Disease relevance of HE-NECA

• The A2a agonist 2-hexynyl-5'-N-ethylcarboxamidoadenosine induced dose-related hypotension (eg, 0.003 mg/kg; peak, -36 mm Hg; time to peak, 0.32 hour) with reflex tachycardia (eg, 0.003 mg/kg; peak, 152 bpm; time to peak, 0.35 hour) [1].

High impact information on HE-NECA

• In the adenylyl cyclase assays the A2A receptor agonists, HE-NECA and NECA, increased cyclic AMP accumulation in untreated human neutrophils with an EC50 value of 43 (40 - 47) and 255 (228 - 284) nM, respectively [2].
• 2. ZM241385 was nearly equipotent to displace [3H]CGS21680 (30 nM) binding to hippocampal (Ki of 0.52 nM) and to striatal membranes (Ki of 0.35 nM), whereas HENECA was a more potent displacer of [3H]CGS21680 binding to striatal (Ki of 4.5 nM) than to hippocampal membranes (Ki of 19 nM) [3].
• A similar pattern of Fos-like immunoreactivity was obtained after administration of the A2A agonist HENECA (5 mg/kg) which displays higher selectivity for A2A receptors than CGS 21680 [4].
• NECA (10 micrograms/kg) and 2-hexynyl-NECA (10 micrograms/kg) decreased peak values for platelet accumulation by 35.3 +/- 6.9% and 52.5 +/- 5.9% and the area under curve values by 37.7 +/- 8.7% and 41.2 +/- 12.0%, respectively [5].
• Pharmacology of the new selective A2a adenosine receptor agonist 2-hexynyl-5'-N-ethylcarboxamidoadenosine [6].

Associations of HE-NECA with other chemical compounds

• The A2 adenosine receptor agonist HENECA did not produce ANF release [7].

Gene context of HE-NECA

• The pharmacological profile of 2-hexynyl-5'-N-ethylcarboxamidoadenosine (2HE-NECA, CAS 141018-30-6), a new selective A2a adenosine receptor agonist, was characterized [6].

References