Cimetidine - CAS 51481-61-9
Catalog number: 51481-61-9
Category: Inhibitor
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Molecular Formula:
C10H16N6S
Molecular Weight:
252.34
COA:
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Targets:
Histamine Receptor
Description:
Cimetidine, a histamine congener, competitively inhibits histamine binding to histamine H2 receptors.
Purity:
>98%
Synonyms:
SKF-92334; SKF 92334; SKF92334
MSDS:
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InChIKey:
AQIXAKUUQRKLND-UHFFFAOYSA-N
InChI:
InChI=1S/C10H16N6S/c1-8-9(16-7-15-8)5-17-4-3-13-10(12-2)14-6-11/h7H,3-5H2,1-2H3,(H,15,16)(H2,12,13,14)
Canonical SMILES:
CC1=C(N=CN1)CSCCNC(=NC)NC#N
1.The effects of cimetidine chronic treatment on conventional antiepileptic drugs in mice.
Świąder MJ1, Barczyński B2, Tomaszewski M2, Świąder K3, Czuczwar SJ4. Pharmacol Rep. 2016 Apr;68(2):283-8. doi: 10.1016/j.pharep.2015.09.009. Epub 2015 Oct 9.
PURPOSE: The aim of this study was to evaluate the effects of 1-day, 7-day and 14-day administrations of cimetidine on the anticonvulsant activity of conventional antiepileptic drugs (AEDs; valproate, carbamazepine, phenytoin and phenobarbital) against maximal electroshock (MES)-induced convulsions in mice.
2.Metformin and cimetidine: Physiologically based pharmacokinetic modelling to investigate transporter mediated drug-drug interactions.
Burt HJ1, Neuhoff S2, Almond L3, Gaohua L4, Harwood MD5, Jamei M6, Rostami-Hodjegan A7, Tucker GT8, Rowland-Yeo K9. Eur J Pharm Sci. 2016 Mar 25;88:70-82. doi: 10.1016/j.ejps.2016.03.020. [Epub ahead of print]
Metformin is used as a probe for OCT2 mediated transport when investigating possible DDIs with new chemical entities. The aim of the current study was to investigate the ability of physiologically-based pharmacokinetic (PBPK) models to simulate the effects of OCT and MATE inhibition by cimetidine on metformin kinetics. PBPK models were developed, incorporating mechanistic kidney and liver sub-models for metformin (OCT and MATE substrate) and a mechanistic kidney sub-model for cimetidine. The models were used to simulate inhibition of the MATE1, MATE2-K, OCT1 and OCT2 mediated transport of metformin by cimetidine. Assuming competitive inhibition and using cimetidine Ki values determined in vitro, the predicted metformin AUC ratio was 1.0 compared to an observed value of 1.46. The observed AUC ratio could only be recovered with this model when the cimetidine Ki for OCT2 was decreased 1000-fold or the Ki's for both OCT1 and OCT2 were decreased 500-fold.
3.Cimetidine as a novel adjunctive treatment for early stage Lyme disease.
Shemenski J1. Med Hypotheses. 2016 Apr 9. pii: S0306-9877(16)30007-X. doi: 10.1016/j.mehy.2016.03.015. [Epub ahead of print]
Lyme disease, caused by the spirochete Borrelia burgdorferi (Bb), is the most common vector-borne illness in the United States. It is a complex disease which may affect the skin, joints, heart, eyes, and central nervous system. Prompt diagnosis and treatment is curative in most instances. However, a significant percentage of patients experience ongoing symptoms after treatment. Currently, there is much controversy regarding the diagnosis, pathophysiology, and treatment of Lyme disease. Pathogen persistence despite treatment lies at the heart of this debate. Many believe that the ongoing symptoms are due to factors such as autoimmunity or permanent damage that is incurred during the active infection. However, there is an emerging school of thought that states that ongoing symptoms are due to a persistent infection that is able to survive both the immune response and antibiotic therapy. Numerous studies have shown that Bb can indeed persist within the host despite treatment and several mechanisms have been proposed to explain Bb's persistence capabilities.
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CAS 51481-61-9 Cimetidine

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