Novel subtype-selective nonpeptide bradykinin receptor antagonists FR167344 and FR173657.

abstract：:Stromal cell-derived factor-1 (SDF-1/CXCL-12) and vascular endothelial growth factor (VEGF), which can be secreted by hypoxic tumors, promote the generation of new blood vessels. These potent angiogenic factors stimulate endothelial cell migration via the activation of Rho GTPases and the phosphatidylinositol 3-kinase...

journal_title：Molecular pharmacology

authors： Carretero-Ortega J,Walsh CT,Hernández-García R,Reyes-Cruz G,Brown JH,Vázquez-Prado J

更新日期：2010-03-01 00:00:00

abstract：:Although both second messenger response systems are fully functional in both cell lines, activation of muscarinic cholinergic receptors only results in inhibition of adenylate cyclase in NG108-15 neuroblastoma X glioma cells and stimulation of phosphoinositide hydrolysis in 1321N1 human astrocytoma cells. Muscarinic r...

journal_title：Molecular pharmacology

authors： Liang M,Martin MW,Harden TK

更新日期：1987-10-01 00:00:00

abstract：:Mitochondrial disorders are devastating genetic diseases for which efficacious therapies are still an unmet need. Recent studies report that increased availability of intracellular NAD obtained by inhibition of the NAD-consuming enzyme poly(ADP-ribose) polymerase (PARP)-1 or supplementation with the NAD-precursor nico...

journal_title：Molecular pharmacology

authors： Felici R,Lapucci A,Cavone L,Pratesi S,Berlinguer-Palmini R,Chiarugi A

更新日期：2015-06-01 00:00:00

abstract：:We reported earlier that delta 9-tetrahydrocannabinol (THC), the main psychoactive ingredient in marihuana, increased markedly the level of unesterified arachidonic acid (AA) in guinea pig cerebral cortex slices prelabeled with [14C]AA. The purpose of the present study was to clarify the mechanism underlying THC-enhan...

journal_title：Molecular pharmacology

authors： Reichman M,Nen W,Hokin LE

更新日期：1991-10-01 00:00:00

abstract：:Valproic acid (VPA) is a widely used antiepileptic agent that is undergoing clinical evaluation for anticancer therapy. We assessed the effects of VPA on angiogenesis in vitro and in vivo. In human umbilical vein endothelial cells, therapeutically relevant concentrations of VPA (0.25 to 1 mM) inhibited proliferation, ...

journal_title：Molecular pharmacology

authors： Michaelis M,Michaelis UR,Fleming I,Suhan T,Cinatl J,Blaheta RA,Hoffmann K,Kotchetkov R,Busse R,Nau H,Cinatl J Jr

更新日期：2004-03-01 00:00:00

abstract：:Consequent to agonist exposure, many G protein-coupled receptors undergo sequestration or internalization. Results with receptors linked to adenylate cyclase, such as the beta 2-adrenergic receptor, or receptors linked to phospholipase C (PLC) have provided conflicting results regarding the role of second messenger-de...

journal_title：Molecular pharmacology

authors： Benya RV,Akeson M,Mrozinski J,Jensen RT,Battey JF

更新日期：1994-09-01 00:00:00

abstract：:Guanidine and its alkyl analogs stimulate the neuromuscular junction presynaptically by inhibiting voltage-gated potassium (Kv) channels, leading to enhanced release of acetylcholine in the synaptic cleft. This stimulatory effect of guanidine underlies its use in the therapy for the neuromuscular diseases myasthenic s...

journal_title：Molecular pharmacology

authors： Kalia J,Swartz KJ

更新日期：2011-12-01 00:00:00

abstract：:In PC12 cells stably expressing alpha(1A)-adrenergic receptors (ARs), norepinephrine (NE) activates several mitogen-activated protein kinase pathways and causes differentiation (). Using retroviral luciferase reporters, we found that NE also activated both signal transducers and activators of transcription (Stat) and ...

journal_title：Molecular pharmacology

authors： Zhong H,Murphy TJ,Minneman KP

更新日期：2000-05-01 00:00:00

abstract：:The interaction of [3H]acetylcholine ([3H]AcCh) with the muscarinic receptor was studied in seven distinct rat brain regions and in heart atrium by employing 10 microM atropine to define specific binding. The specific binding exhibited by the labeled neurotransmitter was found to be sensitive to muscarinic but not to ...

journal_title：Molecular pharmacology

authors： Gurwitz D,Kloog Y,Sokolovsky M

更新日期：1985-09-01 00:00:00

abstract：:Receptors from distant species may have conserved functions despite significant differences in protein sequences. Whereas the noncritical residues are often changed in distant species, the amino acids critical in receptor functions are often conserved. Studying the conserved residues between receptors from distant spe...

journal_title：Molecular pharmacology

authors： Kuei C,Yu J,Zhu J,Wu J,Zhang L,Shih A,Mirzadegan T,Lovenberg T,Liu C

更新日期：2011-11-01 00:00:00

abstract：:Immune-mediated drug hypersensitivity reactions (IDHRs) represent a significant problem due to their unpredictable and severe nature, as well as the lack of understanding of the pathogenesis. Sulfamethoxazole (SMX), a widely used antibiotic, has been used as a model compound to investigate the underlying mechanism of ...

journal_title：Molecular pharmacology

authors： Cheng L,Stewart BJ,You Q,Petersen DR,Ware JA,Piccotti JR,Kawabata TT,Ju C

