Showing papers in "Life Sciences in 1993"

TL;DR: The immunological methods described offer a novel approach with exquisite sensitivity and specificity for delineating the distribution of m1-m5 receptors in animal and human tissues.

TL;DR: Although none of the drugs was potent for [3H]dopamine uptake blockade, sertraline was the most potent (Ki = 260 nM).

TL;DR: The nature of the enzyme(s) catalyzing the major metabolic pathway of diclofenac, 4'-hydroxylation, was investigated in human liver microsomes and appears to be responsible for the oxidation of polar acidic substances such as non-steroidal anti-inflammatory drugs from different chemical classes.

TL;DR: This review summarizes the physical characteristics and distribution of angiotensin converting enzyme (E.C. 3.4.15.1), a known Ang I processing enzyme, and compares its features to what is known of prolyl endopeptidase and neutral endopePTidase 24.24.11.

TL;DR: Muscarinic receptor subtypes in the airways appear to subserve different physiological functions and anticholinergic drugs which selectively block M3 and M1-receptors may have an advantage over currently used non-selective antagonists in the treatment of airway obstruction.

TL;DR: The application of a new synthetic peptide combinatorial library, termed a positional scanning SPCL, which contains all possible hexameric combinations of 18 of the 20 natural L-amino acids, and the most active peptide found corresponded to ahexameric analogue of methionine-enkephalin.

TL;DR: Melatonin-calmodulin binding could modulate many intracellular Ca++ functions and thus, the set-point for cell activity will follow the rhythmic circulating levels of the pineal hormone.

TL;DR: Continuing clinical research involving histological examination of tissue reactions may allow a more complete determination of the effects of formoterol on inflammatory processes in humans and the clinical relevance of any such effects.

TL;DR: It is demonstrated that BQ-123 does not cross the blood-brain barrier, but endothelin acting on ETA receptor plays a role in the pathogenesis of cerebral vasoconstriction in this rat model of SAH.

TL;DR: Bullatacin, a compound isolated from plants of the Annonaceae, and its analogues show in vivo potential as antitumor agents based on their efficacy in normal mice bearing L1210 murine leukemia and athymic mice bearing A2780 conventional ovarian cancer xenografts.

TL;DR: It is concluded that although extensive data is available on 5-HT-neuroendocrine probes, there is no test that is currently available that would fulfil all the proposed requirements for a test to be acceptable, although ipsapirone, m-chlorophenylpiperazine, and possibly fenfluramine challenge tests come very close.

TL;DR: HA-containing neurons unit activity changes dramatically as a function of behavioral state across the sleep-wakefulness continuum, from 2.3 spikes/sec during active waking to virtual silence during slow wave sleep and REM sleep.

TL;DR: The results suggest that the structure of a carboxylic acid drug may predict the degree to which the corresponding acyl glucuronides will form covalent adducts that probably/possibly lead to toxicity.

TL;DR: Platelet serotonin (5-HT) studies were conducted with 12 hyperserotonemic and 12 normoserotonemic age-, sex- and relationship-matched relatives of autistic probands, finding that Hyperserotonemia of autism may be heterogeneous with one subgroup of subjects with increased 5-HT uptake and another subgroup with decreased 5- HT2 binding.

TL;DR: Ba 679 represents a novel type of antimuscarinic bronchodilator with a long duration of action, most likely due to its slow dissociation from Hm3-receptors.

TL;DR: The ability of morphine, fentanyl, butorphanol, nalbuphine, and dezocine to compete with radiolabeled ligands for binding at the mu1, mu2, kappa1, and delta opioid receptors and the sigma receptor was characterized.

TL;DR: Salmeterol was developed to provide prolonged bronchodilatation to control nocturnal symptoms and improve maintenance therapy in asthmatic patients and has greater affinity for the beta 2-adrenoceptor.

TL;DR: The results suggest that ET-1 is involved in part in the maintenance of high blood pressure in malignant hypertension, as exemplified by SHRSP.

TL;DR: Understanding how many non-mutagenic chemicals might alter normal gap junction function should form the basis of "epigenetic" toxicology and restoring normal gap junctions function to cells which have dysfunctional intercellular communication could be the basis for a new approach for therapeutic pharmaceuticals.

TL;DR: The results suggest that morphine is capable of interacting directly with opioid receptors on macrophages, resulting in a decrease in phagocytic function.

TL;DR: The results suggest that nitric oxide (NO) is involved in spinal nociceptive events, and that the increased production of NO following the nocICEptive input may diminish the efficiency of opioid antinociception in the spinal cord.

TL;DR: Rats pretreated with saline and injected daily with cocaine showed increased locomotor activity across the 21-day test period, consistent with the proposed roles of nitric oxide and NMDA-receptors in cellular adaptation and learning.

TL;DR: The cellular localization of peripheral-type benzodiazepine receptors (PBRs) was characterized in several human blood cell subpopulations including erythrocytes, platelets, monocytes and polymorphonuclear neutrophils and the PBR appears to be transcriptionally regulated.

TL;DR: This study correlates the bacteriostatic activity of papaya with its scavenging action on superoxide and hydroxyl radicals which could be part of the cellular metabolism of such enteropathogens.

TL;DR: Antagonist affinity estimates were very similar to those measured earlier in binding studies using animal tissues, and confirmed a small degree of m4 selectivity for tropicamide and secoverine.

TL;DR: The results suggest that drugs effective in blocking 5-HT2 receptors may be useful in preventing or reducing the toxic symptoms due to ergovaline in animals consuming Acremonium coenophialum infected tall fescue.

TL;DR: The peripheral-type benzodiazepine receptor (PBR) seems at best only distantly related to CBRs, and recent cDNA cloning of a PBR component, the isoquinoline binding protein (IBP), shows no apparent sequence homology with any GABAA receptor subunits known to comprise central benzod GABA receptor subtypes.

TL;DR: A survey of the histamine-releasing properties of a variety of opiates shows that the pharmacology of opiate-induced histamine release from mast cells is distinct from that of known opiate receptors.

TL;DR: It is argued that alpha 1- and alpha 2-adrenoceptors within brain and specifically within the PVN are organized in an antagonistic fashion and that the effects of various adrenergic agonists on feeding may reflect the degree to which these agonists act at alpha 1/2- andAlpha 2/2/2 receptors as well the relative balance of these receptors and their activity withinThe PVN.

TL;DR: R-PIA inhibited tumor necrosis factor production by endotoxin-stimulated human monocytes in a concentration-dependent manner with no inhibition of interleukin-6 and TNF inhibition could be an important mechanism by which adenosine analogs exert their antiinflammatory action.