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ZD 7288 is an inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channel [1].

The HCN channel is found in the sinoatrial node (SAN) and is permeable to both Na+ and K+. The HCN current exists in neurons under hyperpolarization of the cell membrane and plays an important role in neuropathic pain [1].

In CA1 pyramidal cells from Wistar rats, ZD 7288 inhibited T-type Ca2+ channel currents in a concentration-dependant way [2]. In neonatal rat facial motoneurones, ZD-7288 (0.1-10 μM) inhibited the hyperpolarisation-activated current with IC50 value of 0.2 μM in a time- and voltage-dependent way [3]. In CA1 pyramidal neurons, ZD 7288 (1-1000 μM) inhibited the hyperpolarization-activated current. However, ZD 7288 had no influence on long-term depression (LTD) of the CA3-CA1 synapse [4].

In rats with chronic visceral pain, ZD 7288 (50-100 nM) significantly inhibited abdominal withdrawal reflex (AWR) scores and electromyographic (EMG) responses. Also, ZD 7288 significantly increased pain thresholds. These results suggested that spinal HCN channels might play a critical role in chronic visceral pain [1].

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