1. Synthesis of [1,2,4]triazolo[1,5-a]pyrazines as adenosine A2A receptor antagonists.

    Bioorganic & Medicinal Chemistry Letters 15(21):4809 (2005) PMID 16153830

    Potent and selective antagonists of the adenosine A2A receptor often contain a nitrogen-rich fused-ring heterocyclic core. Replacement of the core with an isomeric ring system has previously been shown to improve target affinity, selectivity, and in vivo activity. This paper describes the prepar...
  2. Novel diamino derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.

    Journal of Medicinal Chemistry 48(6):2009 (2005) PMID 15771443

    Piperazine derivatives of 2-furanyl[1,2,4]triazolo[1,5-a][1,3,5]triazine have recently been demonstrated to be potent and selective adenosine A(2a) receptor antagonists with oral activity in rodent models of Parkinson's disease. We have replaced the piperazinyl group with a variety of linear, mo...
  3. Synthesis of [1,2,4]triazolo[1,5-a]pyrazines as adenosine A2Areceptor antagonists

    Bioorganic & Medicinal Chemistry Letters 15(21):4809 (2005)

    This paper describes the preparation, by a novel route, of A 2A receptor antagonists containing the [1,2,4]triazolo[1,5- a] pyrazine nucleus, which is isomeric with the [1,2,4]triazolo[1,5- c]pyrimidine core of a series of known A 2A antagonists with in vivo activity...
  4. Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists.

    Bioorganic & Medicinal Chemistry Letters 14(19):4835 (2004) PMID 15341934

    Piperazine derivatives of 2-furanyl[1,2,4]triazolo[1,5-a][1,3,5]triazine have recently been shown to be potent and selective adenosine A(2a) receptor antagonists. We now demonstrate that potent and selective A(2a) receptor antagonists could still be obtained when the arylpiperazines are separate...
  5. Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles.

    Bioorganic & Medicinal Chemistry Letters 14(19):4831 (2004) PMID 15341933

    Piperazine and (R)-2-(aminomethyl)pyrrolidine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine have recently been shown to be potent and selective adenosine A(2a) receptor antagonists. We have replaced the triazolotriazine core structure with two different heterocyclic cores. One of these, t...
  6. Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.

    Journal of Medicinal Chemistry 47(17):4291 (2004) PMID 15294001

    The [1,2,4]triazolo[1,5-a]triazine derivative 3, more commonly known in the field of adenosine research as ZM-241385, has previously been demonstrated to be a potent and selective adenosine A2a receptor antagonist, although with limited oral bioavailability. This [1,2,4]triazolo[1,5-a]triazine c...
  7. Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2areceptor antagonists

    Bioorganic & Medicinal Chemistry Letters 14(19):4835 (2004)

    Derivatives of triazolotriazine and triazolopyrimidine have been found to be potent and selective adenosine A 2a receptor antagonists with oral activity in the mouse catalepsy model.
  8. Studies on adenosine A2areceptor antagonists: comparison of three core heterocycles

    Bioorganic & Medicinal Chemistry Letters 14(19):4831 (2004)

    A comparison of the adenosine A 2a receptor antagonist activity of three heterocyclic series showed that the core deriving from [1,2,4]triazolo[1,5- a]triazine (X = N and Y = CH) afforded compounds with oral activity in the mouse catalepsy model.
  9. Multiple actions of systemic artemin in experimental neuropathy.

    Nature Medicine 9(11):1383 (2003) PMID 14528299

    The clinical management of neuropathic pain is particularly challenging. Current therapies for neuropathic pain modulate nerve impulse propagation or synaptic transmission; these therapies are of limited benefit and have undesirable side effects. Injuries to peripheral nerves result in a host of...