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Chemical Compound Review

KST-1A8434     (4S)-5-(4-chlorophenyl)-N- cyclohexyl-4...

Synonyms: AR-1A6092, AC1L2K9Y, AC1Q29OO, AC1Q3NO0
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Disease relevance of Acarflor

  • Hypoxia has marked effects on artery calibre, which reflects important physiological control mechanisms that are altered in disease states [1].
  • At the end of five months the balloon group had significantly more dysphagia and the calibre of the strictures in the balloon group had narrowed by a greater degree [2].
  • The risk of cholangitis, which used to be a major problem with transpapillary introduced prostheses of smaller calibre, seems definitely diminished by using one with a large calibre [3].
  • PATIENT: A 32 year old man with a one year history of constipation and abdominal distention, a massively dilated ascending and transverse colon, and a normal calibre rectum and descending and sigmoid colon [4].
  • Recanalization was achieved in 48 (80%) patients with a residual stenosis of 58.1 +/- 10.8% (mean +/- ISD; range 33-82%) obstruction diameter and a minimum lumen calibre of 1.10 +/- 0.3 mm (range 0.39-1.95 mm) [5].

Psychiatry related information on Acarflor


High impact information on Acarflor

  • 12 supine subjects tilted in 3 degrees increments from 6 degrees leg-down to 12 degrees leg-up showed linear increase in mean peak blood velocity and reduction in calibre in the common femoral vein (colour-duplex ultrasound) [7].
  • There is extensive pharmacological and physiological evidence that endothelin-1 influences airway calibre [8].
  • At follow-up 6 months to 1 year postoperatively (mean 8 months) all had a good calibre urethra [9].
  • In each instance the pancreatic duct was of near normal calibre, and any other procedure would have involved pancreatic resection [10].
  • It is proposed that the headache is due to stimulation of nociceptive nerve-endings in the walls of meningeal vessels (arterioles, venules, and particularly the dural venous sinuses); and that the aura arises from calibre changes in meningeal vessels that penetrate the outer cortex, resulting in localised inhibition or excitation [11].

Chemical compound and disease context of Acarflor


Biological context of Acarflor

  • However, in small resistance arteries (100-300 microns), EDHF appears to be a major determinant of vascular calibre under normal conditions, and may therefore be of primary importance in the regulation of vascular resistance [16].
  • The tail probably regulates axonal calibre, with interfilament spacing determined by phosphorylation of the KSP motifs [17].
  • In addition to the well-established role of neurofilaments in the control of axonal calibre, there is increasing evidence that neurofilaments can interact with other cytoskeletal components and can modulate the axoplasmic flow [18].
  • In the over and underperfused regions blood flow fluctuated rapidly because of instability of cerebrovascular tone, defined as transient constriction of the smallest cerebral vessels (arterioles) alternating with a normal calibre for these vessels and/or short periods of vasodilatation [19].
  • Following resection, freshly isolated 50-150 mum diameter arterioles from the "web" and adjacent normal calibre bowel were analysed with histology and microvessel physiological studies [20].

Anatomical context of Acarflor

  • Neurofilaments are one of the major components of the neuronal cytoskeleton and are responsible for maintaining the calibre of axons [21].
  • In all species studied, the microvascular network of the nerve has an unusually large calibre and wide spacing, particularly when compared with that of skeletal muscle [22].
  • Axon calibre is crucial to efficient impulse transmission in the peripheral nervous system [23].
  • MRI scan showed a marked reduction in the calibre of the left trigeminal nerve from the nerve root exit zone in the pons to Meckel's cave [24].
  • The use of bile duct calibre as sole criterion for an abnormal scan improved the specificity (76%) and with a corresponding reduction in sensitivity (66%) [25].

Associations of Acarflor with other chemical compounds

  • This suggests that pulmonary micro-embolism produced a decrease in medium or large airway calibre, which was mediated by a prostaglandin-like substance from lung tissue, and did not require the presence of the vagus nerves [26].
  • Small calibre airway reactivity to different contractile and relaxant agents was tested in vitro using small segments (about 1 mm long and 0.2 mm in internal diameter) of guinea-pig isolated intralobular bronchi [27].
  • The perivascular administration of SCH 23390 (10(-9)-10(-5)M) per se did not alter arteriolar calibre nor the arteriolar dilatation provoked by microinjections of acidic cerebrospinal fluid [28].
  • In a randomized, double-blind, placebo controlled cross-over study we have investigated the effect of intravenous magnesium on airway calibre and airway reactivity to histamine in 20 subjects with mild to moderate asthma [29].
  • All children participated in an ongoing multicentre study to compare the effects of long-term treatment either with the beta 2-agonist salbutamol (600 plus the inhaled corticosteroid budesonide (600 (BA+CS), or salbutamol plus placebo (BA+PL), on airway calibre, airway responsiveness and symptoms [30].

