Nylidrin hydrochloride - CAS 849-55-8
Catalog number: 849-55-8
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C19H26NO2Cl
Molecular Weight:
335.87
COA:
Inquire
Targets:
Adrenergic Receptor
Description:
Nylidrin hydrochloride is a beta-adrenergic agonist. It was an effective inhibitor of IgE-mediated release of histamine from passively sensitized rat peritoneal mast cells and human basophils, and of IgG1-mediated release of histamine from passively sensitized guinea pig lung slices. It causes peripheral vasodilation, a positive inotropic effect, and increases gastric volume of gastric juice. It is used in the treatment of peripheral vascular disorders and premature labor. It also can be used as antiallergic agent. It is one of the FDA approved drug as Inhibitors of the Human Sodium Taurocholate Cotransporting Polypeptide (NTCP).
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Purity:
95%
Appearance:
Off-White Solid
Synonyms:
1-p-Hydroxyphenyl-2-(1’-methyl-3’-phenylpropylamino)-1-propanolhydrochloride;Arlidin hydrochloride;Buphenine hydrochloride;Dilatol hydrochloride;p-Hydroxy-alpha-(1-((1-methyl-3-phenylpropyl)amino)ethyl)-benzylalcohohyd;Suprifenpsb hydrochloride;4-[1-hydroxy-2-(4-phenylbutan-2-ylamino)propyl]phenol;hydrochloride;Dilatyl
Solubility:
DMSO:38mg/mL
Storage:
Hygroscopic, -20˚C Freezer, Under Inert Atmosphere
MSDS:
Inquire
Application:
Nylidrin hydrochloride is used in the treatment of peripheral vascular disorders and premature labor. It also can be used as antiallergic agent.
Quality Standard:
USP standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams-Kilos
Melting Point:
198-199 °C (decomp)
InChIKey:
CLJHABUMMDMAFA-UHFFFAOYSA-N
InChI:
InChI=1S/C19H25NO2.ClH/c1-14(8-9-16-6-4-3-5-7-16)20-15(2)19(22)17-10-12-18(21)13-11-17;/h3-7,10-15,19-22H,8-9H2,1-2H3;1H
Canonical SMILES:
CC(CCC1=CC=CC=C1)NC(C)C(C2=CC=C(C=C2)O)O.Cl
1.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Tamiz AP1, Whittemore ER, Zhou ZL, Huang JC, Drewe JA, Chen JC, Cai SX, Weber E, Woodward RM, Keana JF. J Med Chem. 1998 Aug 27;41(18):3499-506.
A series of bis(phenylalkyl)amines, structural analogues of ifenprodil and nylidrin, were synthesized and tested for antagonism of N-methyl-D-aspartate (NMDA) receptors. Potency and subunit selectivity were assayed by electrical recordings in Xenopus oocytes expressing three binary combinations of cloned rat NMDA receptor subunits: NR1A expressed in combination with either NR2A, NR2B, or NR2C. The bis(phenylalkyl)amines were selective antagonists of NR1A/2B receptors. Assayed under steady-state conditions, the most potent of these, N-[2-(4-hydroxyphenyl)ethyl]-5-phenylpentylamine hydrochloride (20), has an IC50 value of 8 nM and >1000-fold selectivity with respect to NR1A/2A and NR1A/2C receptors. The structure-activity relationship of the bis(phenylalkyl)amine series indicates that the piperidine ring and alkyl chain substitutions common to NR2B-selective antagonists such as ifenprodil, CP 101,606, and Ro 25-6981 are not necessary to generate potent and selective ligands.
2.Age-related macular degeneration and nutritional supplementation: a review of randomised controlled trials.
Bartlett H1, Eperjesi F. Ophthalmic Physiol Opt. 2003 Sep;23(5):383-99.
Age-related macular degeneration (AMD) is the leading cause of severe vision loss in the developed world. The lack of effective treatment modalities, coupled with evidence supporting an oxidative pathogenesis, has increased interest in the potential preventative role of nutritional supplementation. This article reviews seven randomised controlled trials (RCTs) that have investigated the role of nutritional supplementation in AMD. Three of these trials reported a positive effect of nutritional supplementation on AMD; the Age-related eye study (AREDS), the Lutein Antioxidant Supplementation Trial (LAST), and the oral zinc trial by Newsome et al. (1988). However, the oral zinc trial by Newsome et al. (1988) was unlikely to detect any difference between treatments smaller than 72%, and the AREDS results were based on a subgroup of their study population. Lutein was considered for the AREDS formulation, but was not commercially available at that time.
3.[Clinical trial on the effect of buphenine, aminophenazone and diphenylpyraline hydrochloride in treating the common cold in children of 6 to 24 months of age].
Montijo-Barrios E1, Cadena F, Ramírez-Mayans JA, Gutiérrez-Castrellón P. Rev Invest Clin. 2011 Jul-Aug;63(4):335-43.
INTRODUCTION: Acute respiratory infections are the second leading cause of morbidity in children under 18 years. Several drugs have been used with variable efficacy and safety, trying to reduce the associated symptoms and improve quality of life.
4.[3H]ifenprodil binding to NMDA receptors in porcine hippocampal brain membranes.
Höfner G1, Wanner KT. Eur J Pharmacol. 2000 Apr 14;394(2-3):211-9.
(+/-)-2-(4-Benzylpiperidino)-1-(4-hydroxyphenyl)propan-1-ol ([3H]ifenprodil) binding to a subcellular fraction of porcine hippocampus, which was obtained by centrifugation on a discontinuous sucrose gradient, was investigated with the objective to label selectively the ifenprodil recognition site of native NMDA receptors. Saturation experiments revealed high-affinity sites for [3H]ifenprodil in this membrane fraction which could be characterised by a K(d) value of 23.0+/-1.8 nM using a one-site model. Calculation of saturation isotherms on the basis of a two-site model yielded a K(d1) value of 10.4+/-2.4 nM and a K(d2) value of 2200+/-1300 nM, respectively. Inhibition of [3H]ifenprodil binding by NR2B subunit-selective NMDA receptor antagonists, by polyamines, by sigma receptor ligands, by a variety of ligands acting at different NMDA receptor recognition sites and by several cations was studied and compared with the effects of these compounds on (5R,10S)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5, 10-imine ([3H]MK-801) binding under non-equilibrium conditions.
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CAS 849-55-8 Nylidrin hydrochloride

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