Basic Esters and Quaternary Derivatives of β-Hydroxy Acids as Antispasmodics<sup>1</sup>

Treves, Gino R.; Testa, Frank C.

doi:10.1021/ja01121a012

Cited by 10 publications

(4 citation statements)

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“…Five ocular mydriatics and cycloplegics are currently available [19]. Cyclopentolate was first synthesized in 1951 by Treves and Testa [20]. Cyclopentolate hydrochloride is a cholinolytic agent that blocks muscarinic acetylcholine receptors.…”

Section: Introductionmentioning

confidence: 99%

Study protocol: Accommodative effects on the musculoskeletal system

et al. 2023

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Accommodation is a phenomenon of the eyeball, which consists of adapting to view objects at different distances. The main aim of this study is to evaluate the effect of accommodations on the musculoskeletal system in myopic and emmetropic subjects. To date, the effect of accommodative paralysis on the musculoskeletal system has not been studied. The research hypothesis based on the current research reports is that accommodation affects the musculoskeletal system in myopic and emmetropic subjects. A smaller aim of the study is to evaluate the effect of unilateral accommodative palsy on the musculoskeletal system in myopic and emmetropic subjects. According to the authors of the previous reports, unilateral accommodative palsy will affect increased musculoskeletal asymmetry in myopic and emmetropic subjects. The surface electromyography (sEMG) of the musculoskeletal system will be performed by using the Noraxon Ultium DTS 8-K MR 3 myo Muscle Master Edition. Cycloftyal (10 mg/ml, eye drops, solution) will be used to paralyze accommodation. After the paralysis of unilateral accommodation, the test will be repeated. Both-sided accommodation will be paralyzed next, and the test will be repeated. The study may provide insight into the effects of accommodation on the musculoskeletal system, and it may also help in understanding the connections between these systems.

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Section: Introductionmentioning

confidence: 99%

Study protocol: Accommodative effects on the musculoskeletal system

et al. 2023

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“…This logic has prompted to synthesize derivatives of natural compounds and the structural analogues of biologically interesting substances with the "lead" (prototype) compound [10]. Many of the currently used antispasmodics [11][12][13][14] (dicyclomine, cyclopentolate, clidinium bromide, mebeverine, metoclopramide, tropicamide), antibiotics [15][16][17][18][19][20] (penicillins, cloxacillin, amoxacillin, ampicillin, cefadroxil, cefaclor, cefixime, cefepime), sulphonamides [21][22][23][24][25] (sulphacetamide, sulphadiazine, sulphasalazine, sulphamethoxazole), anthelmintics [26][27][28] (albendazole, mebedazole, pyrantel pamoate, piperazine, diethylcarbamazine citrate, praziquantel, niclosamide), antimycobacterials [29][30][31] (clofazimine, dapsone, ethambutol, isoniazid, benzothiazole, sulphonamide, rifampin), analgesics [32][33][34][35] (aspirin, diclofenac sodium, ibuprofen, indomethacin, ketoprofen, naproxen, piroxicam), anticonvulsants [36][37][38][39][40] (phenytoin, ethosuximide, carbamazepine, sodium valproate, riluzole), antitumours [41][42][43][44][45][46] (amsacrine, azacitidine, chlorambucil, cyclosporine, fluorouracil), diuretics [47][48]…”

Section: Introductionmentioning

confidence: 99%

Molecular Docking: Metamorphosis in Drug Discovery

Danao¹,

Nandurkar²,

Rokde³

et al. 2023

Biomedical Engineering

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Molecular docking is recognized a part of computer-aided drug design that is mostly used in medicinal chemistry. It has proven to be an effective, quick, and low-cost technique in both scientific and corporate contexts. It helps in rationalizing the ligands activity towards a target to perform structure-based drug design (SBDD). Docking assists the revealing of novel compound of therapeutic interest, forecasting ligand-protein interaction at a molecular basis and delineating structure activity relationships (SARs). Molecular docking acts as a boon to identify promising agents in emergence of diseases which endangering the human health. In this chapter, we engrossed on the techniques, types, opportunities, challenges and success stories of molecular docking in drug development.

