METABOLISM AND DISPOSITION OF VARENICLINE, A SELECTIVE α4β2 ACETYLCHOLINE RECEPTOR PARTIAL AGONIST, IN VIVO AND IN VITRO

2005 ◽  
Vol 34 (1) ◽  
pp. 121-130 ◽  
Author(s):  
R. Scott Obach ◽  
Anne E. Reed-Hagen ◽  
Suzanne S. Krueger ◽  
Beth J. Obach ◽  
Thomas N. O'Connell ◽  
...  
Keyword(s):  
Acetylcholine Receptor ◽  
Partial Agonist

scholarly journals Functional Changes Of Fetal Muscle Acetylcholine Receptor During Mouse Development

Physiology ◽  
1998 ◽  
Vol 13 (5) ◽  
pp. 247-251
Author(s):  
Francesca Grassi ◽  
Fabrizio Eusebi
Keyword(s):  
Acetylcholine Receptor ◽  
Single Channel ◽  
Splice Variants ◽  
Mouse Development ◽  
Functional Changes ◽  
Γ Subunit ◽  
Muscle Innervation ◽  
Fetal Muscle

In developing muscles in vivo and in vitro, the acetylcholine receptor γ-subunit exists in two splice variants, conferring different single-channel open durations (τop) to reconstituted receptors. In mouse muscles, τop changes around birth, possibly as receptors incorporate either variant of γ-subunit. This might be relevant to the concomitant maturation of muscle innervation.

Effect of calcitonin on urine concentration in the rat

1983 ◽  
Vol 244 (4) ◽  
pp. F432-F435 ◽  
Author(s):  
S. Carney ◽  
T. Morgan ◽  
C. Ray ◽  
L. Thompson
Keyword(s):  
Water Permeability ◽  
Partial Agonist ◽  
Collecting Duct ◽  
Free Water ◽  
Urine Concentration ◽  
Distal Nephron ◽  
Free Water Clearance ◽  
Normal Increase

Because mammalian distal nephron segments with both calcitonin- and antidiuretic hormone- (ADH) sensitive adenylate cyclase activity have been described, in vivo and in vitro experiments were performed to study the effect of calcitonin on rat distal nephron water permeability. Calcitonin 1 and 0.1 U/ml, but not 0.01 U/ml, significantly increased the diffusional water permeability in the isolated papillary collecting duct by 15 and 11%, respectively. However, this effect was small when compared with a 68% increase with a supramaximal concentration of ADH (from 4.0 +/- 0.3 to 6.7 +/- 0.9 microns/s; n = 6, P less than 0.01). The normal increase in water permeability with increasing concentration of ADH (0.02 and 0.2 mU/ml) was depressed by the previous addition of calcitonin (1 U/ml) to the bath but was unaltered with the supramaximal ADH concentration (2 mU/ml). Verapamil, a compound that antagonizes cellular calcium entry, did not alter the effect of calcitonin on diffusional water permeability. Calcitonin in concentrations of 0.05, 0.5, and 5 U/ml produced a significant reduction in urine flow and free water clearance. Pretreatment with calcitonin in these concentrations inhibited the antidiuretic action of ADH. These studies suggest that calcitonin acts as a partial agonist to ADH within the distal nephron. It is unclear whether such an action represents a physiological or a pharmacological effect.

scholarly journals Partial agonist activity of R3(BΔ23–27)R/I5 at RXFP3 – Investigation of in vivo and in vitro pharmacology

2015 ◽  
Vol 747 ◽  
pp. 123-131 ◽  
Author(s):  
Lisbeth Kristensson ◽  
Gaëll Mayer ◽  
Karolina Ploj ◽  
Martina Wetterlund ◽  
Susanne Arlbrandt ◽  
...  
Keyword(s):  
Partial Agonist ◽  
Agonist Activity ◽  
Partial Agonist Activity ◽  
In Vitro Pharmacology
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