Clemastine - CAS 15686-51-8
Category: Inhibitor
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Molecular Formula:
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Histamine Receptor
Clemastine is a histamine H1 antagonist commonly used for the symptoms of allergic rhinitis, hay fever, and cold.
Brife Description:
histamine H1 antagonist
HS 592; HS-592; HS592; Meclastin; Mecloprodin; Clemastina; Tavist; Meclastine
Canonical SMILES:
1.Treatment of angiotensin receptor blocker-induced angioedema: A case series.
Strassen U1, Bas M1, Hoffmann TK2, Knopf A2, Greve J2. Laryngoscope. 2015 Jul;125(7):1619-23. doi: 10.1002/lary.25163. Epub 2015 Feb 3.
BACKGROUND: Angiotensin II receptor antagonists have been proposed as a replacement therapy after the occurrence of either an angiotensin converting enzyme (ACE) inhibitor-induced angioedema or cough. However, recent studies indicate that angioedema is associated with elevated bradykinin levels in a small fraction of patients treated with angiotensin-II-receptor blockers, suggesting a common pathophysiological mechanism. To date, a standard treatment for angiotensin II receptor blocker-induced angioedema does not exist.
2.Asymmetric synthesis of H1 receptor antagonist (R,R)-clemastine.
Lee SY1, Jung JW1, Kim TH1, Kim HD2. Arch Pharm Res. 2015 Dec;38(12):2131-6. doi: 10.1007/s12272-015-0641-4. Epub 2015 Jul 29.
The first asymmetric synthesis of (R,R)-clemastine (1) has been accomplished by the coupling of (R)-tertiary alcohol 2 and (R)-chloroethylpyrrolidine 3 via O-alkylation. (R)-Tertiary alcohol 2 was synthesized by stereoselective alkylation of chiral α-benzyloxy ketone with Grignard reagent via chelation-controlled 1,4-asymmetric induction. In the reaction, chiral benzyl group acts as a chiral auxiliary as well as a protecting group. (R)-Chloroethylpyrrolidine 3 was prepared by asymmetric transformation starting with L-homoserine lactone, in which racemization-minimized N-allylation and ring-closing metathesis were involved as key steps.
3.Synergy testing of FDA-approved drugs identifies potent drug combinations against Trypanosoma cruzi.
Planer JD1, Hulverson MA1, Arif JA1, Ranade RM1, Don R2, Buckner FS1. PLoS Negl Trop Dis. 2014 Jul 17;8(7):e2977. doi: 10.1371/journal.pntd.0002977. eCollection 2014.
An estimated 8 million persons, mainly in Latin America, are infected with Trypanosoma cruzi, the etiologic agent of Chagas disease. Existing antiparasitic drugs for Chagas disease have significant toxicities and suboptimal effectiveness, hence new therapeutic strategies need to be devised to address this neglected tropical disease. Due to the high research and development costs of bringing new chemical entities to the clinic, we and others have investigated the strategy of repurposing existing drugs for Chagas disease. Screens of FDA-approved drugs (described in this paper) have revealed a variety of chemical classes that have growth inhibitory activity against mammalian stage Trypanosoma cruzi parasites. Aside from azole antifungal drugs that have low or sub-nanomolar activity, most of the active compounds revealed in these screens have effective concentrations causing 50% inhibition (EC50's) in the low micromolar or high nanomolar range.
4.Clemastine Confers Neuroprotection and Induces an Anti-Inflammatory Phenotype in SOD1(G93A) Mouse Model of Amyotrophic Lateral Sclerosis.
Apolloni S1,2, Fabbrizio P2, Parisi C1, Amadio S2, Volonté C3,4. Mol Neurobiol. 2016 Jan;53(1):518-31. doi: 10.1007/s12035-014-9019-8. Epub 2014 Dec 9.
Mutations in the Cu(2+)/Zn(2+) superoxide dismutase 1 (SOD1) gene underlie 14-23 % of familial and 1-7 % of sporadic cases of amyotrophic lateral sclerosis (ALS), a progressive neurodegenerative disease characterized by a specific loss of motor neurons in the brain and spinal cord. Neuroinflammation and oxidative stress are emerging as key players in the pathogenesis of ALS, thus justifying the interest in glial cells and particularly microglia, in addition to motor neurons, as novel therapeutic approaches against ALS. Recently, histamine was proven to participate in the pathogenesis of neuroinflammatory and neurodegenerative diseases, and particularly, microglia was shown to be sensitive to the histamine challenge mainly through histamine H1 receptors. Clemastine is a first-generation and CNS-penetrant H1 receptor antagonist considered as a safe antihistamine compound that was shown to possess immune suppressive properties. In order to investigate if clemastine might find promising application in the treatment of ALS, in this work, we tested its action in the SOD1(G93A) mouse model which is extensively used in ALS preclinical studies.
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CAS 15686-51-8 Clemastine

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