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Heteroreceptor-mediated modulation of noradrenaline and acetylcholine release from peripheral nerves.
2 Heteroreceptors Modulat ing Noradrenaline Release .................................. 2.1 Muscarinic Receptors ........................................................................ 2.2 Nicotinic
Pharmacokinetics of GW433908, a Prodrug of Amprenavir, in Healthy Male Volunteers
TLDR
GW433908G tablets were well tolerated and delivered plasma amprenavir concentrations equivalent to the recommended therapeutic amprenvir dose but with fewer tablets, suggesting the possibility of a lower pill burden offered by GW4 33908 may be of clinical benefit in the treatment of HIV infection.
Purinoceptor-mediated modulation by endogenous and exogenous agonists of stimulation-evoked [3H]noradrenaline release on rat iris
TLDR
The relatively A1-selective DPCPX 10 and 100 nmol/l increased the evoked [3H]-noradrenaline overflow by about 25%–35%a indicating a minor inhibition of evoked release by endogenous purinoceptor agonists probably via an A1 adenosine receptor.
AF-DX 116 differentiates between prejunctional muscarine receptors located on noradrenergic and cholinergic nerves
TLDR
The data confirm previously reported differences between prejunctional muscarine heteroreceptors in the rat heart which belong to the cardiac subtype (M2α or M2) and autoreceptor in the guinea-pig ileum that cannot be distinguished from the ileal subtype(M2β) or (M3).
Concomitant administration of the α-glucosidase inhibitor voglibose (AO-128) does not alter the pharmacokinetics of glibenclamide
TLDR
Voglibose did not interact with glibenclamide on a pharmacokinetic level and has been proven to be safe for further clinical use.
Voglibose (AO-128) is an efficient alpha-glucosidase inhibitor and mobilizes the endogenous GLP-1 reserve.
TLDR
It is concluded that voglibose treatment effectively inhibits intestinal disaccharidases and thereby mobilizes the endogenous pool of insulinotropic GLP-1.
Muscarinic inhibition of [3H]‐noradrenaline release on rabbit iris in vitro: effects of stimulation conditions on intrinsic activity of methacholine and pilocarpine
TLDR
The results demonstrate a muscarinic inhibition of noradrenaline release from the rabbit isolated iris, and the activation by pilocarpine of the presynaptic receptors provides an alternative explanation for the miosis induced in the rabbit in vivo.
On the opioid receptor subtype inhibiting the evoked release of 3H-noradrenaline from guinea-pig atria in vitro
TLDR
The results show that the 3H-noradrenaline release can be inhibited via activation of presynaptic opioid receptors, and favour the idea that a single population (presumably of the K-subtype of opioid receptors is present at guinea-pig atrial noradrenergic nerves.
The determination of presynaptic pA2 values of yohimbine and phentolamine on the perfused rat heart under conditions of negligible autoinhibition
TLDR
The results confirm the existence of presynaptic inhibitory α2‐adrenoceptors at the adrenergic nerve fibres of the rat heart in vitro and reveal the released endogenous transmitter apparently does not activate a negative feedback mechanism, thus permitting the determination of pA2 values.
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