trans-Triprolidine hydrochloride - CAS 550-70-9
Category: Inhibitor
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Molecular Formula:
C19H22N2.HCl
Molecular Weight:
314.86
COA:
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Targets:
Histamine Receptor
Description:
Trans-Triprolidine hydrochloride is a potent histamine H1 receptor antagonist with anticholinergic properties. Triprolidine is used for the treatment and prevention of allergy.
Brife Description:
histamine H1 receptor antagonist
Purity:
≥99% by HPLC
Related CAS:
486-12-4 (free base)
Appearance:
White to Off-White Solid
Synonyms:
295 C 51, Actidil, Actidilat, Entra, Pro-Actidil, Pro-Entra, Triprolidine HCl, Triprolidine hydrochloride, Triprolidine hydrochloride anhydrous, Venen; (E)-2-[1-(4-Methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl]pyridine hydrochloride; Triprolidine hydrochloride
MSDS:
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Application:
antihistaminic agent
Melting Point:
111-113°C
InChIKey:
WYUYEJNGHIOFOC-NWBUNABESA-N
InChI:
InChI=1S/C19H22N2.ClH/c1-16-7-9-17(10-8-16)18(19-6-2-3-12-20-19)11-15-21-13-4-5-14-21;/h2-3,6-12H,4-5,13-15H2,1H3;1H/b18-11+;
Canonical SMILES:
CC1=CC=C(C=C1)C(=CCN2CCCC2)C3=CC=CC=N3.Cl
1.Target-independent prediction of drug synergies using only drug lipophilicity.
Yilancioglu K1, Weinstein ZB, Meydan C, Akhmetov A, Toprak I, Durmaz A, Iossifov I, Kazan H, Roth FP, Cokol M. J Chem Inf Model. 2014 Aug 25;54(8):2286-93. doi: 10.1021/ci500276x. Epub 2014 Aug 1.
Physicochemical properties of compounds have been instrumental in selecting lead compounds with increased drug-likeness. However, the relationship between physicochemical properties of constituent drugs and the tendency to exhibit drug interaction has not been systematically studied. We assembled physicochemical descriptors for a set of antifungal compounds ("drugs") previously examined for interaction. Analyzing the relationship between molecular weight, lipophilicity, H-bond donor, and H-bond acceptor values for drugs and their propensity to show pairwise antifungal drug synergy, we found that combinations of two lipophilic drugs had a greater tendency to show drug synergy. We developed a more refined decision tree model that successfully predicted drug synergy in stringent cross-validation tests based on only lipophilicity of drugs. Our predictions achieved a precision of 63% and allowed successful prediction for 58% of synergistic drug pairs, suggesting that this phenomenon can extend our understanding for a substantial fraction of synergistic drug interactions.
2.Priapism, an emerging complication in β-thalassemia intermedia patients.
Mallat NS1, Wehbe D, Haddad A, Cappellini MD, Marcon A, Koussa S, Abboud MR, Radwan A, Taher AT. Hemoglobin. 2014;38(5):351-4. doi: 10.3109/03630269.2014.960087.
The increase in survival rate of β-thalassemia (β-thal) patients allowed for the appearance and manifestation of several complications in almost every organ system. Priapism in β-thal patients is rarely reported in the literature. We herein report and investigate the occurrence of two cases of priapism in two young patients with β-thal intermedia (β-TI). The potential mechanisms are due to either a cellular mechanism involving a thrombus obstructing the efferent venules of the corpora cavernosa leading to priapism, or a recently elucidated functional mechanism that causes alteration of nitric oxide (NO) response of the penis, ultimately causing priapism. This should incite clinicians for a close follow-up and monitoring of high risk patients who are susceptible to developing priapism.
3.Effect of premedications in a murine model of asparaginase hypersensitivity.
Fernandez CA1, Smith C1, Karol SE1, Ramsey LB1, Liu C1, Pui CH1, Jeha S1, Evans WE1, Finkelman FD1, Relling MV2. J Pharmacol Exp Ther. 2015 Mar;352(3):541-51. doi: 10.1124/jpet.114.220780. Epub 2015 Jan 8.
A murine model was developed that recapitulates key features of clinical hypersensitivity to Escherichia coli asparaginase. Sensitized mice developed high levels of anti-asparaginase IgG antibodies and had immediate hypersensitivity reactions to asparaginase upon challenge. Sensitized mice had complete inhibition of plasma asparaginase activity (P = 4.2 × 10(-13)) and elevated levels of mouse mast cell protease 1 (P = 6.1 × 10(-3)) compared with nonsensitized mice. We investigated the influence of pretreatment with triprolidine, cimetidine, the platelet activating factor (PAF) receptor antagonist CV-6209 [2-(2-acetyl-6-methoxy-3,9-dioxo-4,8-dioxa-2,10-diazaoctacos-1-yl)-1-ethyl-pyridinium chloride], or dexamethasone on the severity of asparaginase-induced allergies. Combining triprolidine and CV-6209 was best for mitigating asparaginase-induced hypersensitivity compared with nonpretreated, sensitized mice (P = 1.2 × 10(-5)). However, pretreatment with oral dexamethasone was the only agent capable of mitigating the severity of the hypersensitivity (P = 0.
4.Functional pharmacology of H1 histamine receptors expressed in mouse preoptic/anterior hypothalamic neurons.
Tabarean IV1. Br J Pharmacol. 2013 Sep;170(2):415-25. doi: 10.1111/bph.12286.
BACKGROUND AND PURPOSE: Histamine H1 receptors are highly expressed in hypothalamic neurons and mediate histaminergic modulation of several brain-controlled physiological functions, such as sleep, feeding and thermoregulation. In spite of the fact that the mouse is used as an experimental model for studying histaminergic signalling, the pharmacological characteristics of mouse H1 receptors have not been studied. In particular, selective and potent H1 receptor agonists have not been identified.
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CAS 550-70-9 trans-Triprolidine hydrochloride

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