Biomedical subjects

R A Fairhurst

Publications and source records attributed to R A Fairhurst.

3 recordsLinked to original sources

PubMed2006

Effect of indacaterol, a novel long-acting beta2-agonist, on isolated human bronchi.

Indacaterol is a novel beta2-adrenoceptor agonist in development for the once-daily treatment of asthma and chronic obstructive pulmonary disease. The present study evaluated the relaxant effect of indacaterol on isolated human bronchi obtained from lungs of patients undergoing surgery for lung carcinoma. Potency (-logEC50), maximal relaxant effect (Emax) and onset of action were determined at resting tone. Duration of action was determined against cholinergic neural contraction induced by electrical field stimulation (EFS). At resting tone, -logEC50 and Emax values were 8.82+/-0.41 and 77+/-5% for indacaterol, 9.84+/-0.22 and 94+/-1% for formoterol, 8.36+/-0.16 and 74+/-4% for salmeterol, and 8.43+/-0.22 and 84+/-4% for salbutamol, respectively. In contrast to salmeterol, indacaterol did not antagonise the isoprenaline response. Indacaterol's onset of action (7.8+/-0.7 min) was not significantly different from that of formoterol (5.8+/-0.7 min) or salbutamol (11.0+/-4.0 min), but it was significantly faster than that of salmeterol (19.4+/-4.3 min). EFS-induced contractions were inhibited with -logIC50 values of 6.96+/-0.13 (indacaterol), 8.96+/-0.18 (formoterol), 7.18+/-0.34 (salmeterol) and 6.39+/-0.26 (salbutamol). Duration of action was >12 h for indacaterol and salmeterol, and 35.3+/-8.8 and 14.6+/-3.7 min for formoterol and salbutamol, respectively. In isolated human bronchi, indacaterol behaved as a long-acting beta2-adrenoceptor agonist with high intrinsic efficacy and fast onset of action.

Adrenergic beta-Agonists↗

PubMed1995

4,7-Dimethoxybenzo[c]furan.

The title compound, C10H10O3, is nearly planar with a maximum deviation from planarity of 0.140 (2) A for methoxy atom C11. The geometry of the benzo[c]furan moiety is indicative of a non-aromatic ring system. The bond lengths more closely resemble those of two non-interacting diene systems than those of an aromatic one. There are alternating long and short bond lengths around the ring skeleton with the long and short C-C bonds averaging 1.437 (2) and 1.354 (2) A, respectively. There are close C-H ... O intermolecular contacts which may help stabilize the molecule in the solid state.

Benzofurans↗

PubMed1995

Two [7.3.1]azabicyclo-z-3-ene-1,5-diyne analogues of dynemicin A.

The crystal structures of methyl 6-methoxy-17-oxo-2-azatricyclo[7.7.1.0(3,8)]heptadeca-3(8),4 ,6,13-tetraene- 11,15-diyne-2-carboxylate ethyl acetate solvate, (1), 2C19H15NO4.0.5C4H8O2, and tricyclo[3.3.1.1(3,7)]decyl 6-methoxy-17-oxo-2-azatricyclo[7.7.1.0(3,8)]heptadeca-3(8),4 ,6,13-tetraene- 11,15-diyne-2-carboxylate ethyl acetate solvate, (2), C28H27NO4.0.5C4H8O2, are reported. For compound (1), two crystallographically independent molecules are observed. Interestingly, for both compounds (1) and (2), a molecule of ethyl acetate is found in the crystal lattice disordered about an inversion center. The azabicyclo[7.3.1]enediyne core appears to be fairly rigid. Only minor differences are observed in the ring conformation between the two independent molecules in (1) and between compounds (1) and (2) themselves. The conformation is also similar to that found in deoxydynemicin A [Shiomi, Iinuma, Naganawa, Hamada, Hattori, Nakamura, Takeuchi & Iitaka (1990). J. Antibiot. 43, 1000-1005] and triacetyldynemicin A [Konishi, Ohkuma, Tsuno, Oki, Van Duyne & Clardy (1990). J. Am. Chem. Soc. 112, 3715-3716]. The transannular diyne distance (C3...C8) averages 3.428 (2) A for compound (1) and is 3.403 (3) A for compound (2).

Anthraquinones↗