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Chemical Compound Review

TEPROTIDE     1-[1-[2-[[4-aminocarbonyl-2- [[1-[5...

Synonyms: Teprotido, Teprotidum, BPP-9a, AGN-PC-00MEB2, CCRIS 9333, ...
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Disease relevance of TEPROTIDE


High impact information on TEPROTIDE

  • In patients who had received no previous drug treatment, log baseline plasma renin activity and change in mean blood pressure after SQ 20881 correlated significantly (r = 0.651, P less than 0.05) [5].
  • SQ 20881 allows prompt evaluation of the role of renin in hypertensive emergencies and permits early choice of appropriate therapy based on the prevailing mechanism [5].
  • Although small amounts of kininogen-like substrate were found in uterine tissue, detectable kinin levels (greater than 4 pg) could not be found in bathing media during maximal kallikrein-induced contractions or after uterine tissue was incubated with high concentrations of the enzyme in the presence of SQ 20881, a kininase II inhibitor [6].
  • In dogs receiving approximately equal to 5 mEq/day of sodium, intrarenal infusion of P 113 increased renal blood flow (RBF) from 219.8 +/- 32.3 to 282.7 +/- 20.0 ml/min (P less than 0.004), and with intrarenal SQ 20881 infusion from 215.3 +/- 14.2 to 278.0 +/- 22.2 ml/min (p less than 0.005) [7].
  • The effects of intrarenal infusion of 1-sar-8-ala angiotension II (P 113) and a converting enzyme inhibitor, SQ 20881, at doses that did not affect systemic blood pressure (2.0 mug/kg per min) were studied in conscious, uninephrectomized dogs [7].

Chemical compound and disease context of TEPROTIDE


Biological context of TEPROTIDE

  • Effects of the converting enzyme inhibitor (SQ 20881) on the pulmonary circulation in man [9].
  • During converting enzyme inhibition with SQ 20881, mean arterial pressure and heart rate remained unchanged following arginine vasopressin blockade in both normohydrated and fluid-restricted animals. alpha-Adrenergic receptor blockade reduced the blood pressure of normohydrated SHR, from 160 +/- 7 to 81 +/- 8 mm Hg [10].
  • Endopeptidase B purified from pool 3 is inhibited by bradykinin-potentiating peptide 9a (BPP9a, SQ 20881) (< Glu-Trp-Pro-Arg-Pro-Gln-Ile-Pro-Pro), a competitive inhibitor of the hydrolysis of bradykinin (Km = 3.5 X 10(-5) M, Ki = 3 X 10(-6) M) which also completely inhibits the inactivation of LH-RH [11].
  • Treatment of hypoxic rats with SQ 20881 was found to significantly decrease right ventricular pressure, tissue weight, absolute protein content, and in vitro protein synthesis after 7 days compared to saline-treated hypoxic rats [4].
  • In contrast, converting enzyme inhibitor SQ 20881 (SQ) or dopamine (DA) significantly increased PRA and body temperature of sheep [12].

Anatomical context of TEPROTIDE


Associations of TEPROTIDE with other chemical compounds


Gene context of TEPROTIDE

  • The renal vascular response to SQ 20881 paralleled the endocrine response: An identical threshold dose (30 microgram/kg) increased renal blood flow and reduced plasma angiotensin II concentration, which fell despite a progressive rise of plasma renin activity [20].
  • The arterial pressure compensation of two animals with intact kidneys was significantly reduced when the angiotensin-converting enzyme inhibitor (SQ 20881) was infused before the haemorrhage [22].
  • Plasma bradykinin concentration did not change in response to SQ 20881, which also blocks kininase II [20].
  • It is concluded that the action of SQ 20881 on human blood kinin system, besides inhibition of kininase, involves also reduction of kininogen, the mechanism of which remains to be clarified [23].

Analytical, diagnostic and therapeutic context of TEPROTIDE

  • Reduction in hypertension-induced protein synthesis in the rat pulmonary trunk after treatment with teprotide (SQ 20881) [4].
  • Addition of converting-enzyme inhibitor, SQ 20881 to the perfusion medium competitively prevented the potentiation of AI on the assay organs without altering its direct effects [24].


