摘要:
La séquence d'ADNc codant pour un peptide natriurétique de cervelle de porc et des gènes associés codant pour des peptides canins et humains avec activité natriurétique sont décrits. On a découvert que le gène rend accessible les ADNs codant pour des peptides natriurétiques analogues dans d'autres espèces vertébrés. Les gènes codant pour ces peptides natriurétiques peuvent être utilisés pour obtenir des modifications de la séquence en vue de produire des formes alternées des peptides natriurétiques et en vue de produire des quantités pratiques de ces protéines. Les peptides natriurétiques de la présente invention peuvent également être synthétisés par voie chimique.
摘要:
Synthetic natriuretic peptides (SNP) composed of 23 amino acid residues of which residues 2 - 23 have the natural L-configuration while the amino-terminal residue is derived from an unnatural amino acid having the D-configuration. The compounds possess diurectic, natriuretic, vasorelaxant, smooth muscle relaxant, hypotensive, and anti-hypertensive activites, and a process for their preparation is also disclosed, together with pharmaceutical preparations thereof and with their use in the practice of medicine. Salts of said synthetic natriuretic peptides with pharmaceutically acceptable acids are also disclosed.
摘要:
The cDNA sequence encoding porcine brain natriuretic peptide and related genes encoding canine and human peptides with natriuretic activity are disclosed. The gene is shown to make accessible the DNAs encoding analogous natriuretic peptides in other vertebrate species. The genes encoding these NPs can be used to effect modifications of the sequence to produce alternate forms of the NPs and to provide practical amounts of these proteins. The NPs of the invention can also be synthesized chemically.
摘要:
A peptide derivative of the formula wherein A is hydrogen or a hydrocarbon acyl having 2 to 18 carbon atoms which is substituted by an amino group at the α-position; B is F-Gly wherein F is a neutral a-amino acid residue, or NH-(CH 2 )nCO wherein n is an integer of 1 to 4; C is a neutral a-amino acid residue; and E is L-Arg or D-Arg; when A, B and C are hydrogen, Gly-Gly, and Met or lie, respectively, E is D-Arg, or its pharmacologically acceptable salt has strong hypotensive and natriuretic activity; therefore it is useful as a therapeutic drug for hypertension, a diuretic, and a therapeutic drug for cardiac and cerebral circulatory diseases.
摘要:
Atrial peptides comprising the amino acid sequence as follows: wherein R₁ is hydrogen, Ser, Cit, SerSer, Arg, Carbamoyl Ser, Guanido-Ser-Ser, Amcca, Guanido-Amcca, Lys, ArgArg, Ser-Arg, Ser-Lys, Acetyl-Ser-Ser, D-Ser-Ser, Ser-D-Ser, Guanido-Aocta, Aunda, Aocta, Ahexa, HSer, Apenta, Papaa, Abuta, Mamba, Orn, D-Orn or Acetyl-apenta, Acetyl-Ahexa, Guanido; R₂ is Cys, D-Cys or Pen; R₃ is L-Phe, D-Ala, L-Ala, D-Val, D-Cha, Sar, D-Phg, Aib, β-Ala or Gly; R₄ is Phe, Trp, D-Tic, L-Tic, N-MePhe, D-Ala, Tyr, 2-Thi, DimeDOPA or DOPA; R₅ is Gly-Gly, Ala-Gly, D-Ala-Gly, Gly-Ala, Amcca, Mapaa or Papaa; R₆ is Arg, D-Arg or Cit; R₇ is Ile, Leu, D-Leu or Met; R₈ is Asp, Asn, β-methylAsp, cycloAsp, Gly or Ser; R₉ is Arg, D-Arg or Ala; R₁₀ is Ile, Leu or Phe; R₁₁ is Cys, D-Cys, HCys, Cys-4-thiomethylproline, or trans-4-thiomethylproline; R₁₂ is absent, Phe, D-Ala-Phe, D-Phe, Cha, Pro, D-Pro, 2-Thi, Aic, D-Tic, trans-4-FPro, L-Tic, Leu, Ile or β-NAl; R₁₃ is OH, Arg, Arg-NH₂, D-Arg, Gln, Lys, HomoArg, or Gly; or pharmaceutically acceptable salts, esters or amides thereof.
摘要:
A peptide derivative of the formula wherein A is hydrogen or a hydrocarbon acyl having 2 to 18 carbon atoms which is substituted by an amino group at the α-position; B is F-Gly wherein F is a neutral a-amino acid residue, or NH-(CH 2 )nCO wherein n is an integer of 1 to 4; C is a neutral a-amino acid residue; and E is L-Arg or D-Arg; when A, B and C are hydrogen, Gly-Gly, and Met or lie, respectively, E is D-Arg, or its pharmacologically acceptable salt has strong hypotensive and natriuretic activity; therefore it is useful as a therapeutic drug for hypertension, a diuretic, and a therapeutic drug for cardiac and cerebral circulatory diseases.