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Chemical Compound Review

Antalarmin     N-butyl-N-ethyl-4,8,9- trimethyl-7-(2,4,6...

Synonyms: AGN-PC-00F0RA, CHEMBL296641, SureCN466243, CHEBI:166501, NSC-715590, ...
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Disease relevance of Antalarmin


Psychiatry related information on Antalarmin


High impact information on Antalarmin

  • We found that antalarmin, a CRH receptor type 1 antagonist, decreased FasL expression and promoted apoptosis of activated T lymphocytes, an effect which was potentiated by CRH and inhibited by antalarmin [7].
  • Embryos from mothers that lacked T cells or from syngeneic matings were not rejected when the mothers were given antalarmin [7].
  • Female rats treated with antalarmin showed a marked decrease in implantation sites and live embryos and diminished endometrial FasL expression [7].
  • Stress-induced reinstatement of alcohol seeking was not significantly affected by antalarmin in Wistar rats but was fully blocked in msP animals [8].
  • These effects appeared to be mediated via the R1 receptors because the CRH receptor antagonists, astressin and antalarmin but not anti-sauvagine 30, could block them [9].

Chemical compound and disease context of Antalarmin


Biological context of Antalarmin

  • Antalarmin significantly inhibited a repertoire of behaviors associated with anxiety and fear such as body tremors, grimacing, teeth gnashing, urination, and defecation [11].
  • Fetuses infused with vehicle delivered at a mean gestational age of 141.8 +/- 0.9 days compared with antalarmin-infused sheep at 148.8 +/- 1.6 days (P = 0.0036, unpaired Student's t-test) [12].
  • Receptor autoradiography indicated an up-regulation of dopamine D2, but no change in D1, binding in striatum, and Golgi-Cox analysis of striatal medium spiny neurones indicated that chronic antalarmin treatment increased spine density [13].
  • We tested the hypothesis that fetal CRH is a primary factor in the onset of parturition in sheep by using a Type I CRH receptor antagonist, antalarmin, to block the endogenous action of CRH [12].
  • Collectively, these findings demonstrate that multiple signalling systems are susceptible to modulation by social isolation and that antalarmin can reverse some, but not all, isolation-induced alterations in brain chemistry [14].

Anatomical context of Antalarmin

  • After oral administration, significant antalarmin concentrations were detected in the systemic circulation and the cerebrospinal fluid by a mass spectrometry-gas chromatography assay developed specifically for this purpose [11].
  • Human adrenal cortical and/or chromaffin cells in co-culture were incubated with CRH, antalarmin, and both CRH and antalarmin in vitro [15].
  • The width of the adrenal cortex of animals treated with antalarmin was reduced by 31% compared with that in controls without atrophy of the gland [1].
  • Of chief interest was whether the CRH-R1-selective pyrrolopyrimidine, antalarmin, shown previously to have activity in the central nervous system (CNS), would differ in its antagonist profile from the CRH-R1- & 2-selective peptide, astressin B, which is unlikely to have access to the CNS following systemic administration [16].
  • Thus, chronic antalarmin treatment modulates dopaminergic pathways and implies that chronic treatment with drugs of this class may ultimately alter postsynaptic signaling mechanisms within the basal ganglia [13].

Associations of Antalarmin with other chemical compounds


Gene context of Antalarmin

  • CRH inhibited EVT invasion in Matrigel invasion assays, and this effect was blocked by the CRH receptor type 1 (CRHR1)-specific antagonist antalarmin [20].
  • The action of CRH was completely inhibited by antalarmin [15].
  • We previously showed that acute stress increases rat blood-brain barrier (BBB) permeability, an effect involving brain mast cells and CRF, as it was absent in W/W(v) mast cell-deficient mice and was blocked by the CRF-receptor antagonist, Antalarmin [21].
  • The performance-enhancing effects of Ucn in both water maze and passive avoidance paradigms were reversed by i.c.v. pretreatment with D-Phe CRF(12-41) (2.5, 5 microg), a broad CRF(1)/CRF(2) receptor antagonist, or antalarmin (10 microg), a potent, nonpeptide, CRF(1) selective receptor antagonist [22].
  • These effects were mediated by the CRH type 1 receptor because its antagonist antalarmin blocked CRH-induced apoptosis and Fas ligand expression [23].