  1. Accentuated vascular and endocrine response to SQ 20881 in hypertension. Williams, G.H., Hollenberg, N.K. N. Engl. J. Med. (1977) [Pubmed]
  2. Reactive hyperreninemia in renovascular hypertension after angiotensin blockage with saralasin or converting enzyme inhibitor. Case, D.B., Laragh, J.H. Ann. Intern. Med. (1979) [Pubmed]
  3. Converting enzyme inhibition augments and competitive inhibition of angiotensin II partially restores reflex adrenal catecholamine release in anephric dogs. Cimmino, V.M., Badder, E.M., Strefling, A.M., Seaton, J.F., Harrison, T.S. Endocrinology (1978) [Pubmed]
  4. Reduction in hypertension-induced protein synthesis in the rat pulmonary trunk after treatment with teprotide (SQ 20881). McKenzie, J.C., Hung, K.S., Mattioli, L., Klein, R.M. Proc. Soc. Exp. Biol. Med. (1984) [Pubmed]
  5. Converting enzyme inhibition in hypertensive emergencies. Tifft, C.P., Gavras, H., Kershaw, G.R., Gavras, I., Brunner, H.R., Liang, C.S., Chobanian, A.V. Ann. Intern. Med. (1979) [Pubmed]
  6. Kallikrein-induced uterine contraction independent of kinin formation. Chao, J., Buse, J., Shimamoto, K., Margolius, H.S. Proc. Natl. Acad. Sci. U.S.A. (1981) [Pubmed]
  7. Effect of intrarenal angiotensin II blockade on renal function in conscious dogs. Kimbrough, H.M., Vaughan, E.D., Carey, R.M., Ayers, C.R. Circ. Res. (1977) [Pubmed]
  8. Angiotensin-converting enzyme inhibitor (SQ 20881) in the diagnosis of renovascular hypertension. Rosenthal, T., Kissin, E., Jacob, E.T., Stern, N., Levi, Y., Adar, R. Angiology. (1979) [Pubmed]
  9. Effects of the converting enzyme inhibitor (SQ 20881) on the pulmonary circulation in man. Niarchos, A.P., Roberts, A.J., Laragh, J.H. Am. J. Med. (1979) [Pubmed]
  10. Does vasopressin sustain blood pressure in conscious spontaneously hypertensive rats? Filep, J., Fejes-Tóth, G. Hypertension (1986) [Pubmed]
  11. Screening for rabbit brain neuropeptide-metabolizing peptidases. Inhibition of endopeptidase B by bradykinin potentiating peptide 9a (SQ 20881). Martins, A.R., Caldo, H., Coelho, H.L., Moreira, A.C., Antunes-Rodrigues, J., Greene, L.J., Martins de Camargo, A.C. J. Neurochem. (1980) [Pubmed]
  12. Dopaminergic modulation of some central actions of angiotensin II in vivo. Huang, B.S., Malvin, R.L. Proc. Soc. Exp. Biol. Med. (1988) [Pubmed]
  13. The effect of angiotensin I converting enzyme inhibitor (SQ 20881) on the release of prostaglandins by rabbit kidney, in vivo. Johns, E.J., Murdock, R., Singer, B. Br. J. Pharmacol. (1977) [Pubmed]
  14. Angiotensin-converting enzyme substrates hydrolyzed by fibroblasts and vascular endothelial cells. Rubin, D.B., Mason, R.J., Dobbs, L.J. Exp. Lung Res. (1982) [Pubmed]
  15. Effect of SQ 14225 and SQ 20881 on the norepinephrine contents of the central nervous system. Domínguez, A.E., Fernández, B.E., Seeber, A.M. Arch. Int. Physiol. Biochim. (1981) [Pubmed]
  16. Saralasin and SQ 20881 : their effects on central nervous system norepinephrine. Martínez Seeber, A., Fernández, B.E., Domínguez, A.E., Vidal, N.A. Arch. Int. Physiol. Biochim. (1978) [Pubmed]
  17. The granulocyte-angiotensin system. Angiotensin I-converting activity of cathepsin G. Klickstein, L.B., Kaempfer, C.E., Wintroub, B.U. J. Biol. Chem. (1982) [Pubmed]
  18. Evidence against a pressor role for vasopressin in spontaneous hypertension. Sladek, C.D., Blair, M.L., Mangiapane, M. Hypertension (1987) [Pubmed]
  19. Mechanism of blood pressure reduction by teprotide (SQ 20881) in rats. Jaeger, P., Ferguson, R.K., Brunner, H.R., Kirchertz, E.J., Gavras, H. Kidney Int. (1978) [Pubmed]
  20. Renal vascular response to interruption of the renin-angiotensin system in normal man. Hollenberg, N.K., Williams, G.H., Taub, K.J., Ishikawa, I., Brown, C., Adams, D.F. Kidney Int. (1977) [Pubmed]
  21. Elevation of substance P-like immunoreactivity in rat central nervous system by protease inhibitors. Hanson, G.R., Lovenberg, W. J. Neurochem. (1980) [Pubmed]
  22. Quantitative analysis of the acute response to haemorrhage of the renin-angiotensin-vasoconstrictor feedback loop in areflexic dogs. Brough, R.B., Cowley, A.W., Guyton, A.C. Cardiovasc. Res. (1975) [Pubmed]
  23. Blood kinin system in renal hypertensive patients administered with SQ 20881. Edery, H., Rosenthal, T., Amitzur, G., Stern, N. Adv. Exp. Med. Biol. (1979) [Pubmed]
  24. High degree of conversion of angiotensin I to angiotensin II in the mesenteric circulation of the isolated perfused terminal ileum of the cat. Türker, R.K., Ercan, Z.S. Arch. Int. Physiol. Biochim. (1975) [Pubmed]
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