ReN-1869 hydrochloride (Synonyms: NNC-05-1869 hydrochloride)

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ReN 1869 hydrochloride is a novel, selective histamine H₁ receptor antagonist, which demonstrates affinity to the histamine H₁ receptor (guinea pig brain) with K_i of 0.19±0.04 μM and the non-selective σ site (guinea pig brain) with K_i of 0.45 μM.

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ReN-1869 hydrochloride Chemical Structure

CAS No. : 170149-76-5

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Description	ReN 1869 hydrochloride is a novel, selective histamine H₁ receptor antagonist, which demonstrates affinity to the histamine H₁ receptor (guinea pig brain) with K_i of 0.19±0.04 μM and the non-selective σ site (guinea pig brain) with K_i of 0.45 μM.
IC₅₀ & Target	Ki: 0.19±0.04 μM (histamine H₁ receptor)^[1]
In Vitro	ReN 1869 is a highly selective tricyclic antihistamine that shows functional histamine H₁ receptor antagonism. Binding studies with radioactively labelled ReN 1869 reveals high affinity only for the histamine H₁ receptor in addition to some affinity for a sigma site. ReN 1869 is profiled for activity at 10 μM at various receptors, transporters, enzymes and ion channels. ReN 1869 only demonstrates affinity to the histamine H1 receptor (guinea pig brain, [³H]pyrilamine) with a K_i of 0.19±0.04 μM and the non-selective σ site [guinea pig brain, [³H]1,3-di-tolylguanidine (DTG)] with a K_i of 0.45 μM. ReN 1869 dose-dependently reduces the responses with IC₅₀ of 1.70±0.002 μM^[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. ReN-1869 hydrochloride Related Antibodies
In Vivo	The in vivo binding of [³H]Mepyramine to mouse spinal cord and cerebellar histamine H₁ receptors is dose-dependently inhibited by ReN 1869. ReN 1869 (in doses as low as 10 μg/kg i.p.) significantly inhibits the histamine-evoked paw edema. The ED₅₀ is approximately 300 μg/kg. Interestingly, even a high dose of Mepyramine (10 mg/kg) is unable to inhibit significantly this type of edema (0.29±0.06 versus 0.34±0.05 in controls, n=7).ReN 1869 (1 mg/kg s.c.) is administered 30 min before paw injection with carrageenan and has no effect on the development of the paw edema. Dexamethasone (1 mg/kg s.c.) is given 1 h before carrageenan and expectedly diminished the edema. This effect is not affected by the simultaneous administration of 1 mg/kg ReN 1869^[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight	397.94
Formula	C₂₄H₂₈ClNO₂
CAS No.	170149-76-5
SMILES	O=C([C@H]1CN(CC/C=C2C3=CC=CC=C3CCC4=CC=CC=C\24)CCC1)O.[H]Cl
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (277 KB) Handling Instructions (2659 KB)
References	[1]. Olsen UB, et al. ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation. Eur J Pharmacol. 2002 Jan 18;435(1):43-57. [Content Brief]

Kinase Assay
^[1]

ReN 1869 is labelled with ³H in the tricyclic ring system resulting in a specific activity of 40 Ci/mmol. Thawed membranes (1 mg protein/tube), test compounds and [³H]ReN 1869 are added to test tubes in a final volume of 0.5 mL. Unless otherwise indicated, the concentration of the radioligand is 5 nM and non-specific binding is defined as the binding in the presence of 10 μM ReN 1869. Samples are incubated for 120 min at 37 °C in a shaking water bath. Free and bound radioactivity is separated by filtration over Whatman GF/F filters that are washed with 25 mL of ice-cold buffer (20 mM Tris-HCl, pH 7.4). Radioligand bound to filters accounted for 5-700 dpm that is subtracted before calculating specific binding^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Olsen UB, et al. ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation. Eur J Pharmacol. 2002 Jan 18;435(1):43-57. [Content Brief]

ReN-1869 hydrochloride Related Classifications

Inflammation/Immunology Endocrinology

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ReN-1869170149-76-5NNC-05-1869ReN1869ReN 1869Histamine ReceptorInhibitorinhibitorinhibit

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