Analytical, diagnostic and therapeutic context of Antalarmin


  1. Chronic effects of a nonpeptide corticotropin-releasing hormone type I receptor antagonist on pituitary-adrenal function, body weight, and metabolic regulation. Bornstein, S.R., Webster, E.L., Torpy, D.J., Richman, S.J., Mitsiades, N., Igel, M., Lewis, D.B., Rice, K.C., Joost, H.G., Tsokos, M., Chrousos, G.P. Endocrinology (1998) [Pubmed]
  2. Facilitation of Cardiac Vagal Activity by CRF-R1 Antagonists during Swim Stress in Rats. Wood, S.K., Verhoeven, R.E., Savit, A.Z., Rice, K.C., Fischbach, P.S., Woods, J.H. Neuropsychopharmacology (2006) [Pubmed]
  3. 4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1, 3-thiazol-2-amine hydrochloride (SSR125543A), a potent and selective corticotrophin-releasing factor(1) receptor antagonist. II. Characterization in rodent models of stress-related disorders. Griebel, G., Simiand, J., Steinberg, R., Jung, M., Gully, D., Roger, P., Geslin, M., Scatton, B., Maffrand, J.P., Soubrié, P. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
  4. Corticotropin-releasing factor 1 receptor-mediated mechanisms inhibit colonic hypersensitivity in rats. Greenwood-Van Meerveld, B., Johnson, A.C., Cochrane, S., Schulkin, J., Myers, D.A. Neurogastroenterol. Motil. (2005) [Pubmed]
  5. Corticotropin releasing hormone (CRH) antagonist attenuates adjuvant induced arthritis: role of CRH in peripheral inflammation. Webster, E.L., Barrientos, R.M., Contoreggi, C., Isaac, M.G., Ligier, S., Gabry, K.E., Chrousos, G.P., McCarthy, E.F., Rice, K.C., Gold, P.W., Sternberg, E.M. J. Rheumatol. (2002) [Pubmed]
  6. The Anxiogenic Drug Yohimbine Reinstates Palatable Food Seeking in a Rat Relapse Model: a Role of CRF(1) Receptors. Ghitza, U.E., Gray, S.M., Epstein, D.H., Rice, K.C., Shaham, Y. Neuropsychopharmacology (2006) [Pubmed]
  7. Corticotropin-releasing hormone promotes blastocyst implantation and early maternal tolerance. Makrigiannakis, A., Zoumakis, E., Kalantaridou, S., Coutifaris, C., Margioris, A.N., Coukos, G., Rice, K.C., Gravanis, A., Chrousos, G.P. Nat. Immunol. (2001) [Pubmed]
  8. Variation at the rat Crhr1 locus and sensitivity to relapse into alcohol seeking induced by environmental stress. Hansson, A.C., Cippitelli, A., Sommer, W.H., Fedeli, A., Bj??rk, K., Soverchia, L., Terasmaa, A., Massi, M., Heilig, M., Ciccocioppo, R. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  9. Up-regulation of nitric oxide synthase and modulation of the guanylate cyclase activity by corticotropin-releasing hormone but not urocortin II or urocortin III in cultured human pregnant myometrial cells. Aggelidou, E., Hillhouse, E.W., Grammatopoulos, D.K. Proc. Natl. Acad. Sci. U.S.A. (2002) [Pubmed]
  10. Effect of antalarmin, a novel corticotropin-releasing hormone antagonist, on the dynamic function of the preterm ovine fetal hypothalamo-pituitary-adrenal axis. Young, I.R., Chan, E.C., Smith, R., Chrousos, G.P., Veldhuis, J.D., Canny, B.J. Neuroendocrinology (2002) [Pubmed]
  11. Oral administration of a corticotropin-releasing hormone receptor antagonist significantly attenuates behavioral, neuroendocrine, and autonomic responses to stress in primates. Habib, K.E., Weld, K.P., Rice, K.C., Pushkas, J., Champoux, M., Listwak, S., Webster, E.L., Atkinson, A.J., Schulkin, J., Contoreggi, C., Chrousos, G.P., McCann, S.M., Suomi, S.J., Higley, J.D., Gold, P.W. Proc. Natl. Acad. Sci. U.S.A. (2000) [Pubmed]
  12. A corticotropin-releasing hormone type I receptor antagonist delays parturition in sheep. Chan, E.C., Falconer, J., Madsen, G., Rice, K.C., Webster, E.L., Chrousos, G.P., Smith, R. Endocrinology (1998) [Pubmed]
