| 摘要 |
Novel diquaternary polypeptides possessing skeletal muscle relaxation activity represented by the formulae: <IMAGE> and <IMAGE> wherein: R is lower alkyl; R1 and R2 are lower alkyl or R1 and R2, together with the nitrogen to which they are attached form a heterocyclic ring having 5 to 7 member atoms; R3 is lower alkyl, [N,N-di(lower alkyl)-3-piperidinium](+), or [N,N-di(lower alkyl)-4-piperidinium](+)R4 is selected from the group consisting of t-butyl, benzyl or fluorenylmethyl; A1 is selected from the group consisting of trans-4-acetoxyproline, phenylalanine, glutamic acid- gamma -methyl ester, or proline; AA2 is selected from the group consisting of phenylalanine, leucine, 3-(2-naphthyl)alanine, 3-(1-naphthyl)alanine, and 3-cyclohexylalanine; AA3 is proline when R3 is [N,N-di(lower alkyl)-3-piperidinium](+) or [N,N-di(lower alkyl)-4-piperidinium](+), and is Orn( delta -N(+)-R-R1-R2) or Lys( epsilon -N(+)-R-R1-R2) when R3 ia lower alkyl; AA4 is Orn( delta -N(+)-R-R1-R2) or Lys( epsilon -N(+)-R-R1-R2); Z (-) is a pharmaceutically acceptable anion; and (R)mR1R2N(+) represents the acceptable anion; (R)mR1R2N(+)- represents the alpha amino group of AA1; and m represents an integer of 0 or 1 with the proviso that m is zero only when AA1 is trans-4-acetoxyproline or proline.
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