Gene context of Acarflor


Analytical, diagnostic and therapeutic context of Acarflor

  • The effects of two pranayama yoga breathing exercises on airway reactivity, airway calibre, symptom scores, and medication use in patients with mild asthma were assessed in a randomised, double-blind, placebo-controlled, crossover trial [36].
  • A limited dilatation was performed initially if a small calibre endoscope was unable to pass through the stricture [37].
  • The small calibre chest tube with a one way valve is recommended as a safe and easy technique [38].
  • Assuming this effect on upper airway calibre is not eliminated by sleep, mandibular advancement oral appliances may reduce the severity of obstructive sleep apnoea by maintaining patency of the velopharynx, particularly in its lateral dimension [39].
  • CONCLUSION: The results suggest that carinal transplantation can succeed if (1) the calibre of the graft is matched with that of the recipient; (2) there is an abundant blood supply to the graft; (3) appropriate immunosuppression is provided; (4) ventilation is adequate during surgery [40].


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  2. Balloon or bougie for dilatation of benign oesophageal stricture? An interim report of a randomised controlled trial. Cox, J.G., Winter, R.K., Maslin, S.C., Jones, R., Buckton, G.K., Hoare, R.C., Sutton, D.R., Bennett, J.R. Gut (1988) [Pubmed]
  3. Palliative treatment of obstructive jaundice by transpapillary introduction of large bore bile duct endoprosthesis. Huibregtse, K., Tytgat, G.N. Gut (1982) [Pubmed]
  4. Loss of interstitial cells and a fibromuscular layer on the luminal side of the colonic circular muscle presenting as megacolon in an adult patient. Faussone-Pellegrini, M.S., Fociani, P., Buffa, R., Basilisco, G. Gut (1999) [Pubmed]
  5. Pre-existing coronary stenoses in patients with first myocardial infarction are not necessarily severe. Hackett, D., Davies, G., Maseri, A. Eur. Heart J. (1988) [Pubmed]
  6. Measuring outcome. Tennant, A. Br. Med. Bull. (2000) [Pubmed]
  7. Posture, blood velocity in common femoral vein, and prophylaxis of venous thromboembolism. Ashby, E.C., Ashford, N.S., Campbell, M.J. Lancet (1995) [Pubmed]
  8. Endothelin immunoreactivity of airway epithelium in asthmatic patients. Springall, D.R., Howarth, P.H., Counihan, H., Djukanovic, R., Holgate, S.T., Polak, J.M. Lancet (1991) [Pubmed]
  9. A new treatment for urethral strictures. Milroy, E.J., Chapple, C.R., Cooper, J.E., Eldin, A., Wallsten, H., Seddon, A.M., Rowles, P.M. Lancet (1988) [Pubmed]
  10. Duct obstruction with an acrylate glue for treatment of chronic alcoholic pancreatitis. Little, J.M., Stephen, M., Hogg, J. Lancet (1979) [Pubmed]
  11. Migraine: A vasomotor instability of the meningeal circulation. Blau, J.N. Lancet (1978) [Pubmed]
  12. Effect of salbutamol and ipratropium bromide on airway calibre and bronchial reactivity in asthma and chronic bronchitis. Higgins, B.G., Powell, R.M., Cooper, S., Tattersfield, A.E. Eur. Respir. J. (1991) [Pubmed]
  13. The effect of pre- and postnatal undernutrition on the calibre growth of central motor fibres: a morphometric ultrastructural study on rat cortico-spinal tract. Sima, A., Sourander, P. Acta Neuropathol. (1976) [Pubmed]
  14. Low-dose theophylline: a new anti-inflammatory role in asthma management? MacLeod, D., Djukanović, R. Monaldi archives for chest disease = Archivio Monaldi per le malattie del torace / Fondazione clinica del lavoro, IRCCS [and] Istituto di clinica tisiologica e malattie apparato respiratorio, Università di Napoli, Secondo ateneo. (1996) [Pubmed]
  15. Risk factors for development of flucloxacillin associated jaundice. Fairley, C.K., McNeil, J.J., Desmond, P., Smallwood, R., Young, H., Forbes, A., Purcell, P., Boyd, I. BMJ (1993) [Pubmed]
  16. Endothelium-dependent hyperpolarization: a role in the control of vascular tone. Garland, C.J., Plane, F., Kemp, B.K., Cocks, T.M. Trends Pharmacol. Sci. (1995) [Pubmed]
  17. Deletions of the heavy neurofilament subunit tail in amyotrophic lateral sclerosis. Al-Chalabi, A., Andersen, P.M., Nilsson, P., Chioza, B., Andersson, J.L., Russ, C., Shaw, C.E., Powell, J.F., Leigh, P.N. Hum. Mol. Genet. (1999) [Pubmed]
