Total views : 226

A Mini Review on Biological Activities of 6-(4-Chlorophenyoxy)-Tetrazolo [5,1-A] Phthalazine (Quan-0808) Compound


  • Department of Pharmacy, GRD(PG) IMT, Dehradun - 248009, (Uttarakhand), India


Purpose: QUAN-0808 (6-(4-chlorophenoxy)-tetrazolo[5,1-a]phthalazine) was tested for the anticonvulsant, anti-inflammatory, analgesic, anticoagulant, antithrombotic and antidepressant effects.

Approaches: Anticonvulsant activity was testedby electroshock seizure model and neurotoxicity was tested by the rotarod neurotoxicity test in mice. In chemically induced models of seizure like pentylenetetrazole, isoniazid, thiosemicarbazide and 3-mercaptopropionic acid were further tested for the anticonvulsant activity.

Findings: QUAN-0808 caused significant anticonvulsant activity against all types of seizures. It appreciably reduced xylene-induced ear edema, reduced the prostaglandin E2 and nitric oxide levels on the edema and reduced acetic acid-induced capillary permeability hyperactivity and reduced acetic acid-induced writhing response. It exhibited anti-inflammatory and antinociceptiveeffect in a dose-dependent manner.

Conclusions: The peripheral effect mechanisms of QUAN-0808 may be related to a reduced in the formation of PGE2, NO, bradykinin and additional inflammatory mediators. The anticoagulant and antithrombotic effects of Q808 delayed bleeding and clotting time in mice. QUAN-0808 exerts anticoagulant, antithrombotic and antidepressant effect, exhibited a significant reduction in immobility as antidepressant.


Tetrazolo-Phthalazine, Anticonvulsant, Antidepressive, QUAN-0808, Anti-Inflammatory, Antinociceptive, Antithrombotic.

Full Text:

 |  (PDF views: 63)


