The invention relates to new basic amino acid derivatives of general formula I and the preparation and use thereof in treatment of pain. The compounds have histogranin-like antinociceptive, morphine potentiating and COX-2 induction modulating activities. ##STR1##

wherein:

    • A is -hydrogen, —(C1-C8)alkyl or —(C1-C8)alkyl substituted by hydroxy;
    • B is —(C1-C6)alkylguanidino, —(C1-C6)alkyl(4-imidazo-lyl), —(C1-C6)alkylamino, p-aminophenylalkyl(C1-C6)—, p-guanidinophenylalkyl(C1-C6)— or 4-pyridinylalkyl(C1-C6)—;
    • R1, R2 and R3 are, independent of one another, -hydrogen, -arylcarbonylamino, —(C1-C6)alkoylamino, —(C1-C6)alkylamino, —(C1-C6)alkyloxy, —(C1-C6)alkylaminocarbonyl, -carboxy, —OH, -benzoyl, -p-halogenobenzoyl, -methyl, —S-(2,4-dinitrophenyl), —S-(3-nitro-2-pyridinesulfenyl), -sulfonyl, -trifluoromethyl, —(C1-C6)alkylaminocarbonylamino, -halo or -amino;
    • R4 and R5 are, independent of one another, -hydrogen, —(C1-C6)alkyl, -methyloxy, -nitro, -amino, -arylcarbonylamino, —(C1-C6)alkoylamino, —(C1-C6)alkylamino, -halo or —OH.
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