Cholinesterase inhibition by phenothiazine and nonphenothiazine antihistaminics: Analysis of its postulated role in synergizing organophosphate toxicity
Several antihistaminic compounds inhibit in vitro pseudocholinesterase (ChE) from several sources (human, rat, or horse plasma), pI50 ranging from 5.0 to 6.0. This inhibition is competitive with acetylcholine (ACh) and is reversible. Acetylcholinesterase (AChE) from rat brain was nonsensitive to ant...
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| Formato: | Capítulo de libro |
| Lenguaje: | Inglés |
| Publicado: |
1975
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| LEADER | 08864caa a22011657a 4500 | ||
|---|---|---|---|
| 001 | PAPER-18693 | ||
| 003 | AR-BaUEN | ||
| 005 | 20230518205004.0 | ||
| 008 | 190411s1975 xx ||||fo|||| 00| 0 eng|d | ||
| 024 | 7 | |2 scopus |a 2-s2.0-0016610747 | |
| 024 | 7 | |2 cas |a chlorpheniramine, 132-22-9; cholinesterase, 9001-08-5; dichlorvos, 62-73-7; dimenhydrinate, 523-87-5; diphenhydramine 8 bromotheophyllinate, 3427-80-3; diphenhydramine, 147-24-0, 58-73-1; mepyramine maleate, 59-33-6; mepyramine, 6036-95-9, 91-84-9; proadifen, 302-33-0, 62-68-0; promazine, 53-60-1, 58-40-2; promethazine, 58-33-3, 60-87-7; tripelennamine, 154-69-8, 91-81-6; Cholinesterase Inhibitors; Cholinesterases, EC 3.1.1.8; Dichlorvos, 62-73-7; Diphenhydramine, 58-73-1; Histamine H1 Antagonists; Organophosphorus Compounds; Phenothiazines; Proadifen, 302-33-0 | |
| 040 | |a Scopus |b spa |c AR-BaUEN |d AR-BaUEN | ||
| 030 | |a TXAPA | ||
| 100 | 1 | |a Fernández, G. | |
| 245 | 1 | 0 | |a Cholinesterase inhibition by phenothiazine and nonphenothiazine antihistaminics: Analysis of its postulated role in synergizing organophosphate toxicity |
| 260 | |c 1975 | ||
| 270 | 1 | 0 | |m Fernández, G.; Cátedra de Toxicología y Química Legal, Facultad de Ciencias Exactas, Ciudad Universitaria de Nunez, Buenos Aires, Argentina |
| 506 | |2 openaire |e Política editorial | ||
| 504 | |a Arterberry, Bonifaci, Nash, Quinby, Potentiation of phosphorus insecticides by phenothiazine derivatives (1962) JAMA, 182, pp. 110-112 | ||
| 504 | |a Augustinsson, Cholinesterase A study in comparative enzymology (1948) Acta Physiologica Scandinavica, 15, p. 1 | ||
| 504 | |a Augustinsson, Cholinesterase: A study in comparative enzymology (1948) Acta Physiol. Scand., 15, pp. 448-472 | ||
| 504 | |a Augustinsson, Butyryl and propionyl cholinesterases and related types of eserine sensitive esterases (1960) The Enzymes, 4, pp. 521-540. , P. Boyer, H. Lardy, K. Myrbäck, Academic Press, New York | ||
| 504 | |a Benstz, Effect of synthetic hibernatory substances on serum and erythrocyte cholinesterase and circulation (1956) Klin. Wochenschr., 34, pp. 796-798 | ||
| 504 | |a Bernsohn, Namajuska, Cochrane, The effect of chlorpromazine on respiration and glycolysis in rat brain (1956) Archives of Biochemistry and Biophysics, 62, pp. 274-283 | ||
| 504 | |a Bonomolo, Mariani, Action of Largactil on the cholinesterase activity of nervous tissue (1955) Riv Neurol, 25, pp. 824-828 | ||
