Release enhancement

Several cholinergic strategies, other than cholinesterase inhibition, have been employed with the intention of ameliora ting the symptoms of AD. These include precursor loading acetylcholine release enhancement, and direct activation of both muscarinic and nicotinic receptors. 

Source-term turbulence, as would be caused by vessel rupture or after a turbulent jet release, enhances combustion in vapor clouds. 

Sagi, A. Segal, E. Satchi-Fainaro, R. Shabat, D. Remarkable drug-release enhancement with an elimination-based AB3 self-immolative dendritic amplifier. Bioorg. Med. Chem. 2007, 15, 3720-3727. 

CRS releases enhanced POLARA software for the drug development. Can Corp News Jan. 29, 2001. 

Mignot E, Renaud A, Nishino S, Arrigoni J, Guilleminault C, Dement WC (1993) Canine cataplexy is preferentially controlled by adrenergic mechanisms evidence using monoamine selective uptake inhibitors and release enhancers. Psychopharmacology 113 76-82... 

Increased char promotion Reduced flammability Wider range of endotherm and water release Enhanced oxide thermal barrier) )... 

Aiken SP, Lampe BJ, Murphy PA et al. (1995) Reduction of spike frequency adaptation and blockade of M-current in rat CA1 pyramidal neurons by linopirdine (DuP 996), a neurotransmitter release enhancer. Br J Pharmacol 115(7) 1163-1168... 

Schnee ME, Brown BS (1998) Selectivity of linopirdine (DuP 996), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons. J Pharmacol Exp Ther 286(2) 709—717... 

Tatavarti, A. S., and Hoag, S. W. (2006), Microenvironmental pH modulation based release enhancement of a weakly basic drug from hydrophilic matrices, J. Pharm. Sci., 95,1459-1468. 

The interaction of cyclosporine with the plasma and tissue renin-angiotensin-aldosterone systems (RAS) has been extensively studied [21, 22]. Sodium depletion, a condition that stimulates renin release, enhances acute CSA nephrotoxicity [23, 24]. In rats, CSA treatment enhanced plasma renin activity (PRA) [21, 25, 26], increased renal renin content [21], promoted juxtaglomerular hypertrophy and hyperplasia [27,... 

Ca2+ Fluxes. As can be expected, sulphonylureas increase net Ca2+ uptake along voltage-dependent Ca2+ channels (Henquin, 1980b Ammon et al., 1986) and, as far as the chemical structure is concerned, only those sulphonylureas that produce insulin release enhance uptake of Ca2+ (Heilman, 1981). Uptake of Ca2+ is associated with increased [Ca2+]j (Abrahamson et al., 1985). In HIT cells, membrane depolarization effected by the addition of glibenclamide or tolbutamide increased intracellular Ca2+ by activating voltage-dependent Ca2+ channels (Nelson et al., 1987). 

Immunoglobulin G 10-30 glass polvvinyl toluene PHEMA-PEMA platelets leucocytes fibroblasts and red cells adhesion and release enhanced (5) phagocytosis enhanced (6) adhesion prevented (7)... 

Monoamine oxidase inhibitors The MAO inhibitors increase brain amine levels by interfering with their metabolism in the nerve endings, resulting in an increase in the vesicular stores of norepinephrine and serotonin. When neuronal activity discharges the vesicles, increased amounts of the amines are released, enhancing the actions of these neurotransmitters. 

Takahashi et al. found increased dopamine release by nicotine in cigarette smokers but not in nonsmokers. Dopamine release enhances the rewarding effect of smoking in those who become dependent. Nicotine activates the ventrotegamentum area that leads to release of dopamine. 

Ocusert provides uniform controlled release (20 or 40 pg/h for 7 days) of pilocarpine as an ocular hypotensive drug and has been commercialized in 1974. Ocusert consists of two outer layers of ethylene-vinyl acetate copolymer (EVA) and an inner layer of pilocarpine in alginate gel within di-(ethylhexyl) phthalate for a release enhancer, sandwiched between EVA layers. ... 

Tam, S.W.,Tinker, W.J., Huang, S.-M., and Chorvat, R.J. (1998) 2-Fluoro-4-pyridinylmethyl analogues of linopirdine as orally active acetylcholine release-enhancing agents with good efficacy and duration of action. Journal of Medicinal Chemistry, 41, 4615—4622. 

Release enhancement Increase of the rate of the drug liberation/dissolution from the carrier... 

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