Detailed Explanation
Pentapeptide neurotransmitters (Met-enkephalin and Leu-enkephalin) that bind δ-opioid receptors to modulate pain at the spinal cord level. Discovered in 1975 by John Hughes and Hans Kosterlitz in Aberdeen, they were the first endogenous opioid peptides identified.
Both are just 5 amino acids: Tyr-Gly-Gly-Phe-Met (Met-enkephalin) and Tyr-Gly-Gly-Phe-Leu (Leu-enkephalin). They are produced from the precursor proenkephalin and rapidly degraded by membrane-bound enkephalinases, limiting their effect to local signaling. Enkephalin degradation inhibitors are being investigated as a potentially safer alternative to exogenous opioid drugs for pain management.
Key Facts
- Pentapeptide neurotransmitters (Met-enkephalin and Leu-enkephalin) that bind δ-opioid receptors to modulate pain at the spinal cord level.
- Discovered in 1975 by John Hughes and Hans Kosterlitz in Aberdeen, they were the first endogenous opioid peptides identified.
- Both are just 5 amino acids: Tyr-Gly-Gly-Phe-Met (Met-enkephalin) and Tyr-Gly-Gly-Phe-Leu (Leu-enkephalin).
- They are produced from the precursor proenkephalin and rapidly degraded by membrane-bound enkephalinases, limiting their effect to local signaling.
- Enkephalin degradation inhibitors are being investigated as a potentially safer alternative to exogenous opioid drugs for pain management.
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