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GC-MS Analysis of Methanolic Extract of Rubus ellipticus
Published in Parimelazhagan Thangaraj, Phytomedicine, 2020
Elizabeth George, Blassan P. George, Sajeesh Thankarajan, Parimelazhagan Thangaraj, Kasipandi Muniyandi, Saikumar Sathyanarayanan
The compound 3-piperidinecarboxamide, N,N-diethyl, inhibits the secretion of prolactin and growth hormones and reverses levodopa-induced dyskinesias in Parkinsonian monkeys (Cabergoline Basic information 2008). Moreover, anti-teratogenic effects of tumor inhibitors and analgesic properties were shown by [2-(4-hydroxy-phenyl)-ethyl]-carbamic acid ethyl ester. (The mass spectra of compounds identified through GC-MS are provided in Figure 6.2). However, there are many other unknown compounds in the chromatogram which need to be further identified.
Cholinergic Agonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Rupali Patil, Aman Upaganlawar
It is a carbamic acid ester and a substrate for AChE forming a relatively stable carbamoylated intermediate with the enzyme which then becomes reversibly inactivated. This results in the potentiation of cholinergic activity throughout the body (Harvey et al., 2011). Methyl carbamate of an amine-substituted phenol is an essential moiety of the physostigmine (Brunton, 2011).
Mechanisms of action
Published in Fazal-I-Akbar Danish, Ahmed Ehsan Rabbani, Pharmacology in 7 Days for Medical Students, 2018
Fazal-I-Akbar Danish, Ahmed Ehsan Rabbani
Physostigmine: It is a reversible anticholinesterase. Chemically it is a carbamic acid ester and a substrate for acetylcholinesterase. The action of acetylcholinesterase on this drug results in the formation of a relatively stable carbamoylated intermediate with the enzyme, which thus becomes inactive. This in turn leads to prolongation of acetylcholine action on cholinoceptors throughout the body. The duration of action of physostigmine is about 2–4 hours.
Electrophysiological study of the interactive role of the cannabinoid breakdown inhibitors and L-type calcium channels on granular neurons in the hippocampal dentate gyrus in rats
Published in Neurological Research, 2022
Seyed Asaad Karimi, Fatemeh Kazemi, Hamidreza Komaki, Masoumeh Kourosh Arami, Siamak Shahidi, Alireza Komaki
A potent and selective inhibitor of FAAH, URB597 (carbamic acid, N-cyclohexyl-, 3′-(aminocarbonyl) [1,1′-biphenyl]-3-yl ester) (Sigma, USA), and verapamil, as a blocker of Ca2+channels (Sigma, Germany) were used. The vehicle for the control group included 0.9% normal saline (sodium chloride (NaCl)) and dimethyl sulfoxide (DMSO) provided from Sigma Co., USA. The chemicals were freshly administered by intraperitoneal injection (i.p) at a concentration of 0.1 ml per 100 g of animal’s body weight. The DMSO volume regarding both drugs was less than 10%, which was employed by saline as the vehicle. The daily i.p injection of verapamil hydrochloride or its vehicle was done at the concentrations of 10, 25, or 50 mg/kg for 13 days [25–29]. Following obtaining the steady-state baseline response for LTP recording, URB597 or its vehicle was injected intraperitoneally at 0.1 or 0.3 mg/kg.
Pyrethroid based pesticides – chemical and biological aspects
Published in Critical Reviews in Toxicology, 2021
Anandha Rao Ravula, Suresh Yenugu
CAs are derived from carbamic acid and the first one among this class, carbaryl, was introduced in 1956 as a lawn and garden insecticide. Its broad-spectrum insect control activity and low toxicity to mammals allowed it to be a preferred choice. CAs are less persistent in the environment unlike OPs and OCs and are rapidly detoxified in animal tissues. The mode of action of CAs is similar to that of OPs as both are inhibitors of acetylcholinesterase (AChE). While CAs inhibit AChE activity by phosphorylation resulting in the formation of a reversible complex, OPs form an irreversible complex (Darvesh et al. 2008). Since CAs are considered to be safer than OPs, as they exhibit reversible action on AChE and do not cause severe poisoning in cholinergic pathway (Silva et al. 2013), they are proposed as therapeutic drugs (physostigmine derived from Physostigma venenosum) for neuromuscular disorders such as myasthenia gravis.
In vitro phase I metabolism of vinclozolin by human liver microsomes
Published in Xenobiotica, 2019
Marycarmen Cruz-Hurtado, Ma de Lourdes López-González, Victor Mondragón, Adolfo Sierra-Santoyo
In rats, Vin is efficiently metabolized by first undergoing a non-enzymatic hydrolysis to generate 2-[[(3,5-dichlorophenyl)-carbamoyl]oxy]-2-methyl-3-butenoic acid (M1) and 3',5'-dichloro-2-hydroxy-2-methylbut-3-enanilide (M2) metabolites (Sierra-Santoyo et al., 2004; Szeto et al., 1989). Regarding phase I metabolism, Vin is metabolized to at least seven metabolites by reactions catalyzed by the cytochrome P450 (CYP) 2A, 2B and 3A subfamilies (Sierra-Santoyo et al., 2012). Vin is metabolized to [3-(3,5-dichlorophenyl)-5-methyl-5-(1,2-dihydroxyethyl)-1,3-oxazolidine-2,4-dione] (M4) and N-(2,3,4-trihydroxy-2-methyl-1-oxo)-3,5-dichlorophenyl-1-carbamic acid (M7) metabolites; these products are unstable in physiological conditions and are finally converted to 3′,5′-dichloro-2,3,4-trihydroxy-2-methylbutyranilide (DTMBA, formerly denoted as M5 metabolite) (Figure 1). DTMBA represents the main metabolic product of Vin present in organs and tissues, except in the adipose tissue, and may also be formed from M2 metabolite (Sierra-Santoyo et al., 2008). Bursztyka et al. (2008), proposed that M1 is hydroxylated in its ethylene group to form a metabolite designated as M6 and converted to DTMBA via ring closure to form M4. The 3,5-dichloroaniline (M3) metabolite formation has been reported as a product not NADPH-dependent from M2, however, it may not represent an important metabolite in mammals (Sierra-Santoyo et al., 2012). With respect to phase II metabolism, glucuronide- and sulfate-DTMBA and M4 conjugates have been reported as the main Vin metabolites excreted in urine (Bursztyka et al., 2008; Cruz-Hurtado et al., 2018; Rathahao-Paris et al., 2014).