Pharmacodynamic and pharmacokinetic profile of RBx 343E48F0: A novel, long acting muscarinic receptor antagonist

European Journal of Pharmacology

Volumn 658, Issue 2-3, 2011, Pages 219-228

  Gupta, Suman ^a   Malhotra, Shivani ^a   Sinha, Sandeep ^a   Singh, Shashi K ^a   Singh, Rakesh K ^a   Krishna, Siddarangaiah ^a,b   Chhabra, Pooja ^a   Chaira, Tridib ^a   Kannayiram, Janaki ^a   Sharma, Pradeep ^a   Aeron, Shelly ^a   Kaur, Jaskiran ^a,c   Kumar, Naresh ^a,d   Sattigeri, Jitendra ^a   Shirumalla, Raj K ^a   Paliwal, Jyoti ^a   Dastidar, Sunanda G ^a   Cliffe, Ian A ^a   Ray, Abhijit ^a   Bhatnagar, Pradip ^a  

^a RANBAXY RESEARCH LABORATORIES   (India)

^b SYNGENE INTERNATIONAL LTD   (India)

^c Anima Cell Metrology Inc   (United States)

^d JUBILANT BIOSYS LTD   (India)

Author keywords

Chronic Obstructive Pulmonary Disease; Intratracheal; Muscarinic receptor antagonist

Indexed keywords

3 BENZYL 1 [3 [[2 (3,3 DIFLUOROCYCLOPENTYL) 2 HYDROXY 2 PHENYLACETYL]OXY]PROPYL] 2 METHYL 1H IMIDAZOL 3 IUM BROMIDE; ACETYLCHOLINE; ACLIDINIUM BROMIDE; BRONCHODILATING AGENT; CARBACHOL; METHACHOLINE; MUSCARINIC M2 RECEPTOR; MUSCARINIC M3 RECEPTOR; MUSCARINIC RECEPTOR BLOCKING AGENT; RBX 343E45F0; TIOTROPIUM BROMIDE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BRONCHOSPASM; CONTROLLED STUDY; DOG; DOSE RESPONSE; DOSE TIME EFFECT RELATION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG RECEPTOR BINDING; DRUG RETENTION; DRUG SELECTIVITY; DRUG STRUCTURE; FEMALE; GUINEA PIG; HUMAN; IN VITRO STUDY; IN VIVO STUDY; LIGAND BINDING; NONHUMAN; PRIORITY JOURNAL; RAT; SINGLE DRUG DOSE;

ACETYLCHOLINE; ANIMALS; BRONCHOCONSTRICTION; FEMALE; GUINEA PIGS; HUMANS; IMIDAZOLES; METHACHOLINE CHLORIDE; MUSCARINIC ANTAGONISTS; RATS; RECEPTORS, MUSCARINIC; RESPIRATION, ARTIFICIAL; SUBSTRATE SPECIFICITY;

EID: 79953773310     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2011.02.024     Document Type: Article

References (23)

1. Barnes, P.J., 2003. Therapy of chronic obstructive pulmonary disease. Pharmacol. Ther. 97, 87-94.
2. Barnes, P.J., 2004. Alveolar macrophages as orchestrators of COPD. COPD 1, 59-70.
3. Barnes, P.J., Belvisi, M.G., Mak, J.C., Haddad, E.B., O'Connor, B., 1995. Tiotropium bromide (Ba 679 BR), a novel long-acting muscarinic antagonist for the treatment of obstructive airways disease. Life Sci. 56, 853-859.
4. Casarosa, P., Bouyssou, T., Germeyer, S., Schnapp, A., Gantner, F., Pieper, M., 2009. Preclinical evaluation of long-acting muscarinic antagonists: comparison of tiotropium and investigational drugs. JPET 330, 660-668.
5. Cazzola, M., Matera, M.G., 2008. Novel long-acting bronchodilators for COPD and asthma. Br. J. Pharmacol. 155, 291-299.
6. Cheng, Y., Prusoff, W.H., 1973. Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 per cent inhibition (IC50) of an enzymatic reaction. Biochem. Pharmacol. 22, 3099-3108.
7. Coulson, F.R., Fryer, A.D., 2003. Muscarinic acetylcholine receptors and airway diseases. Pharmacol. Ther. 98, 59-69.
8. Disse, B., Reichl, R., Speck, G., Traunecker, W., Ludwig, Rominger, K.L., Hammer, R., 1993. Ba 679 BR, a novel long-acting anticholinergic bronchodilator. Life Sci. 52, 537-544.
9. Fitzgerald, M.F., Fox, J.C., 2007a. Emerging trends in the therapy of COPD: novel anti-inflammatory agents in clinical development. Drug Discov. Today 12, 479-486. (Pubitemid 46795591)
10. Fitzgerald, M.F., Fox, J.C., 2007b. Emerging trends in the therapy of COPD: novel antiinflammatory agents in clinical development. Drug Discov. Today 12, 472-478.
11. Fryer, A.D., Jacoby, D.B., 1998. Muscarinic receptors and control of airway smooth muscle. Am. J. Respir. Crit. Care Med. 158, S154-S160.
12. Gross, N.J., 2004. Tiotropium bromide. Chest 126, 1946-1953. (Pubitemid 39644003)
13. Gross, N.J., 2006. Anticholinergic agents in asthma and COPD. Eur. J. Pharmacol. 533, 36-39.
14. Gross, N.J., Skorodin, M.S., 1984. Role of the parasympathetic system in airway obstruction due to emphysema. N. Engl. J. Med. 311, 421-425.
15. Haddad, E., Patel, H., Keeling, J.E., Yocoub, M.H., Barnes, P.J., Belvisi, M.G., 1999. Pharmacological characterization of the muscarinic receptor antagonist, glycopyrrolate, in human and guinea-pig airways. Br. J. Pharmacol. 127, 413-420.
16. Hanania, N.A., Donohue, J.F., 2007. Pharmacologic interventions in chronic obstructive pulmonary disease: bronchodilators. Proc. Am. Thorac. Soc. 4, 526-534.
17. Kenakin, T., 1993. Synoptic receptor function. Trends Pharmacol. Sci. 14, 431-432.
18. Koumis, T., Samuel, S., 2005. Tiotropium bromide: a new long-acting bronchodilator for the treatment of chronic obstructive pulmonary disease. Clin. Ther. 27, 377-392.
19. Lopez, A.D., Shibuya, K., Rao, C., Mathers, C.D., Hansell, A.L., Held, L.S., Schmid, V., Buist, S., 2006. Chronic obstructive pulmonary disease: current burden and future projections. Eur. Respir. J. 27, 397-412.
20. Moriya, H., Takagi, Y., Nakanishi, T., Hayashi, M., Tani, T., Hirotsu, I., 1999. Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland. Life Sci. 64, 2351-2358. (Pubitemid 29274228)
21. Sinha, S., Gupta, S., Malhotra, S., Krishna, N.S., Meru, A.V., Babu, V., Bansal, V., Garg, M., Kumar, N., Chugh, A., Ray, A., 2010. AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder. Br. J. Pharmacol. 160, 1119-1127.
22. Ten Berge, R.E., Zaagsma, J., Roffel, A.F., 1996. Muscarinic inhibitory autoreceptors in different generations of human airways. Am. J. Respir. Crit. Care Med. 154, 43-49.
23. Welte, T., Miravitlles, M., Hernandez, P., Eriksson, G., Peterson, S., Polanowski, T., Kessler, R., 2009. Efficacy and tolerability of budesonide/formoterol added to tiotropium in patients with chronic obstructive pulmonary disease. Am. J. Respir. Crit. Care Med. 180, 741-750.