17124-82-2
Chemical Structure
Nordimaprit
- CAS. Nr.: 17124-82-2
- Formula:C5H13N3S
- Molecular Weight:147.24
IUPAC Name: 2-(dimethylamino)ethyl carbamimidothioate
InChIKey: MUYRPUKYVOXLSN-UHFFFAOYSA-N
SMILES: N=C(SCCN(C)C)N
Biological Activity: Nordimaprit is a reversible, non-competitive H3 receptor antagonist with a pKi value of 5.94. Nordimaprit exhibits essentially no activity against H1 receptors and only weak agonistic activity against H2 receptors. Nordimaprit induces selective chemotaxis of eosinophils in rabbit eyes, triggering severe eosinophilic uveitis and ocular symptoms such as corneal edema, opacity, and inflammation. Nordimaprit reduces melanin content and inhibits tyrosinase activity, and exerts toxic effects on melanoma cells. Nordimaprit can be used in studies related to anterior uveitis and melanoma[1][2][3][4].
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Nordimaprit | Nordimaprit is a reversible, non-competitive H3 receptor antagonist with a pKi value of 5.94. Nordimaprit exhibits essentially no activity against H1 receptors and only weak agonistic activity against H2 receptors. Nordimaprit induces selective chemotaxis of eosinophils in rabbit eyes, triggering severe eosinophilic uveitis and ocular symptoms such as corneal edema, opacity, and inflammation. Nordimaprit reduces melanin content and inhibits tyrosinase activity, and exerts toxic effects on melanoma cells. Nordimaprit can be used in studies related to anterior uveitis and melanoma. | |||||||||||||||||||||
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References
- [1]. Mindel JS, et al. Eosinophil chemotaxis and anterior uveitis from topical dimaprit and nordimaprit. Investigative ophthalmology & visual science. 1986 Oct;27(10):1504-11.
- [2]. Kathmann M, et al. Nordimaprit, homodimaprit, clobenpropit and imetit: affinities for H3 binding sites and potencies in a functional H3 receptor model. Naunyn-Schmiedeberg's archives of pharmacology. 1993 Nov;348(5):498-503.
- [3]. Fechner GA, et al. Inhibition of melanogenesis in human melanoma cells by novel analogues of the partial histamine (H2) agonist nordimaprit. Biochemical pharmacology. 1993 Jul 06;46(1):47-54.
- [4]. Dale MM, et al. A comparison of dimaprit, nordimaprit, methylamine and chloroquine as inhibitors of mitogen-induced lymphocyte activation. British journal of pharmacology. 1984 Sep;83(1):293-8.
