Purification of enkephalin, an endogenous composition in the hum

Details Purification of enkephalin, an endogenous composition in the hum Purification of enkephalin, an endogenous composition in the hum

1976-03-15

1978-08-08

Phillips, Delbert R.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

424177, C07C10352, A61K 3700

Patent

active

041056515

ABSTRACT:
The purification of an endogenous composition isolated from mammalian brain tissue and termed enkephalin ("in the head"). Enkephalin is recovered from brain tissue by acetone solution and purified by means of column and thin layer chromatography. The composition which is a mixture of two pentapeptides, namely, (a) H-Tyr-Gly-Gly-Phe-Met-OH and (b) H-Tyr-Gly-Gly-Phe-Leu-OH wherein the ratio of a:b is from 3:1 to 4:1 has been found to be a non-addictive narcotic and an opiate agonist.
The synthesis of the pentapeptide composition from the known structure above is accomplished by conventional solution techniques of protection of the amino groups, such as t-butyloxycarbonyl, benzyloxycarbonyl, and t-amyloxycarbonyl, or the solid phase peptide synthesis of R. Bruce Merrifield using a polymeric support and the same or similar amine protecting groups.

REFERENCES:
hughes et al., Nature, 258, 577-579 (1975).

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