136647-02-4

UK 78282 Hydrochloride is used in the synthetic preparation of N-arylalkylpiperidine and -pyrrolidine derivatives for treating irritable bowel syndrome.

UK-78282 blocks both Kv1.3 and Kv1.4. Kv1.3 and Kv1.4 are members of the Shaker family of voltage-gated potassium channels. Kv1.3 is expressed in brain and in effector memory T (Tem) cellsand Kv1.4 is expressed in brain. Both channels are involved in setting the membrane potential of neurons. In additionKv1.3 maintains the membrane potential for T memory cells and is up-regulated upon T cell activationcontributing to multiple immune processes and disorders. Blockers of Kv1.3 have long been sought for therapeutic benefitand they are also valuable tools for studying the immune system. Selective blockers of Kv1.4 are desiredas there are few if any currently available. UK-78282 is valuable for immune system studieswhere the absence of Kv1.4 makes it functionally selective for Kv1.3and it has shown suppression of T cell activation. UK-78282 is also valuable for the study of Kv1.4 function.

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