| 504 | |a Castro, Effects of alkylating agents on human plasma cholinesterase. The role of sulfhydryl groups in its active center (1968) Biochem. Pharmacol., 17, pp. 295-303 | ||
| 504 | |a Courvoisier, Fournel, Ducrot, Kolsky, Koetsche, The pharmacology of 3-chloro-10-(3-dimethylaminopropyl)phenothiazine. A substance which potentiates anesthetics and causes hibernation (1953) Arch. Int. Pharmacodyn. Ther., 92, pp. 305-361 | ||
| 504 | |a Da Cruz, Action of chlorpromazine on blood phosphatase and cholinesterase activity (1955) C. R. Soc. Biol. Paris, 149, pp. 1829-1831 | ||
| 504 | |a Díaz Gómez, Castro, Studies on the interaction between inhibitors of drug metabolism and horse plasma cholinesterase (1971) Biochem. Pharmacol., 20, pp. 929-942 | ||
| 504 | |a Engelhard, Prchal, Neuner, Acetylcholinesterase (1967) Angew. Chem., 6, pp. 615-626 | ||
| 504 | |a Erdös, Baert, Shanor, Foldes, The inhibitory effect of chlorpromazine and chlorpromazine sulfoxide on human cholinesterase (1958) Arch Int Pharmacodyn Ther, 117, pp. 163-167 | ||
| 504 | |a Fried, Antopol, Effects of psychotomimetic compounds on human pseudocholinesterase (1957) J Appl Physiol, 11, pp. 25-28 | ||
| 504 | |a Gordon, N-(Diethylaminoethyl)phenothiazine, a specific inhibitor of pseudocholinesterase (1948) Nature (London), 162, p. 146 | ||
| 504 | |a Johanneson, Lausen, Chlorpromazine as an inhibitor of brain cholinesterase (1961) Acta Pharmacologica et Toxicologica, 18, pp. 398-406 | ||
| 504 | |a Kalckar, Shafran, Differential spectrophotometry of purine compounds by means of specific enzymes. III. Studies of the enzymes of purine metabolism (1947) J. Biol. Chem., 167, pp. 461-475 | ||
| 504 | |a Kingsbury, Organo-phosphorus esters and phenothiazines acting synergistically as antihelmintics (1961) Res. Vet. Sci., 2, pp. 265-271 | ||
| 504 | |a Lineweaver, Burk, Determination of enzyme dissociation constants (1934) J. Amer. Chem. Soc., 56, pp. 658-666 | ||
| 504 | |a Maickel, Diverse central effects of chlorpromazine (1968) Int. J. Neuropharmacol., 7 (1), pp. 23-27 | ||
| 504 | |a Michel, Electrometric method for determination of red blood cell and plasma cholinesterase activity (1949) J. Lab. Clin. Med., 34, pp. 1564-1568 | ||
| 504 | |a Simon, Winter, The effect of antihistaminics on red blood cell acetylcholinesterase activity in vitro (1970) Biochem. Pharmacol., 19 (5), pp. 1843-1845 | ||
| 504 | |a Todrick, The inhibition of cholinesterases by antagonist of acetylcholine and histamine (1954) Br J Pharmacol Chemother, 9, pp. 76-83 | ||
| 504 | |a Usdin, Su, Usdin, Effects of psychotropic compounds on enzyme systems. I. Inhibition of human plasma and erythrocyte cholinesterases (1961) Proc. Soc. Exp. Biol. Med., 108, pp. 457-460 | ||
| 504 | |a Vincent, Acetylcholine and synthetic antihistaminics in dog experiments (1950) C. R. Soc. Biol. Paris, 144, pp. 148-158 | ||
| 504 | |a Webb, (1963) Enzyme and Metabolic Inhibitors, , Academic Press, New York | ||
