Disease relevance of Sovcaine

• Tertiary amine local anesthetics, such as dibucaine and tetracaine, have been found to reversibly modify the blood-borne implantation and experimental metastatic properties of B16 melanoma cells in syngeneic C57BL/6 mice [1].
• The effect of colchicine and dibucaine on the morphogenesis of Semliki Forest virus [2].
• In contrast, dibucaine, a local anesthetic, greatly inhibited the formation of envelope dimers (E1-E2) in plasma membranes, but not in virus particles [3].
• Induction of apoptotic cell death in a neuroblastoma cell line by dibucaine [4].
• Pain relief of oral ulcer by dibucaine-film [5].

High impact information on Sovcaine

• Asp70 to Gly substitution characteristic of 'atypical' BCHE, failed to alter its Km towards BTCh or dibucaine binding but reduced hydrolytic activity to 25% of control [6].
• This release of fatty acids was partially inhibited by dibucaine, the phospholipase A2 inhibitor, which we have previously shown to protect mitochondria against damage associated with Ca2+ and reactive oxygen species [7].
• Structural difference at the active site of dibucaine resistant variant of human plasma cholinesterase [8].
• However, chlorpromazine, TMB 8, and dibucaine, which interfere with intracellular membrane transport of Ca2+, inhibited this platelet activation (change in LT, 14C-5HT release and TX synthesis [9].
• Extracellular Ca2+ chelation (EGTA) and PLA2 inhibitor therapy (aristolochic acid, dibucaine, or mepacrine) each conferred significant protective effects [10].

Chemical compound and disease context of Sovcaine

• In a 13-year-old girl, photoallergic dermatitis was caused by dibucaine hydrochloride, which was used as a local anesthetic in the treatment of her dental caries [11].
• Overexpression of regucalcin suppresses cell death and apoptosis in cloned rat hepatoma H4-II-E cells induced by lipopolysaccharide, PD 98059, dibucaine, or Bay K 8644 [12].
• Trifluoperazine (TFP) is a potent antipsychotic agent, dibucaine (DBC) is a local anaesthetic and praziquantel (PZQ) is a highly effective agent against schistosomiasis [13].
• The infectivity of herpes simplex virus type 1 (HSV-1) was found to be markedly reduced by treating virions with the tertiary amine local anesthetics lidocaine, dibucaine and tetracaine [14].
• Allergic contact dermatitis from dibucaine in Proctosedyl ointment without cross-sensitivity [15].

Biological context of Sovcaine

• Another type of substitution, that of Asp-74 by Gly or Asn, generated an active enzyme with increased resistance to succinylcholine and dibucaine; thus mimicking in an AChE molecule the phenotype of the atypical butyrylcholinesterase natural variant (D70G mutation) [16].
• Uptake of dibucaine into large unilamellar vesicles in response to a membrane potential [17].
• First, treatment of whole cells in a complete media with dibucaine caused precursor cleavage and product accumulation with kinetics that were consistent with previous morphologic observations on mucocyst formation [18].
• The stage of virus assembly inhibited by colchicine and dibucaine was studied by experiments with [3H]-leucine or [35S]methionine [2].
• [3H]Me-TRH binding was inhibited by classical local anesthetics with the order of potency (IC50 values): dibucaine (0.37 mM) greater than tetracaine (1.2 mM) greater than lidocaine (3.3 mM) greater than procaine and benzocaine (greater than 10 mM) [19].

Anatomical context of Sovcaine

• The protein composition of the microvesicles shed from aggregating platelets was similar to that of microvesicles shed by platelets in which the association of the membrane skeleton with the plasma membrane had been disrupted by incubation of platelets with dibucaine or ionophore A23187 [20].
• The effect of the local anesthetics SKF 525-A, dibucaine, tetracaine, procaine, and benzocaine on sarcoplasmic reticulum vesicles was studied [21].
• Colchicine (100 micron) disrupted the microtubles of the baby hamster kidney cells (BHK-21), whereas dibucaine did not alter microtubule polymerization [2].
• Isolation and genetic characterization of dibucaine-resistant variants of a mouse lymphocytic cell line [22].
• Interaction of dibucaine and calcium ion on a calcium pump reconstituted from defined components of intestinal brush border [23].

Associations of Sovcaine with other chemical compounds

• Membrane renewal after dibucaine deciliation of Tetrahymena. Freeze-fracture technique, cilia, membrane structure [24].
• METHODS: From a large group of healthy blood donors (n = 2609), we selected all the 58 individuals with low serum cholinesterase activity: among them 28 subjects had abnormal dibucaine and fluoride inhibition numbers [25].
• DNA damage induced by bleomycin in the presence of dibucaine is not predictive of cell growth inhibition [26].
• The relationship of calcium to receptor-controlled stimulation of phosphatidylinositol turnover. Effects of acetylcholine, adrenaline, calcium ions, cinchocaine and a bivalent cation ionophore on rat parotid-gland fragments [27].
• Tetrodotoxin and dibucaine significantly suppressed the ionomycin-evoked [3H]GABA release and ionomycin increased fluorescence intensity of bis-oxonol, suggesting the involvement of membrane depolarization in this release [28].

Gene context of Sovcaine

• Inhibition of Bax-induced cytochrome c release from neural cell and brain mitochondria by dibucaine and propranolol [29].
• Treatment of human platelets with A23187 and dibucaine, activators of calpain, caused cleavage of actin-binding protein and talin in a time-dependent manner [30].
• Unusual results for dibucaine inhibition led to the recognition of a new allele (E1k) also segregating in these families [31].
• For dibucaine, the enthalpy of transfer was smaller with delta H approximately -2 kcal/mol but was still about one-third of the total free energy change [32].
• [3H]PCP binding was inhibited by chlorpromazine (IC50 = 6.3 x 10(-5)M), tetracaine (IC50 = 4.2 x 10(-6)M), and dibucaine (IC50 = 2.7 x 10(-4)M) [33].

Analytical, diagnostic and therapeutic context of Sovcaine

• Fourth, one-dimensional peptide mapping of the 45-kilodalton product confirmed that the post-translationally derived product in whole cell pulse-chase experiments was similar to the purified products in the cortex fraction and in dibucaine-released mucus [18].
• Membrane-free trichocyst contents were isolated by density gradient centrifugation; they are converted from the contracted to the expanded state by Dibucain, CTMAB and CPC, and also by exogenous ATPase (Apyrase) [34].
• A water-soluble three-layered oral mucosa-adhesive film made from hydroxypropyl cellulose containing dibucaine (0.25 mg of drug/cm(2)) was designed for alleviation of severe pain due to oral ulcers, caused by chemotherapy and/or radiotherapy [5].
• Locations of local anesthetic dibucaine in model membranes and the interaction between dibucaine and a Na+ channel inactivation gate peptide as studied by 2H- and 1H-NMR spectroscopies [35].
• LDH leakage was markedly suppressed by perfusion at 25 degrees C or with 0.1 mM dibucaine or 2 mM lidocaine [36].

References