Urethra.

“…5B). Effects of the biologically-active (-)-enantiomer of cromakalim the biological activity (Hof et al, 1988 ;Evans et al, 1992). In the present experiments, the time course and amplitude of urethral relaxation evoked by the racemic mixture could be exactly mimicked by half the concentration of (-)-cromakalim.…”

“…The potency of (+)-cromakalim to activate KGS-43 pS was much openers to relax pig urethral smooth muscle can be accounted for by activation of gliben Introduction of the mechanisms involved in relaxation of smooth muscle and has led to the development and synthesis of a number of cromakalim derivatives (reviewed by Evans et al ., 1992). A wide…”

“…Phone : 092-642-6077, Fax : 092-642-6079 ; E-mail:noritera@linne.med.kyushu-u.ac.jp TERAMOTO et al cromakalim) in smooth muscle cells (reviewed by Kuriyama et al, 1995). It has become confined to the (-)-enantiomer (BRL 38227 or levcromakalim ; Hof et al, 1988 ;Edwards et al, 1991 ;Evans et al, 1992). Thus, the purified (-)-cromakalim has been the major form utilized in recent investigations on the mechanisms involved in smooth muscle relaxation (Edwards et al, 1991 ;Brading, 1996, 1997).…”

Structure-Activity Relationships of KATP Channel Openers

“…Opening of K ATP channels by KCOs hyperpolarizes the plasma membrane and reduces the cellular electrical excitability. KCOs exhibit chemical heterogeneity comprising as different structural classes [4][5][6][7][8] as the benzopyrans, cyanoguanidines, thioformamides, thiadiazines, cyclobutenediones, dihydropyridine-related structures, and tertiary carbinols.…”

Diazoxide in the treatment of schizophrenia: novel application of potassium channel openers in the treatment of schizophrenia*

“…In addition, with the characterization of potassium channel structure and function came the realization that some CNS disorders may be the result of potassium channel dysfunction. Consequently, a number of compounds have been identified that modulate potassium channels and it has been speculated that these could have been the result of the treatment of selected disorders including schizophrenia (22, 23). Diazoxide is a potassium channel opener from benzothiadiazine derivative related to the thiazide diuretics.…”