Introduction: The δ opioid receptor mediates various pharmacological effects such as antinociceptive and antidepressant effects, whereas it does not appear to induce μ opioid-like side effects such as dependence, respiratory depression and constipation. Therefore, the δ opioid receptor is a promising drug target. Areas covered: This review covers literature and patents concerning non-peptidic δ opioid receptor agonists, antagonists, modulators and ligands from 2000 to 2012. Pharmacological effects induced by δ receptor agonists or antagonists are also discussed. Expert opinion: Potential therapeutic effects by δ receptor agonists are antinociceptive, antidepressant, anxiolytic, cardioprotective and neuroprotective effects. Among them, anxiolytic effects are of particular interest because the anxiolytic effects by a δ receptor agonist have been observed in humans. Although non-peptidic δ receptor agonists were reported to show convulsive effects via the δ opioid receptor, some δ receptor agonists are known...

Non-peptidic δ opioid receptor agonists and antagonists (2000 – 2012)

The invention belongs to the field of medicine synthesis, and provides a 1-benzyl-6-carbomethoxy methyl tetrahydroisoquinoline derivative, a preparation method and an application in resisting aggregation of thrombocyte, and particularly relates to a novel 1-substituted-benzyl-N-alkyl (acyl)-6-carbomethoxy methyl-7-methoxyl-1,2,3,4-tetrahydroisoquinoline derivative as shown in the formula (see the specification), a preparation method and an application for resisting the aggregation activity of the thrombocyte. According to the derivative, the in-vitro thrombocyte aggregation-resisting activity is tested by virtue of a Born turbidimetry, a test result shows that the derivative has the thrombocyte aggregation resisting activity, and the activity is obviously higher than positive reference clopidogrel sulfate. The nitrogen decoration of the 1-benzyl-6-carbomethoxy methyl tetrahydroisoquinoline derivative is favorable for improving the thrombocyte aggregation resisting activity. The 1-benzyl-6-carbomethoxy methyl tetrahydroisoquinoline derivative can be used for further preparing an antithrombus drug and has a good practical value and application prospect.

1-benzyl-6-carbomethoxy methyl tetrahydroisoquinoline derivative, preparation method and application in resisting aggregation of thrombocyte

Compounds of general formula (I) wherein D, E, R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.

1,2,3,4-Tetrahydroisoquinoline Derivatives, Preparations Thereof and Uses Thereof

The title compound, C4H2Cl2N4O2, is a key intermediate in the synthesis of a purine scaffold, as nucleophilic substitution of the chlorides allows access to a diverse array of potentially biologically active compounds. The mol­ecules exhibit an intramolecular N—H⋯O hydrogen bond between the ortho amino and nitro substituents. Pairs of mol­ecules associate across a crystallographic centre of symmetry through N—H⋯N intermolecular hydrogen bonding between the ortho amino group and the ring N atom.

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4-Amino-2,6-dichloro-5-nitropyrimidine

The title compound, C7H10ClN5O2, was synthesized as part of a study to demonstrate the reactivity of 4-amino-2,6-di­chloro-5-nitro­pyrimidine with respect to various amine substitutions. The structure determination allowed unambiguous assignment of the regioselectivity of the substitution of the propyl­amine group at the 6-position. Intra- and intermolecular N—H⋯O and N—H⋯N hydrogen bonding yields polymeric chains of coplanar mol­ecules. There are two independent molecules in the asymmetric unit.

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Christian Oliver Janssen

Papers

1,2,3,4-Tetrahydroisoquinoline Derivatives, Preparations Thereof and Uses Thereof

4-Amino-2,6-dichloro-5-nitropyrimidine

4-Amino-2-chloro-5-nitro-6-(propylamino)pyrimidine