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Its poor absorption (N.B.quaternary N; absorption rate <10%) necessitates parenteral administration. Because the therapeutic effect is usually weak, a potent analgesic is given concurrently, e.g., the opioid meperidine. Note that some spasms of intestinal musculature can be effectively relieved by organic nitrates (in biliary colic) or by nifedipine (esophageal hypertension and achalasia).
This change propagates to the G-protein: the ?-subunit exchanges GDP for GTP, then dissociates from the two other subunits, associates with an effector protein, and alters its functional state. The ?-subunit slowly hydrolyzes bound GTP to GDP. G?-GDP has no affinity for the effector protein and reassociates with the ? and ? subunits (A).

 

Thus, cholesterol-containing stones can be dissolved slowly. This effect can be achieved by long-term oral administration of chenodeoxycholic acid (CDCA) or ursodeoxycholic acid (UDCA). Both are physiologically occurring, stereoisomeric bile acids (position of the 7-hydroxy group being ? in UCDA and ? in CDCA).
At rest, the intracellular concentration of free calcium ions (Ca2+) is kept at 0. 1 ?M (see p. 128 for mechanisms involved). During excitation, a transient rise of up to 10 ?M elicits contraction in muscle cells (electromechanical coupling) and secretion in glandular cells (electrosecretory coupling).

 

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