| 520 | 3 | |a Several antihistaminic compounds inhibit in vitro pseudocholinesterase (ChE) from several sources (human, rat, or horse plasma), pI50 ranging from 5.0 to 6.0. This inhibition is competitive with acetylcholine (ACh) and is reversible. Acetylcholinesterase (AChE) from rat brain was nonsensitive to antihistaminics even at a concentration of 4 mm. Antihistaminics do not compete with either organophosphates or quaternary ammonium compounds in inhibiting ChE. Inhibition of ChE by antihistaminics is more pronounced at alkaline pH values than at acidic or neutral pH. Administration of promethazine ip to rats at a dose of 50 mg/kg resulted in a 90% inhibition of ChE 1 hr later, while the AChE was totally nonsensitive to the inhibitor even when the dose of the antihistamine was doubled. Results were analyzed in relation to the postulated role of ChE inhibition in antihistaminic potentiation of organophosphorus intoxication. © 1975. |l eng | |
| 593 | |a Cátedra de Toxicología y Química Legal, Facultad de Ciencias Exactas, Ciudad Universitaria de Nunez, Buenos Aires, Argentina | ||
| 593 | |a Laboratorio de Química, Biotoxicológica, CITEFA, Zufriátegui y Varela, Villa Martelli, Pcia. de Buenos Aires, Argentina | ||
| 690 | 1 | 0 | |a ANTIHISTAMINIC AGENT |
| 690 | 1 | 0 | |a CHLORPHENIRAMINE |
| 690 | 1 | 0 | |a CHOLINESTERASE |
| 690 | 1 | 0 | |a CHOLINESTERASE INHIBITOR |
| 690 | 1 | 0 | |a DICHLORVOS |
| 690 | 1 | 0 | |a DIMENHYDRINATE |
| 690 | 1 | 0 | |a DIPHENHYDRAMINE |
| 690 | 1 | 0 | |a DIPHENHYDRAMINE 8 BROMOTHEOPHYLLINATE |
| 690 | 1 | 0 | |a MEPYRAMINE |
| 690 | 1 | 0 | |a MEPYRAMINE MALEATE |
| 690 | 1 | 0 | |a ORGANOPHOSPHATE |
| 690 | 1 | 0 | |a PHENOTHIAZINE DERIVATIVE |
| 690 | 1 | 0 | |a PROADIFEN |
| 690 | 1 | 0 | |a PROMAZINE |
| 690 | 1 | 0 | |a PROMETHAZINE |
| 690 | 1 | 0 | |a TRIPELENNAMINE |
| 690 | 1 | 0 | |a BRAIN |
| 690 | 1 | 0 | |a DRUG POTENTIATION |
| 690 | 1 | 0 | |a DRUG TOXICITY |
| 690 | 1 | 0 | |a ENVIRONMENTAL HEALTH |
| 690 | 1 | 0 | |a HORSE |
| 690 | 1 | 0 | |a HUMAN |
| 690 | 1 | 0 | |a INTOXICATION |
| 690 | 1 | 0 | |a NORMAL HUMAN |
| 690 | 1 | 0 | |a PESTICIDE POISONING |
| 690 | 1 | 0 | |a RAT |
| 690 | 1 | 0 | |a THEORETICAL STUDY |
| 690 | 1 | 0 | |a ANIMAL |
| 690 | 1 | 0 | |a CHOLINESTERASE INHIBITORS |
| 690 | 1 | 0 | |a CHOLINESTERASES |
| 690 | 1 | 0 | |a DICHLORVOS |
| 690 | 1 | 0 | |a DIPHENHYDRAMINE |
| 690 | 1 | 0 | |a DRUG SYNERGISM |
| 690 | 1 | 0 | |a FEMALE |
| 690 | 1 | 0 | |a HISTAMINE H1 ANTAGONISTS |
| 690 | 1 | 0 | |a HORSES |
| 690 | 1 | 0 | |a HUMAN |
| 690 | 1 | 0 | |a IN VITRO |
| 690 | 1 | 0 | |a ORGANOPHOSPHORUS COMPOUNDS |
| 690 | 1 | 0 | |a PHENOTHIAZINES |
| 690 | 1 | 0 | |a PROADIFEN |
| 690 | 1 | 0 | |a RATS |
| 653 | 0 | 0 | |a dramamine; pyrilamine; skf 525 a |
| 700 | 1 | |a Díaz Gómez, M.I. | |
| 700 | 1 | |a Castro, JosA. | |
| 773 | 0 | |d 1975 |g v. 31 |h pp. 179-190 |k n. 2 |p Toxicol. Appl. Pharmacol. |x 0041008X |w (AR-BaUEN)CENRE-35 |t Toxicology and Applied Pharmacology | |
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| 856 | 4 | 0 | |u https://hdl.handle.net/20.500.12110/paper_0041008X_v31_n2_p179_Fernandez |y Handle |
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| 999 | |c 79646 | ||