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[edit | edit source]
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[edit | edit source]
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[edit | edit source]
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[edit | edit source]
References[edit | edit source]
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