  13. Chronic corticotropin-releasing factor type 1 receptor antagonism with antalarmin regulates the dopaminergic system of Fawn-Hooded rats. Lawrence, A.J., Parish, C.L., Chen, F., Lodge, D.J., Krstew, E.V., Card, K., Finkelstein, D.I., Horne, M.K. J. Neurochem. (2005) [Pubmed]
  14. The CRF1 receptor antagonist, antalarmin, reverses isolation-induced up-regulation of dopamine D2 receptors in the amygdala and nucleus accumbens of fawn-hooded rats. Djouma, E., Card, K., Lodge, D.J., Lawrence, A.J. Eur. J. Neurosci. (2006) [Pubmed]
  15. Effects of a novel corticotropin-releasing-hormone receptor type I antagonist on human adrenal function. Willenberg, H.S., Bornstein, S.R., Hiroi, N., Päth, G., Goretzki, P.E., Scherbaum, W.A., Chrousos, G.P. Mol. Psychiatry (2000) [Pubmed]
  16. Corticotropin-releasing hormone antagonists, astressin B and antalarmin: differing profiles of activity in rhesus monkeys. Broadbear, J.H., Winger, G., Rivier, J.E., Rice, K.C., Woods, J.H. Neuropsychopharmacology (2004) [Pubmed]
  17. Marked suppression of gastric ulcerogenesis and intestinal responses to stress by a novel class of drugs. Gabry, K.E., Chrousos, G.P., Rice, K.C., Mostafa, R.M., Sternberg, E., Negrao, A.B., Webster, E.L., McCann, S.M., Gold, P.W. Mol. Psychiatry (2002) [Pubmed]
  18. Corticotropin-releasing factor 1 antagonists selectively reduce ethanol self-administration in ethanol-dependent rats. Funk, C.K., Zorrilla, E.P., Lee, M.J., Rice, K.C., Koob, G.F. Biol. Psychiatry (2007) [Pubmed]
  19. Recent advances with the CRF1 receptor: design of small molecule inhibitors, receptor subtypes and clinical indications. McCarthy, J.R., Heinrichs, S.C., Grigoriadis, D.E. Curr. Pharm. Des. (1999) [Pubmed]
  20. Corticotropin-releasing hormone modulates human trophoblast invasion through carcinoembryonic antigen-related cell adhesion molecule-1 regulation. Bamberger, A.M., Minas, V., Kalantaridou, S.N., Radde, J., Sadeghian, H., Löning, T., Charalampopoulos, I., Brümmer, J., Wagener, C., Bamberger, C.M., Schulte, H.M., Chrousos, G.P., Makrigiannakis, A. Am. J. Pathol. (2006) [Pubmed]
  21. Corticotropin-releasing factor (CRF) can directly affect brain microvessel endothelial cells. Esposito, P., Basu, S., Letourneau, R., Jacobson, S., Theoharides, T.C. Brain Res. (2003) [Pubmed]
  22. Urocortin shares the memory modulating effects of corticotropin-releasing factor (CRF): mediation by CRF1 receptors. Zorrilla, E.P., Schulteis, G., Ormsby, A., Klaassen, A., Ling, N., McCarthy, J.R., Koob, G.F., De Souza, E.B. Brain Res. (2002) [Pubmed]
  23. Corticotropin-releasing hormone induces Fas ligand production and apoptosis in PC12 cells via activation of p38 mitogen-activated protein kinase. Dermitzaki, E., Tsatsanis, C., Gravanis, A., Margioris, A.N. J. Biol. Chem. (2002) [Pubmed]
  24. Maternal and fetal hypothalamic-pituitary-adrenal axes during pregnancy and postpartum. Mastorakos, G., Ilias, I. Ann. N. Y. Acad. Sci. (2003) [Pubmed]
  25. The Effects of Corticoptropin-Releasing Factor and the Urocortins on Striatal Dopamine Release Induced by Electrical Stimulation-An in vitro Superfusion Study. Bagosi, Z., Jászberényi, M., Bujdosó, E., Telegdy, G. Neurochem. Res. (2006) [Pubmed]
  26. Quantitative determination of antalarmin, a novel corticotropin-releasing hormone receptor-1 antagonist, in canine plasma by HPLC-MS. Fox, S.D., Roman, J.M., Cizza, G., Veenstra, T.D., Issaq, H.J. Journal of separation science. (2005) [Pubmed]
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