Muscarinic receptors are altered by sulfhydryl reagents. Arsenic compounds, which have been used as insecticides, exert their toxic effects by combining with sulfhydryl groups. We compared the action of arsenicals and other sulfhydryl reagents on the muscarinic receptor from invertebrate and vertebrate species (locust and rat). Disulfide-reducing reagents dithiothreitol (DTT) and British Anti-Lewisite (BAL), but not arsenicals, inhibited [3H]quinuclidinyl benzilate ([3H]QNB) binding. However, after disulfide reduction, arsenicals caused a further inhibition of muscarinic binding. The effect of DTT + arsenicals was largely irreversible. The locust receptors were more sensitive to the action of both disulfide reagents either in the absence or presence of arsenicals than the rat receptors. The sulfhydryl reagent p-chloromercuric benzoate (PCMB) was more effective at inhibiting the locust receptors than the rat receptors, but addition of arsenicals did not cause further inhibition in either the locust or rat receptors. In locust, DTT + cacodylate and DTT + arsenite caused a reduction in the number of sites without modifying the affinity of [3H]QNB binding. In rat, DTT + arsenite caused a decrease in the affinity, while DTT + cacodylate caused a decrease in the affinity of [3H]QNB binding and its number of sites. Competition experiments after DTT + cacodylate showed that the IC50 and the Hill coefficient (nH) remained unchanged in the locust. In the rat, the IC50 for atropine was increased without alteration in the nH, and both parameters were increased for carbachol. These results are explained assuming that the binding site of the locust receptor has a disulfide group similar to that of the mammalian receptor, but that the hydrophobic interactions within the binding site are weaker in the locust receptor. The higher sensitivity of the insect receptor to sulfhydryl reagents could be of interest for developing methods of pest control.

01 Sep 1984·The Journal of cell biologyQ1 · BIOLOGY

Identification and extraction of proteins that compose the triad junction of skeletal muscle.

Q1 · BIOLOGY

Article

Author: Caswell, Anthony H. ; Brunschwig, J. P.

Treatment of both transverse tubules and terminal cisternae with a combination of Triton X-100 and hypertonic K cacodylate causes dissolution of nonjunctional proteins and selective retention of membrane fragments which are capable of junction formation. Treatment of vesicles with Triton X-100 and either KCl or K gluconate causes complete dissolution of all components. Therefore K cacodylate exerts a specific preservative action on the junctional material. The membrane fragment from treatment of transverse tubules with Triton X-100 + cacodylate contains a protein of Mr = 80,000 in SDS gel electrophoresis as the predominant protein while lipid composition is enriched in cholesterol. The membrane fragment retains in electron microscopy the trilaminar appearance of the intact vesicles. Freeze fracture of transverse tubule fragments reveals a high density of low-profile, intercalated particles, which frequently form strings or occasional small arrays. The fragments from Triton X-100 plus cacodylate treatment of terminal cisternae include the protein of Mr = 80,000 as well as the spanning protein of the triad, calsequestrin, and some minor proteins. The fragments are almost devoid of lipid and display an amorphous morphology suggesting membrane disruption. The ability of the transverse tubular fragment, which contains predominantly the Mr = 80,000 protein, to form junctions with terminal cisternae fragments suggests that it plays a role in anchoring the membrane to the junctional processes of the triad. The junctional proteins may be solubilized in a combination of nonionic detergent and hypertonic NaCl. Subsequent molecular sieve chromatography gives an enriched preparation of the spanning protein. This protein has subunits of Mr = 300,000, 270,000 and 140,000 and migrates in the gel as a protein of Mr = 1.2 X 10(6) indicating a polymeric structure.

01 Jan 1980·Dermatology

Treatment of Verruca plana with 5% 5-FIuorouraciI Ointment

Article

Author: Chun, Soo Il ; Kim, Joong-Gie ; Lee, Sungnack

11 patients with verruca plana were treated with 5% 5-Fluorouracil ointment as a twice daily topical application with open dressing. The patients were chosen among those who failed to be cured with various topical agents such as salicylic acid, vitamin A acid and dinitrochlorobenzene (DNCB), or even with carbon dioxide cryotherapy, oral administration of methotrexate and intramuscular injection of sodium cacodylate. In 9 patients, all the treated warts completely disappeared within 3–5 weeks. 2 of these patients had recurrence after 3 weeks and 2 months, respectively. In 2 patients, some lesions disppeared while others failed to be healed. The major clinical adverse reactions were hyperpigmentation (8 cases), erythema (5 cases) and erosion (5 cases).

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Indication	Country/Location	Organization	Date
Skin Diseases, Eczematous	CN	Tianjin Jinyao Pharmaceutical Co., Ltd.	-

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