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Phosphatidylinositol 4,5-bisphosphate induced flunitrazepam sensitive-GABAA receptor increase in synaptosomes from chick forebrain
(Springer/Plenum Publishers, 2007-06)
The flunitrazepam sensitive-GABAA receptor density was increased by cytochalasins C and D at 37°C suggesting that microfilament depolymerization induces exposure to the radioligand of a GABAA receptor in synaptosomes (Pharm ...
Design, synthesis, biological evaluation and binding mode modeling of benzimidazole derivatives targeting the cannabinoid receptor type 1
(Wiley-VCH Verlag, 2015)
© 2015 Wiley-VCH Verlag GmbH & Co. KGaA. A series of N-acyl-2,5-dimethoxyphenyl-1H-benzimidazoles were designed based on a CoMFA model for cannabinoid receptor type 1 (CB1) ligands. Compounds were synthesized and radioligand ...
N-SUBSTITUTION AND á1-ADRENERGIC RECEPTOR AFFINITY OF LAUDANOSINE ANALOGUES
(Sociedad Chilena de Química, 2006)
Adenosine receptor ligands: Coumarin–Chalcone hybrids as modulating agents on the activity of hARs
(MDPI AG, 2020-09)
Adenosine receptors (ARs) play an important role in neurological and psychiatric disorders such as Alzheimer’s disease, Parkinson’s disease, epilepsy and schizophrenia. The different subtypes of ARs and the knowledge on ...
Receptor binding mode and pharmacological characterization of a potent and selective dual CXCR1/CXCR2 non-competitive allosteric inhibitor
(Wiley Blackwell Publishing, Inc, 2012-01)
Background and Purpose: DF 2156A is a new dual inhibitor of IL-8 receptors CXCR1 and CXCR2 with an optimal pharmacokinetic profile. We characterized its binding mode, molecular mechanism of action and selectivity, and ...
Characterization of tachykinin NK2 receptor in the anterior pituitary gland
(Pergamon-Elsevier Science Ltd, 2003-09)
Tachykinins are a family of bioactive peptides that interact with three subtypes of receptors: NK1, NK2 and NK3. Substance P has greater affinity for NK1, and neurokinin A (NKA) for NK2 receptor subtype. Although only NK1 ...
Increased density of alpha-adrenoceptors in vas-deferens of spontaneously hypertensive rats (SHR), indicated by functional and receptor-binding studies
(Elsevier B.V., 1992-07-21)
Pharmacological parameters were determined from contractile responses mediated by alpha-adrenoceptors in vas deferens from spontaneously hypertensive rats (SHR) and corresponding normotensive controls, Wistar Kyoto rats ...
The role of the agonist binding site in Ca2+ inhibition of the recombinant 5-HT3A receptor
(2001)
The mechanism and site of action of Ca2+ at the recombinant murine 5-hydroxytryptamine (5-HT)3A receptor were investigated using whole-cell voltage clamp, radioligand binding and single-cell Ca2+ imaging. Inhibition of the ...
N-substitution and alpha(1)-adrenergic receptor affinity of laudanosine analogues
(SOCIEDAD CHILENA DE QUIMICA, 2006-09)
Benzyltetrahydroisoquinoline (BTHIQ) molecules are able to adopt widely differing conformations that depend on the presence or absence of N-substituents. To assess the possible role of BTHIQ conformation on the affinity ...
Sino-aortic denervation causes right atrial beta adrenoceptor down-regulation
(Williams & Wilkins, 1997-02-01)
Rat isolated right atria obtained 1 wk after sinoaortic denervation were less sensitive to the chronotropic actions of beta-agonists than were tissues obtained from animals that underwent sham surgery or no surgery at all. ...