Biphalin

Biphalin is a dimeric enkephalin endogenous peptide (Tyr-D-Ala-Gly-Phe-NH)2 composed of two tetrapeptides derived from enkephalins, connected 'tail-to-tail' by a hydrazide bridge. The presence of two distinct pharmacophores confers on biphalin a high affinity for both mu and delta opioid receptors, therefore it has analgesic activity. It has been shown that biphalin presents a considerable antinociceptive profile. The extraordinary in vivo potency shown by this compound is coupled with low side-effects, in particular reduced gastrointestinal motility.

History

Biphalin was first synthesized in 1982 by scientists at the University of Arizona. It was developed as a potential new treatment for pain, with the aim of creating a drug that had the analgesic properties of morphine but without the addictive side effects.

Pharmacology

Biphalin is a potent analgesic, significantly more potent than morphine. It acts as an agonist at both the mu and delta opioid receptors, but has a higher affinity for the delta receptor. This dual action is thought to be responsible for its powerful analgesic effect.

Clinical use

Biphalin is not currently used in clinical practice, but it has been the subject of research due to its potential as a new type of painkiller. Studies have shown that it has a strong analgesic effect in animals, and it is hoped that it could be used to treat severe pain in humans in the future.

See also

• Enkephalin
• Opioid receptor
• Analgesic

References

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