  • Zhang L, Guan LP, Sun XY, Wei CX, Chai KY, Quan ZS. Synthesis and anticonvulsant activity of 6-alkoxy[1,2,4]triazolo[3,4-a]phthalazines. ChemBiol Drug Des, 2009, 73, 313–319.
  • Chen J, Sun XY, Chai KY, Lee JS, Song MS, Quan ZS. Synthesis and anticonvulsant evaluation of 4-(4alkoxylphenyl)-3-ethyl-4H-1,2,4-triazoles as open-chain analogues of 7-alkoxyl-4,5-dihydro[1,2,4]triazolo[4,3a]quinolines. Bioorg Med Chem, 2007, 15, 6775–6781.
  • El-Gazzar AR, El-Enany MM, Mahmoud MN. Synthesis, analgesic, anti-inflammatory, and antimicrobial activity of some novel pyrimido[4,5-b]quinolin-4-ones. Bioorg Med Chem, 2008 16, 3261–3273.
  • Israili ZH. Clinical pharmacokinetics of angiotensin II (AT1) receptor blockers in hypertension. J Hum Hypertens, 2000, 14, Suppl 1, S73–86.
  • Sun X-Y, Wei C-X, Deng X-Q, Sun Z-G, Quan Z-S. Evaluation of the anticonvulsant activity of 6-(4chlorophenyoxy)-tetrazolo[5,-a] phthalazine in various experimental seizure models in mice. Pharmacological Reports, 2010, 62, 273-277.
  • Al-Soud YA, Al-Masoudi NA, FerwanahAel-R. Synthesis and properties of new substituted 1,2,4-triazoles: potential antitumor agents. Bioorg Med Chem, 2003, 8, 1701-1708.
  • Sun XY, Zhang L, Wei CX, Piao HR, Quan ZS. Characterization of the anticonvulsant activity of doxepin in various experimental seizure models in mice. Pharmacol Rep, 2009, 61, 245–251.
  • Castel-Branco MM, Alves GL, Figueiredo IV, Falcao AC, Caramona MM. The maximal electroshock seizure (MES) model in the preclinical assessment of potential n ew antiepileptic drugs. Methods Find ExpClinPharmacol, 2009, 31, 101-106.
  • Talarek S, Listos J, Fidecka S. Role of nitric oxide in the development of tolerance to diazepam-induced motor impairment in mice. Pharmacol Rep, 2008, 60, 475-482.
  • Karnik AV, Malviya NJ, Kulkarni AM, Jadhav BL. Synthesis and in vitro antibacterial activity of novel heterocyclic derivatives of 18-nor-equilenin. Eur J Med Chem, 2006, 41, 891–895.
  • Li CM, Wang MH. Anti-inflammatory effect of the water fraction from hawthorn fruit on LPS-stimulated RAW 264.7 cells. Nutr Res Pract, 2011, 2, 101–106.
  • Santos EN, Lima JCS, Noldin VF, Cechinel-Filho V, Rao VSN, Lima EF, Schmeda-Hirschmann G, Paulo T. Sousa Jr.IV; Domingos T.O. Martins. Anti-inflammatory, antinociceptive, and antipyretic effects of methanol extract of Cariniana-rubrastem bark in animal models. An Acad Bras Ciênc, 2011, 2, 557–566.
  • Sarkar D, Fisher PB. Molecular mechanisms of aging associated inflammation. Cancer Lett, 2006, 236, 13-23.
  • Silva LMCM, Lima V, Holanda ML, Pinheiro PG, Rodrigues JAG, Lima MEP, Benevides NMB. Antinociceptive and anti-inflammatory activities of lectin from marine red alga Pterocladiella-capillacea. Biol Pharm Bull, 2010, 5, 830–835.
  • Huang GJ, Huang SS, Lin SS, Shao YY, Chen CC, Hou WC, Kuo YH. Analgesic effects and the mechanisms of anti-inflammation of ergostatrien-3b-ol from Antrodiacam-phoratasubmerged whole broth in mice. J Agric Food Chem, 2010, 58, 7445–7452.
  • Karin M, Lawrence T, Nizet V. Innate immunity gone awry: linking microbial infections to chronic inflammation and cancer. Cell, 2006, 124, 823–835.
  • Yu H-L, Zhang F, Lan, T, Quan Z-S. Effects of 6-(4chlorophenoxy)-tetrazolo[5,1-a]phthalazine on Anticoagulation in Mice and the Inhibition of Experimental Thrombosis in Rats. J Cardiovasc Pharmacol, 2014, 64(6), 560–566.
  • Abdullah GZ, Abdulkarim MF, Salman IM, Ameer OZ, Yam MF, Mutee AF, Chitneni M, Elrashid S Mahdi, Mahiran Basri, Munavvar A Sattar, and Azmin M Noor. In vitro permeation and in vivo anti-inflammatory and analgesic properties of nanoscaled emulsions containing ibuprofen for topical delivery. Int J Nanomed, 2011, 6, 387–396.
  • Barros WM, Rao VSN, Silva RM, Lima JCS, Martins DTO. Anti-inflammatory effect of the ethanolic extract from Bowdichiavirgili-oidesH.B.K stem bark. An Acad Bras Ciênc, 2010, 3, 609–616.
  • Bars D, Gozariu M, Cadden SW. Animal models of nociception. Pharmacol Rev, 2001, 53, 597–652.
  • Okusada K, Nakamoto K, Nishida M, Fujita-Hamabe W, Kamiya K, Mizushina Y, Satake T, Tokuyama S. The antinociceptive and anti-inflammatory action of the CHCl3-soluble phase and its main active component, damnacanthal, isolated from the root of Morindacitrifolia. Biol Pharm Bull, 2011, 1, 103–107.
  • Jedinak A, Dudhgaonkar S, Wu QL, Simon J, Sliva D. Anti-inflammatory activity of edible oyster mushroom is mediated through the inhibition of NF-kB and AP-1 signaling. Nutr J, 2011, 10, 52.
  • Salvemini D, Ischiropoulos H, Cuzzocrea S. Roles of nitric oxide and superoxide in inflammation. Methods MolBiol, 2003, 225, 291–303.
  • Botting RM. Vane's discovery of the mechanism of action of aspirin changed our understanding of its clinical pharmacology. Pharmacol Rep, 2010, 62, 518–525.
  • Yun KJ, Kim JY, Kim JB. Inhibition of LPS-induced NO and PGE2 production by asiatic acid via NF-kB inactivation in RAW264.7 macrophages: possible involvement of the IKK and MAPK pathways. IntImmunopharmacol, 2008, 3, 431–441.
  • Capone ML, Tacconelli S, Rodriguez LG, Patrignani P. NSAIDs and cardiovascular disease: transducing human pharmacology results into clinical read-outs in the general population. Pharmacol Rep, 2010, 62, 518-525.
  • Harris SG, Padilla J, Koumas L, Ray D, Phipps RP. Prostaglandins as modulators of immunity. Trends Immunol, 2002, 3, 144–150.
  • MullaWA, Kuchekar SB, Thorat VS, Chopade AR, Kuchekar BS. Antioxidant, antinociceptive and antiinflammatory activities of ethanolic-axtract of leaves of Alo-casiaindica (Schott.). J Young Pharm, 2010, 2, 137-143.
  • Yoon WJ, Ham YM, Kim KN, Park SY, Lee NH, Hyun CG, Lee WJ. Anti-inflammatory activity of brown alga Dictyotadichotomain murine macrophage RAW264.7 cells. J Med Plant Res, 2009, 3, 1–8.
  • Crain SM, Shen KF. Acute thermal hyperalgesia elicited by low-dose morphine in normal mice is blocked by ultralow dose naltrexone, unmasking potent opioid analgesia. Brain Res, 2001, 88, 75–82.
  • Chu C, Huang Y, Chen YF, Wu JH, Rahman K, Zheng HC, Qin LP. Anti-nociceptive activity of aqueous fraction from the MeOH extracts of Paederiascandensin mice. J Ethnopharmacol, 2008, 118, 177–180.
  • da Silveira e Sá Rde C, de Oliveira LE, Nóbrega FF, Bhattacharyya J, de Almeida RN. Antinociceptive and toxicological effects of Dioclea grandiflora seed pod in mice. J Biomed Biotechnol, 2010, 10, 1–6.
  • Mbiantcha M, Kamanyi A, Teponno RB, Tapondjou AL, Watcho P, Nguelefack TB: Analgesic and antiinflammatory properties of extracts from the bulbils of Dioscoreabul-biferaL. varsativa (Dioscoreaceae) in mice and rats. Evid Based Complement Alternat Med, 2011, 10, 1–9.
  • Yu H-L, Feng-Zhang, Li Y-J, Gong G-H, Quan Z-S. Antiinflammatory and antinociceptive effects of 6-(4- chlorophenoxy)-tetrazolo[5,1-a] phthalazine in mice. Pharmacological Reports, 2012, 64 (5), 1155-1165.
  • Feng Z, Jiang H-C, Chen X-R, Ma Z, Yu H-L, Quan Z-S. Antidepressant-like effect of 6-(4-chlorophenoxy)tetrazolo[5,1-a] phthalazine in mice. Chinese J Pharmcol & Toxicol, 2013, 27(5), 10.3867/j.issn.10003002.2013.05.003.