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Page 1
BK channel modulators: a comprehensive overview.
Nardi A, Olesen SP. Nardi A, et al. Curr Med Chem. 2008;15(11):1126-46. doi: 10.2174/092986708784221412. Curr Med Chem. 2008. PMID: 18473808 Review.
On the contrary, three BK openers that were progressed to clinical development have recently been discontinued (NS8, BMS204352 and TA1702) and, at the present time, only one drug candidate targeting BK channels (andolast) remains in the early phases of clinical development …
On the contrary, three BK openers that were progressed to clinical development have recently been discontinued (NS8, BMS204352 and TA1702) a …
Gateways to clinical trials.
Bayés M, Rabasseda X, Prous JR. Bayés M, et al. Methods Find Exp Clin Pharmacol. 2007 Jun;29(5):359-73. Methods Find Exp Clin Pharmacol. 2007. PMID: 17805439
101M, 12B75; ABT-869, Agomelatine, Alvocidib hydrochloride, Amb a 1 ISS-1018, AMG-386, Andolast, AP-23573, Arsenic trioxide, ATI-7505; BAY-68-4986, Berberine chloride, BNP-1350, BrachySil, Brostallicin hydrochloride; Caldaret hydrate, Cancer vaccine, Cediranib, CHAMPION ev …
101M, 12B75; ABT-869, Agomelatine, Alvocidib hydrochloride, Amb a 1 ISS-1018, AMG-386, Andolast, AP-23573, Arsenic trioxide, ATI-7505 …
A potential anti-asthmatic drug, CR 2039, enhances the anticonvulsive activity of some antiepileptic drugs against pentetrazol in mice.
Czuczwar SJ, Gasior M, Kozicka M, Pietrasiewicz T, Turski WA, Kleinrok Z. Czuczwar SJ, et al. Eur Neuropsychopharmacol. 1998 Aug;8(3):233-8. doi: 10.1016/s0924-977x(97)00077-1. Eur Neuropsychopharmacol. 1998. PMID: 9716318
CR 2039 (4-(1H-tetrazol-5-yl)-N-[4-(1H-tetrazol-5-yl]phenylbenzam ide), in doses of 10, 20, and 100 mg/kg i.p., did not modify the seizure pattern observed after subcutaneous pentetrazol, administered at its CD97 of 90 mg/kg for the clonic phase. ...In conclusion, …
CR 2039 (4-(1H-tetrazol-5-yl)-N-[4-(1H-tetrazol-5-yl]phenylbenzam ide), in doses of 10, 20, and 100 mg/kg i.p., did not modify …
CR 2039, a new bis-(1H-tetrazol-5-yl)phenylbenzamide derivative with potential for the topical treatment of asthma.
Revel L, Colombo S, Ferrari F, Folco G, Rovati LC, Makovec F. Revel L, et al. Eur J Pharmacol. 1992 Dec 8;229(1):45-53. doi: 10.1016/0014-2999(92)90284-b. Eur J Pharmacol. 1992. PMID: 1282105
The pharmacological activity of CR 2039 (4-(1H-tetrazol-5-yl)-N-(4-[1H-tetrazol-5-yl]phenylbenzam ide)) a newly discovered antiallergic compound is described. ...CR 2039 inhibited dose dependently guinea-pig lung cAMP-phosphodiesterase with an IC50 of …
The pharmacological activity of CR 2039 (4-(1H-tetrazol-5-yl)-N-(4-[1H-tetrazol-5-yl]phenylbenzam ide)) a newly discovered ant …
Gateways to clinical trials.
Bayes M, Rabasseda X, Prous JR. Bayes M, et al. Methods Find Exp Clin Pharmacol. 2003 Jun;25(5):387-408. Methods Find Exp Clin Pharmacol. 2003. PMID: 12851663
This issue focuses on the following selection of drugs: AdGVVEGF121.10, anakinra, andolast, anidulafungin, APC-2059, l-arginine hydrochloride, aripiprazole, arzoxifene hydrochloride, asimadoline; Bexarotene, bimatoprost, bimosiamose, bizelesin, BMS-188667, botulinum toxin …
This issue focuses on the following selection of drugs: AdGVVEGF121.10, anakinra, andolast, anidulafungin, APC-2059, l-arginine hydro …
Efficacy of Andolast in Mild to Moderate Asthma: A Randomized, Controlled, Double-Blind Multicenter Study (The Andast Trial).
