| Identification | Back Directory | [Name]
NS 1738 | [CAS]
501684-93-1 | [Synonyms]
NS 1738
NSC 213859
1-(5-Chloro-2-hydroxy-phenyl)-3-(2-chloro-5-trifluoromethyl-phenyl)-urea
N-(5-Chloro-2-hydroxyphenyl)-N'-[2-chloro-5-(trifluoromethyl)phenyl]urea
Urea, N-(5-chloro-2-hydroxyphenyl)-N'-[2-chloro-5-(trifluoromethyl)phenyl]- | [Molecular Formula]
C14H9Cl2F3N2O2 | [MDL Number]
MFCD11100189 | [MOL File]
501684-93-1.mol | [Molecular Weight]
365.13 |
| Chemical Properties | Back Directory | [Boiling point ]
344.1±42.0 °C(Predicted) | [density ]
1.617±0.06 g/cm3(Predicted) | [storage temp. ]
Store at RT | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
White crystalline solid. | [pka]
8.08±0.13(Predicted) | [color ]
Off-White to Light Grey | [InChI]
1S/C14H9Cl2F3N2O2/c15-8-2-4-12(22)11(6-8)21-13(23)20-10-5-7(14(17,18)19)1-3-9(10)16/h1-6,22H,(H2,20,21,23) | [InChIKey]
OUDXRNQPVSMGDW-UHFFFAOYSA-N |
| Hazard Information | Back Directory | [Description]
NS 1738 is a positive allosteric modulator of the α7-containing neuronal nicotinic acetylcholine receptors (nAChRs). When applied in the presence of ACh, NS 1738 increases the peak amplitude of the current flowing through α7-containing nAChRs (EC50 = 3.4 μM). NS 1738 displays no substantial activity for α4β2-, α3β3-, and α1-containing receptors. It is modestly brain-penetrant and counteracts (-)-scopolamine-induced deficit in acquisition of a water-maze learning task in rats. NS 1738 also improves performance in the rat social recognition test. NS 1738 is used to selectively evaluate the role of α7-containing nAChRs in signaling pathways. | [Uses]
NS 1738 is a selective a7 nAchR allosteric modulator. | [Biological Activity]
Selective positive allosteric modulator of α 7 nicotinic acetylcholine receptors. Exhibits no substantial activity for α 4 β 2, α 3 β 3 and α 1-containing receptors. Displays cognitive-enhancing properties in vivo . | [in vivo]
To estimate the ability of NS 1738 to permeate the blood-brain barrier, rats are administered 10 mg/kg NS 1738 intraperitoneally. Peak brain concentrations are measured approximately 30 min after injection, and they amount to ~80 ng/mL (~200 nM) at this dose. The ratio between the amount of compound entering the brain and that in plasma is AUCbrain /AUCplasma=0.50. The half-life in plasma is estimated to 42 min. Incubation of NS1738 with isolated liver microsomes in vitro indicates that approximately 60 and 75% of NS 1738 is metabolized via the cytochrome P450 system in mouse and rat, respectively, within 1 h. Adult rats administered NS 1738 at 10 and 30 mg/kg i.p. immediately following the initial exposure to a juvenile rat (T1) display significant decreases in the investigative duration of a subsequent exposure to the same juvenile (T2) 2 h later (T2/T1 ratio of 0.69±0.13 and 0.61±0.07, respectively)[1]. | [storage]
Store at RT | [References]
[1] DANIEL B TIMMERMANN. An allosteric modulator of the alpha7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo.[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 323 1: 294-307. DOI: 10.1124/jpet.107.120436
[2] QING CHENG Jerrel L Y. Presynaptic α7 nicotinic acetylcholine receptors enhance hippocampal mossy fiber glutamatergic transmission via PKA activation.[J]. Journal of Neuroscience, 2014: 124-133. DOI: 10.1523/jneurosci.2973-13.2014
[3] KELEN FREITAS M I D F Ivy Carroll. The antinociceptive effects of nicotinic receptors α7-positive allosteric modulators in murine acute and tonic pain models.[J]. Journal of Pharmacology and Experimental Therapeutics, 2013, 344 1: 264-275. DOI: 10.1124/jpet.112.197871 |
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