  18. Neurofilament homeostasis and motoneurone degeneration. Perrone Capano, C., Pernas-Alonso, R., di Porzio , U. Bioessays (2001) [Pubmed]
  19. Focal ischaemia caused by instability of cerebrovascular tone during attacks of hemiplegic migraine. A regional cerebral blood flow study. Friberg, L., Olsen, T.S., Roland, P.E., Lassen, N.A. Brain (1987) [Pubmed]
  20. Radiation induced small bowel "web" formation is associated with acquired microvascular dysfunction. Hatoum, O.A., Binion, D.G., Phillips, S.A., O'Loughlin, C., Komorowski, R.A., Gutterman, D.D., Otterson, M.F. Gut (2005) [Pubmed]
  21. Neurofilaments and neurological disease. Al-Chalabi, A., Miller, C.C. Bioessays (2003) [Pubmed]
  22. A descriptive study of the blood vessels of the sciatic nerve in the rat, man and other mammals. Bell, M.A., Weddell, A.G. Brain (1984) [Pubmed]
  23. Anti-myelin-associated glycoprotein antibodies alter neurofilament spacing. Lunn, M.P., Crawford, T.O., Hughes, R.A., Griffin, J.W., Sheikh, K.A. Brain (2002) [Pubmed]
  24. Persistence of attacks of cluster headache after trigeminal nerve root section. Matharu, M.S., Goadsby, P.J. Brain (2002) [Pubmed]
  25. The predictive value of transabdominal ultrasonography in the diagnosis of biliary tract complications after orthotopic liver transplantation. Hussaini, S.H., Sheridan, M.B., Davies, M. Gut (1999) [Pubmed]
  26. The role of prostaglandins in the bronchoconstriction induced by pulmonary micro-embolism in the guinea-pig. Clay, T.P., Hughes, J.M. J. Physiol. (Lond.) (1980) [Pubmed]
  27. The guinea-pig isolated bronchus for the in vitro study of small calibre airway reactivity. Advenier, C., Freslon, J.L. Br. J. Pharmacol. (1985) [Pubmed]
  28. Vasomotor responses of cerebral arterioles in situ to putative dopamine receptor agonists. Edvinsson, L., McCulloch, J., Sharkey, J. Br. J. Pharmacol. (1985) [Pubmed]
  29. Effect of intravenous magnesium sulphate on airway calibre and airway reactivity to histamine in asthmatic subjects. Hill, J.M., Britton, J. British journal of clinical pharmacology. (1996) [Pubmed]
  30. The effect of an inhaled corticosteroid (budesonide) on exercise-induced asthma in children. Dutch CNSLD Study Group. Waalkens, H.J., van Essen-Zandvliet, E.E., Gerritsen, J., Duiverman, E.J., Kerrebijn, K.F., Knol, K. Eur. Respir. J. (1993) [Pubmed]
  31. Atrophy of large myelinated axons in metallothionein-I, II knockout mice. Stankovic, R.K. Cell. Mol. Neurobiol. (2005) [Pubmed]
  32. Urotensin II: its function in health and its role in disease. Ong, K.L., Lam, K.S., Cheung, B.M. Cardiovascular drugs and therapy / sponsored by the International Society of Cardiovascular Pharmacotherapy. (2005) [Pubmed]
  33. Distal axonopathy in peripheral nerves of PMP22-mutant mice. Sancho, S., Magyar, J.P., Aguzzi, A., Suter1, U. Brain (1999) [Pubmed]
  34. Large calibre primary afferent neurons projecting to the gracile nucleus express neuropeptide Y after sciatic nerve lesions: an immunohistochemical and in situ hybridization study in rats. Zhang, X., Meister, B., Elde, R., Verge, V.M., Hökfelt, T. Eur. J. Neurosci. (1993) [Pubmed]
  35. Correlation between endometrial histology, microvascular density and calibre, matrix metalloproteinase-3 and bleeding pattern in women using a levonorgestrel-releasing intrauterine system. Oliveira-Ribeiro, M., Petta, C.A., De Angelo Andrade, L.A., Bahamondes, L., Hidalgo, M.M. Hum. Reprod. (2004) [Pubmed]
  36. Effect of yoga breathing exercises (pranayama) on airway reactivity in subjects with asthma. Singh, V., Wisniewski, A., Britton, J., Tattersfield, A. Lancet (1990) [Pubmed]
  37. Endoscopic palliation for inoperable malignant dysphagia: long term follow up. Maunoury, V., Brunetaud, J.M., Cochelard, D., Boniface, B., Cortot, A., Paris, J.C. Gut (1992) [Pubmed]
  38. Role of small calibre chest tube drainage for iatrogenic pneumothorax. Laub, M., Milman, N., Müller, D., Struve-Christensen, E. Thorax (1990) [Pubmed]
  39. Mandibular advancement oral appliance therapy for obstructive sleep apnoea: effect on awake calibre of the velopharynx. Ryan, C.F., Love, L.L., Peat, D., Fleetham, J.A., Lowe, A.A. Thorax (1999) [Pubmed]
  40. Carinal transplantation. Ueda, H., Shirakusa, T. Thorax (1992) [Pubmed]
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