A-134974 dihydrochloride hydrate (C15-1315-014)

Biochem/physiol Actions

A-134974 is a novel and selective adenosine kinase (AK) inhibitor with IC₅₀ = 60 pM. Systemic A-134974 (i.p.) dose dependently reduced hyperalgesia (ED₅₀= 1 μmol/kg) and at higher doses, reduced locomotor activity (ED₅₀ = 16 μmol/kg). Administration of A-134974 intrathecally (i.t.) was more potent (ED₅₀= 6 nmol) at producing antihyperalgesia than delivering the compound by intracerebralventricular (ED₅₀ = 100 nmol, i.c.v.) or intraplantar (ED₅₀ >300 nmol) routes. In contrast, i.c.v. administration of A-134974 was more effective in reducing locomotor activity than i.t. administration (ED₅₀ values were 1 and >100 nmol, respectively). Increasing the pretreatment time for i.t.-delivered A-134974 caused a greater reduction in locomotor activity (ED₅₀= 10 nmol). This was due to diffusion of A-134974 (i.t.) to supraspinal sites. These data demonstrate that the novel AK inhibitor A-134974 potently reduces thermal hyperalgesia primarily through interactions with spinal sites, whereas its ability to depress locomotor activity is predominantly mediated by supraspinal sites.

Features and Benefits

This compound was developed by Abbott. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Legal Information

Sold under license from Abbott Laboratories.

Molecular Weight: 448.09 (anhydrous basis). Empirical Formula: C₁₁H₁₄IN₅O₂ · 2HCl · xH₂O. Quality Level: 100. Assay: ≥. 98% (HPLC). form: solid. storage condition: desiccated. color: off-white to light tan. solubility: H₂O: soluble. originator: Abbott. SMILES string: O.Cl.Cl.N[C@H]1C[C@H]([C@H](O)[C@@H]1O)n2cc(I)c3c(N)ncnc23. InChI: 1S/C11H14IN5O2.2ClH.H2O/c12-4-2-17(6-1-5(13)8(18)9(6)19)11-7(4)10(14)15-3-16-11. . . /h2-3,5-6,8-9,18-19H,1,13H2,(H2,14,15,16). 2*1H. 1H2/t5-,6+,8+,9-. . . /m0.../s1. InChI key: INMLNTBMPNIKQK-HWZUHWJPSA-N. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable. Personal Protective Equipment: Eyeshields, Gloves, type N95 (US).