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Studies on alpha adrenoceptors in guinea-pig peripheral lung strips (1987)

Turner, A. J. ; Seale, J. P. ; Black, J. L. ; [et al.]

Springer

Naunyn-Schmiedeberg's archives of pharmacology 335 (1987), S. 269-273

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ISSN: 1432-1912

Keywords: Guinea-pig lung ; Noradrenaline ; Catecholamine uptake inhibitors ; α-Adrenoceptors ; Phentolamine ; Prazosin

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Summary Contractile responses of guinea-pig peripheral lung strips to noradrenaline were determined in the presence of propranolol (2.5 × 10−6 mol/l). All strips (n = 44) contracted to noradrenaline and a geometric mean EC50 of 1.4 × 10−6 mol/l (1.1 × 10−6 mol/l, 1.8 x 10−6 mol/l 95% confidence limits) was obtained. Contractions were antagonised by phentolamine (5 × 10−7−10−5 mol/l) and by prazosin (10∞−10−7 mol/l). Dose-ratios (DR) were calculated and log (DR-1) was plotted against log concentration of antagonist to yield slopes (± SE) of 0.84 ± 0.14 and 0.73 ± 0.22 respectively which were not significantly different from unity. A pA2 value (± SE) of 6.7 ± 0.2 was obtained for phentolamine and 7.5 ± 0.1 for prazosin. Yohimbine (10−7−10−5 mol/l) did not significantly affect the maximal tension generated or the EC50 values for noradrenaline. These results suggest that α1 adrenoceptors are mediating the contractile responses to noradrenaline. In the presence of cocaine (10−5 mol/l, n=18), normetanephrine (2 × 10−5 mol/l, n = 15), hydrocortisone (2.5 × 10−5 mol/l, n = 15) and normetanephrine (2 × 10−5-5 mol/l) plus cocaine (10−6 5 mol/l, n=15) pA2 values for phentolamine of 6.9, 6.7, 6.6, and 6.3 respectively were obtained. Since these pA2 values are not significantly different from 6.7, it is unlikely that this original pA2 value, which is lower than values obtained with phentolamine at α-adrenoceptors in other tissues, may be explained by neuronal or extraneuronal uptake of noradrenaline. A possible explanation may be that more than one population of α-adrenoceptors contribute to changes in tension in peripheral lung strips.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00172795

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Deuterium isotope effects on 13C NMR chemical shifts in 7,12-dimethylbenz[a]anthracene (1985)

Jones, D. W. ; Shaw, J. D.

Chichester : Wiley-Blackwell

Organic Magnetic Resonance 23 (1985), S. 787-789

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ISSN: 0749-1581

Keywords: Chemistry ; Analytical Chemistry and Spectroscopy

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: The 100.6 MHz 13C off-resonance-decoupled and polarization-transfer NMR spectra of 7,12-dimethylbenz[a]anthracene and its 5-deuteriated analogue in deuteriated chloroform solution enabled assignments of the shifts of C-3 and C-5 to be revised, and other spectral ambiguities to be reduced. Negative, i.e. upfield, deuterium-induced secondary isotope shifts, Δδ = δ(C…D) - δ(C…H), were evident over one, two, three and four bonds and, also, small apparently significant positive shifts to the methyl carbons at the 7- and 12-positions, i.e. over five and six bonds, respectively. 13C—1H coupling constants were unaffected by the deuteriation.

Additional Material: 2 Tab.