Malerba M, D Amato M, Radaeli A, Giacovelli G, Rovati L, Arshad SH, Holgate ST. Malerba M, et al. Curr Pharm Des. 2015;21(26):3835-43. doi: 10.2174/1381612821666150407101614. Curr Pharm Des. 2015. PMID: 25845448 Clinical Trial.
BACKGROUND: Andolast is a new airway specific anti-inflammatory agent. The aim of the present multicentered, randomized, placebo controlled study is to investigate whether andolast produces a therapeutic response greater than placebo in asthmatic adult patients. ... …
BACKGROUND: Andolast is a new airway specific anti-inflammatory agent. The aim of the present multicentered, randomized, placebo cont …
Andolast acts at different cellular levels to inhibit immunoglobulin E synthesis.
Malerba M, Mennuni L, Piepoli T, Caselli G, Makovec F, Rovati LC, D' Amato M, Ferrari F. Malerba M, et al. Int J Immunopathol Pharmacol. 2009 Jan-Mar;22(1):85-94. doi: 10.1177/039463200902200110. Int J Immunopathol Pharmacol. 2009. PMID: 19309555 Free article.
The anti-asthmatic agent andolast is thought to inhibit the release of allergic mediators, but its mechanism of action is not fully understood. ...Secondly, andolast reduced by about 36 percent (p<0.05) the expression of epsilon germline transcripts in PBMCs stim …
The anti-asthmatic agent andolast is thought to inhibit the release of allergic mediators, but its mechanism of action is not fully u …
Pharmacokinetics of andolast after administration of single escalating doses by inhalation in mild asthmatic patients.
Persiani S, D'Amato M, Makovec F, Arshad SH, Holgate ST, Rovati LC. Persiani S, et al. Biopharm Drug Dispos. 2001 Mar;22(2):73-81. doi: 10.1002/bdd.260. Biopharm Drug Dispos. 2001. PMID: 11745909 Clinical Trial.
Andolast was absorbed after inhalation and was available to the systemic circulation. ...Thus, the data obtained as a whole suggest that andolast pharmacokinetics are dose-independent in the dose range investigated. ...
Andolast was absorbed after inhalation and was available to the systemic circulation. ...Thus, the data obtained as a whole suggest t …
Influence of a potential anti-asthmatic drug, CR 2039, upon the anticonvulsive activity of conventional antiepileptics against maximal electroshock-induced seizures in mice.
Czuczwar SJ, Gasior M, Kozicka M, Pietrasiewicz T, Turski WA, Kleinrok Z. Czuczwar SJ, et al. J Neural Transm (Vienna). 1996;103(12):1371-9. doi: 10.1007/BF01271251. J Neural Transm (Vienna). 1996. PMID: 9029404
CR 2039 [[4-(1H-tetrazol-5-yl)-N-(4-(1H-tetrazol-5-yl]phenylbenza m ide], in doses of 10, 50, and 100 mg/kg i.p., significantly elevated the threshold for electroconvulsions, increasing the CS50 (current strength 50% in mA) values from 6.3 to 7.2, 7.5, and 7.6 mA, r …
CR 2039 [[4-(1H-tetrazol-5-yl)-N-(4-(1H-tetrazol-5-yl]phenylbenza m ide], in doses of 10, 50, and 100 mg/kg i.p., significantl …
Antiallergic and cytoprotective activity of new N-phenylbenzamido acid derivatives.
Makovec F, Peris W, Revel L, Giovanetti R, Redaelli D, Rovati LC. Makovec F, et al. J Med Chem. 1992 Oct 2;35(20):3633-40. doi: 10.1021/jm00098a006. J Med Chem. 1992. PMID: 1433173
The antiallergic activity of one of the more potent compounds of this series, i.e. 4-(1H-tetrazol-5-yl)-N-[4-(1H-tetrazol-5-yl)phenyl]benzamide (compound 44, CR 2039) was furt …
The antiallergic activity of one of the more potent compounds of this series, i.e. 4-(1H-tetrazol-5-yl)- …