Pharmacological Characterization
Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization
... This study reports the design, synthesis, and pharmacological characterization of the fi rst covalent PAM for a class C GPCR. In addition, a combined computational and mutagenesis approach enabled the identi ...
11
Functional and pharmacological characterization of a Shal-related K+ channel subunit in Zebrafish
... and pharmacological properties between zShal3 and mamma- lian Kv4's (this study), it is expected that these additional zShal members will have biophysical and pharmacologi- cal properties resembling their ...
9
Nonclinical and clinical pharmacological characterization of the potent and selective cathepsin K inhibitor MIV 711
... Corresponding plasma CTX-I levels are shown in Fig. 2b. In the vehicle-treated animals, the normal diurnal rhythm in bone resorption was observed, with plasma CTX-I levels being 47% lower than baseline at 8 h post-dose ...
14
Pharmacological characterization of the ergot alkaloid receptor in the salivary gland of the ixodid tick Amblyomma hebraeum
... secreting the excess fluid of the blood meal back into the host’s circulation via the salivary glands. At least three receptors control salivary fluid secretion in the tick Amblyomma hebraeum: (1) dopamine (DA) ...
10
Pharmacological characterization of NMDA like receptors in the single celled organism Paramecium primaurelia
... Our study indicates that the swimming behaviour of paramecia is modified by NMDA and that these changes are controlled by classic receptor antagonists, suggesting the existence of NMDA-l[r] ...
9
PHARMACOLOGICAL CHARACTERIZATION OF Bunodosoma TOXINS ON MAMMALIAN VOLTAGE DEPENDENT SODIUM CHANNELS
... the pharmacological action of three toxins: BcIII (isolated from Bunodosoma caissarum), BgII and BgIII (isolated from Bunodosoma granulifera) on isolated cultured neurons of rat dorsal root ...
7
Pharmacological characterization of CGRP receptor subtypes in rat isolated smooth muscles
... the characterization of a CGRPz receptor, since [Cys(ACM^^)] ha CGRP had less than three thousandth of the activity of ha CGRP, and did not reach a maximum effect despite concentrations up to BxlO'^M, while the ...
208
In vitro pharmacological characterization of SPN-810M (molindone)
... vitro pharmacological studies described in the current manuscript demonstrate that the active substance molindone (SPN-810M) is a potent antagonist for the dopamine recep- tors, D 2S and D 2L , and the serotonin ...
9
HALOGENATED TRIAZINEDIONES BEHAVE AS ANTAGONISTS OF PKR1: IN VITRO AND IN VIVO PHARMACOLOGICAL CHARACTERIZATION
... In both experimental setting we evaluated the ability of the new compounds to quench the effects of Bv8. Bv8 is the Amphibian homologue of PROK2 which, like PROK2, displays no selectivity for either receptors, but about ...
10
Pharmacological characterization of GABAA receptors in taurine-fed mice
... Conclusions: We suggest that the elevated threshold for picrotoxin-induced seizures in taurine-fed mice is due to the reduced binding sites available for picrotoxin binding due to the re[r] ...
5
PHARMACOLOGICAL AND ELECTROPHYSIOLOGICAL CHARACTERIZATION OF A POSTSYNAPTIC MUSCARINIC RECEPTOR IN THE CENTRAL NERVOUS SYSTEM OF THE COCKROACH
... Although the vast majority of cholinergic receptors in insects exhibit nicotinic properties, conventional binding studies using muscarinic antagonists, such as quinuclidinyl benzilate (Dudai and Ben-Barak, 1977; Breer, ...
22
Synthesis and characterization of novel 1,6-dihydropyrimidine derivatives for their pharmacological properties
... on pharmacological properties of thienopyrimidines, in this work, we have undertaken the synthesis of pyrimidine derivative linked to thiophene moieties (4a–d) and ...
8
FABRICATION, CHARACTERIZATION AND PHARMACOLOGICAL ACTIVITY OF USNIC ACID LOADED NANOPARTICLES
... ABSTRACT: Usnic acid is lichen metabolite. Lichen species are the source of usnic acid. It has Antitumor and Anti-proliferation activity. Usnic acid is poorly water soluble drug. So its dissolution and bioavailability is ...
9
Mutual Amide Prodrug of Etodolac-glucosamine: Synthesis, Characterization and Pharmacological Screening
... Coupling reagent based amide synthesis is used for synthesis because of easy step synthesis with direct activation of carboxylic group of EC to generate its active form which can react with amine group of GLU directly in ...
7
Design, Synthesis, Characterization and Pharmacological Evaluation of DPP-IV Inhibitors for Antidiabetic Activity.
... The present study was conducted according to the following design DIPEPTIDYL PEPTIDASE –IV INHIBITORS FROM MEDICINAL CHEMISTRY JOURNALS 24 TRAINING SET MOLECULES AND 201 TEST SET MOLECUL[r] ...
101
Pharmacognostical Standardization Phytochemical Characterization and Pharmacological Studies of Selected Herbal Anti-Neoplastics.
... Spectral peaks of the compound AL – 168 III 19 Data showing the I.R Spectral peaks of the compounds LC – 180 I 20 Data showing the invitro cytotoxicity effects of Alangium 202 lamarckii [r] ...
284
Synthesis, characterization and pharmacological evaluation of some 1,4 dihydropyridines derivatives
... The compounds 2a and 2c–f had lower activity than the standard clotrimazole, while compound 2b was inactive Compounds 2a–f were screened for Cryptococcus neoformans, the compound 2f had [r] ...
6
Anti-inflammatory agents of the carbamoylmethyl ester class: synthesis, characterization, and pharmacological evaluation
... and pharmacological investigation of their ability to inhibit cyclo-oxygenase enzymes 1 and 2, given that gastric toxicity of NSAIDs is linked closely to the ability of these drugs to inhibit prostaglandin ...
9
CHARACTERIZATION OF PHYTOCONSTITUENTS, IN VITRO ANTIOXIDANT ACTIVITY AND PHARMACOLOGICAL INVESTIGATION OF THE ROOT EXTRACT OF TYPHONIUM TRILOBATUM
... Different concentration 200, 100, 50, 25, 12.5, 6.25 µg/ml of root extracts of this plant were subjected to this investigation and the methanol, ethanol and chloroform extracts showed ma[r] ...
12
Characterization of Phenolic Constituents and Pharmacological Activity of Achillea vermicularis
... The total phenolic contents of the extracts prepared using three different extraction methods were determined using the Folin-Ciocalteu reagent (FCR) method and the results obtained w[r] ...
9