Voltage-gated Na+ channels are a primary target for local anesthetics (LAs). Open or inactivated Na+ channels usually have a severalfold higher affinity for LAs than do resting channels. Hille's modulated receptor hypothesis attributed the changes in LA affinity to state-dependent alterations in the conformation of the LA receptor. We expressed wild-type and mutant rat skeletal muscle (mu1) Na+...

Ca2+ release mechanisms were studied in striated muscle from the walking legs of crabs using isometric tension recordings from isolated myofibrillar bundles. Caffeine-induced phasic contractions had properties consistent with Ca2+ release from a sarcoplasmic store, which could be optimally loaded in the presence of ATP at pCa 6.4­6.1. Ryanodine (10 µmol l-1) abolished the caffeine-ind...

BACKGROUND N-methyl-D-aspartate (NMDA)-receptor activation contributes to postoperative hyperalgesia. Studies in volunteers have shown that intravenous local anaesthetics (LAs) prevent the development of hyperalgesic pain states. One potential explanation for this beneficial effect is the inhibition of NMDA receptor activation. Therefore, we studied the effects of LA on NMDA receptor function. ...

Handheld Raman spectroscopy offers a rapid and mobile technique for determining drugs nondestructively. The further advantage analyzing drug products (DPs) thanks to its ability measure samples through packaging, thus preserving evidence integrity continuity. This research evaluated the use of handheld Fourier transform (FT)-Raman characterization street DPs (n = 254) diverse formulations. spec...

The asymmetric unit of the title complex, [Cu(C(2)H(8)N(2))(2)(H(2)O)(2)](C(8)H(8)NO(2))(2)·2H(2)O, contains one anion, one half-cation and one water mol-ecule. The Cu(II) atom in the [Cu(en)(2)(H(2)O)(2)](2+) cation (en is ethyl-enediamine) lies on an inversion centre. The four N atoms of the en ligands in the equatorial plane around the Cu(II) atom form a slightly distorted square-planar arra...

The title compound, [CuPd(CN)(4)(C(4)H(12)N(2))(2)](n), consists of one-dimensional chains. The Cu and Pd atoms are both located on centers of symmetry in an alternating array of [Cu(N-Eten)(2)](2+) (N-Eten = N-ethyl-ethylenediamine) and [Pd(CN)(4)](2-) units. The Pd-C distances of 1.991 (3) and 1.992 (3) Å are inter-mediate values compared with the analogous Ni(II) and Pt(II) complexes [Akitsu...

Effects of the tertiary amines, procaine and lidocaine, its quaternary derivative QX—314, and neutral benzocaine, on Na currents in internally perfused neuro-blastoma cells were studied using the suction-pipette voltage clamp technique (Kostyuk et al. 1975 ; Zubov et al. 1980). Neuroblastoma cells used were N18 A-l and NTR-1 subclones derived from C1300 line (Konobasova et al. 1981) and Neuro 2...