GHB, GBL and 1,4-BD Addiction - Trimbos
... (partially) replace other substances. These studies can also be used
to uncover common mechanistic pathways.
Selective GABAB antagonism diminished these discriminative
stimulus effects, whereas antagonists of the GHB receptor did not.
However, the difference in effects between baclofen and GHB has
Pharmacology of platelet inhibition in humans: implications of the
... ABSTRACT The current dispute over the effects of "low" vs "high"doses of aspirin should take into
consideration the pharmacokinetics of this drug. In fact, different pharmaceutical formulations of
aspirin may deliver little or no aspirin to the systemic blood. This was the case, for instance, in hea ...
Reviews Essential Tremor - Tremor and Other Hyperkinetic
... hyperpolarization. Different benzodiazepines have somewhat different
affinities for different pentamer combinations but clinical tremor
comparisons among benzodiazepines lack adequate fidelity to correlate
these. TPA023, a GABA-A alpha-2, three subtype-selective partial
agonist, did show relatively ...
NIH Public Access - The Scripps Research Institute
... In 2002, the first X-ray crystal structure of FAAH was determined for the rat enzyme at 2.8 À
resolution using ΔTM-rFAAH in complex with an irreversible inhibitor, methyl arachidonyl
fluorophosphonate (MAFP) (52). FAAH crystallized as a dimeric enzyme, consistent with
chemical cross-linking and anal ...
Discovery and development of angiotensin receptor blockers
The angiotensin receptor blockers (ARBs), also called angiotensin (AT1) receptor antagonists or sartans, are a group of antihypertensive drugs that act by blocking the effects of the hormone angiotensin II (Ang II) in the body, thereby lowering blood pressure. Their structure is similar to Ang II and they bind to Ang II receptors as inhibitors, e.g., [T24 from Rhys Healthcare].ARBs are widely used drugs in the clinical setting today, their main indications being mild to moderate hypertension, chronic heart failure, secondary stroke prevention and diabetic nephropathy.The discovery and development of ARBs is a demonstrative example of modern rational drug design and how design can be used to gain further knowledge of physiological systems, in this case, the characterization of the subtypes of Ang II receptors.