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“…Cyclopentolate [2-(dimethylamino)ethyl 2-(1-hydroxycyclopentyl)-2-phenylacetate], 7 a competitive non-selective mAChR antagonist, 8–10 was synthesized by Teves and Testa in 1951. 11 It was used for the first time in the early 1950s, 12 , 13 and initially approved in 1953 by Schieffelin. 14 , 15…”

Section: Introductionmentioning

confidence: 99%

“…1,6 Cyclopentolate [2-(dimethylamino)ethyl 2-(1-hydroxycyclopentyl)-2-phenylacetate], 7 a competitive non-selective mAChR antagonist, [8][9][10] was synthesized by Teves and Testa in 1951. 11 It was used for the first time in the early 1950s, 12,13 and initially approved in 1953 by Schieffelin. 14,15 Nowadays, there are several marketed cyclopentolate formulations (0.2%, 0.5%, 1% or 2%) in different countries such as México (Refractyl, Laboratorios Sophia, 1963), Spain (Colircusí ciclopléjico, Alcon, 1965), 16 Canada (Cyclogyl, Alcon, 1972), 17 the United States (Cyclogyl, Alcon, 1974), 18 and the United Kingdom (Minims, Bausch & Lomb, 1987).…”

Section: Introductionmentioning

confidence: 99%

Ocular Cyclopentolate: A Mini Review Concerning Its Benefits and Risks

Contreras-Salinas¹,

Orozco-Ceja²,

Romero-López³

et al. 2022

OPTH

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Cycloplegic and mydriatic agents are essential in ophthalmological clinical practice since they provide the means for diagnosing and treating certain eye conditions. In addition, cyclopentolate has proven to possess certain benefits compared to other available cycloplegics and mydriatics. Still, the incidence of some adverse drug reactions related to this drug, especially in susceptible patients, has created interest in reviewing the literature about the benefits and risks of using cyclopentolate. A literature search was conducted in Medline/PubMed and Google Scholar, focusing on identifying cyclopentolate’s benefits and risks; the most important benefit was its usefulness for evaluating refractive errors, especially for hyperopic children, pseudomyopia, anterior uveitis, treatment of childhood myopia, idiopathic vision loss, and during examinations before refractive surgery, with particular advantages compared to other cycloplegics. While the risks were divided into local adverse drug reactions such as burning sensation, photophobia, hyperemia, punctate keratitis, synechiae, and blurred vision, which are relatively frequent but mild and temporary; and systemic adverse drug reactions such as language problems, visual or tactile hallucinations and ataxia, but unlike ocular, systemic adverse drug reactions are rare and occur mainly in patients with risk factors. In addition, six cases of abuse were found. The treatment with cyclopentolate is effective and safe in most cases; nevertheless, special care must be taken due to the potential severe ADRs that may occur, especially in susceptible patients like children, geriatrics, patients with neurological disorders or Down’s syndrome, patients with a low blood level of pseudocholinesterase, users of substances with CNS effects, and patients with a history of drug addiction. The recommendations are avoiding the use of 2% cyclopentolate and instead employing solutions with lower concentrations, preferably with another mydriatic such as phenylephrine. Likewise, the occlusion of the nasolacrimal duct after instillation limits the drug’s absorption, reducing the risk of systemic adverse events.

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Basic Esters and Quaternary Derivatives of β-Hydroxy Acids as Antispasmodics¹

Cited by 10 publications

References 0 publications

Study protocol: Accommodative effects on the musculoskeletal system

Study protocol: Accommodative effects on the musculoskeletal system

Molecular Docking: Metamorphosis in Drug Discovery

Ocular Cyclopentolate: A Mini Review Concerning Its Benefits and Risks

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Basic Esters and Quaternary Derivatives of β-Hydroxy Acids as Antispasmodics1

Cited by 10 publications

References 0 publications

Study protocol: Accommodative effects on the musculoskeletal system

Study protocol: Accommodative effects on the musculoskeletal system

Molecular Docking: Metamorphosis in Drug Discovery

Ocular Cyclopentolate: A Mini Review Concerning Its Benefits and Risks

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Product

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Basic Esters and Quaternary Derivatives of β-Hydroxy Acids as Antispasmodics¹