更新日期：2008-06-01 00:00:00

abstract：:Nuclear receptors play important roles in the maintenance of the endocrine system, regulation of organ differentiation, and fetal development. Endocrine disruptors exert their adverse effects by disrupting the endocrine system via various mechanisms. To assess the effects of endocrine disruptors on nuclear receptors, ...

journal_title：Molecular pharmacology

authors： Kanayama T,Kobayashi N,Mamiya S,Nakanishi T,Nishikawa J

更新日期：2005-03-01 00:00:00

abstract：:The gonadotropin-releasing hormone receptor (GnRH-R) of the African catfish couples to phospholipase C and belongs to the large family of G protein-coupled receptors. We recently demonstrated that removal of the carboxyl-terminal tail (S331-Q379) from the catfish GnRH-R results in a loss of agonist binding; the curren...

journal_title：Molecular pharmacology

authors： Blomenröhr M,Heding A,Sellar R,Leurs R,Bogerd J,Eidne KA,Willars GB

更新日期：1999-12-01 00:00:00

abstract：:The ligand recognition site of A2a-adenosine receptors in rabbit striatal membranes was probed using non-site-directed labeling reagents and specific affinity labels. Exposure of membranes to diethylpyrocarbonate at a concentration of 2.5 mM, followed by washing, was found to inhibit the binding of [3H]CGS 21680 and [...

journal_title：Molecular pharmacology

authors： Jacobson KA,Stiles GL,Ji XD

更新日期：1992-07-01 00:00:00

abstract：:The effects of single and repeated electroconvulsive shock (ECS) on the binding of [3H]diprenorphine to rat brain membranes was studied. Repeated but not single ECS significantly increased the Bmax of [3H]diprenorphine binding when measured in the absence but not in the presence of NaCl. On a regional basis the effect...

journal_title：Molecular pharmacology

authors： Hitzemann RJ,Hitzemann BA,Blatt S,Meyerhoff JL,Tortella FC,Kenner JR,Belenky GL,Holaday JW

更新日期：1987-05-01 00:00:00

abstract：:Depolarization-induced 86Rb efflux, an index of K+ efflux, was developed by using mammalian cultured spinal cord neurons to study the effect of gamma aminobutyric acid (GABAB) receptor activation on Ca2(+)-activated K(+)-channels. The Ca2(+)-activated 86Rb efflux was obtained by using two methods. The first method uti...

journal_title：Molecular pharmacology

authors： Kamatchi GL,Ticku MK

更新日期：1990-09-01 00:00:00

abstract：:Equilibrative nucleoside transporters (ENTs) 1 and 2 facilitate nucleoside transport across the blood-testis barrier (BTB). Improving drug entry into the testes with drugs that use endogenous transport pathways may lead to more effective treatments for diseases within the reproductive tract. In this study, CRISPR/CRIS...

journal_title：Molecular pharmacology

authors： Miller SR,Zhang X,Hau RK,Jilek JL,Jennings EQ,Galligan JJ,Foil DH,Zorn KM,Ekins S,Wright SH,Cherrington NJ

更新日期：2021-02-01 00:00:00

abstract：:The nuclear pregnane X receptor (PXR) and constitutive androstane receptor (CAR) play central roles in protecting the body against environmental chemicals (xenobiotics). PXR and CAR are activated by a wide range of xenobiotics and regulate cytochrome P450 and other genes whose products are involved in the detoxificati...

journal_title：Molecular pharmacology

authors： Maglich JM,Stoltz CM,Goodwin B,Hawkins-Brown D,Moore JT,Kliewer SA

更新日期：2002-09-01 00:00:00

abstract：:Cholinesterase inhibitors are commonly used to improve cognition and treat psychosis and other behavioral symptoms in Alzheimer's disease, Parkinson's disease, and other neuropsychiatric conditions. However, mechanisms may exist that down-regulate the synaptic response to altered cholinergic transmission, thus limitin...

journal_title：Molecular pharmacology

authors： Volpicelli-Daley LA,Hrabovska A,Duysen EG,Ferguson SM,Blakely RD,Lockridge O,Levey AI

更新日期：2003-12-01 00:00:00

abstract：:Mitochondria contain specific Ca2+ antagonist binding sites that are associated with an inner mitochondrial membrane anion channel. These mitochondrial Ca2+ antagonist receptors can be solubilized with digitonin and partially purified [as assessed by postreversible (+/-)-[3H]nitrendipine binding] using ion exchange ch...

journal_title：Molecular pharmacology

authors： Zernig G

更新日期：1992-12-01 00:00:00

abstract：:The retinoid-related orphan receptors (RORs) and liver X receptors (LXRs) were postulated to have distinct functions. RORs play a role in tissue development and circadian rhythm, whereas LXRs are sterol sensors that affect lipid homeostasis. In this study, we revealed a novel function of RORalpha (NR1F1) in regulating...

journal_title：Molecular pharmacology

authors： Wada T,Kang HS,Angers M,Gong H,Bhatia S,Khadem S,Ren S,Ellis E,Strom SC,Jetten AM,Xie W

更新日期：2008-03-01 00:00:00

abstract：:We showed previously that subtypes of alpha 1-adrenergic receptors can be differentiated by selective inactivation with chlorethylclonidine (CEC) [Mol. Pharmacol. 32:505-510 (1987)] or by their affinities for the competitive antagonist WB 4101 [Nature (Lond.) 329:333-335 (1987)]. Examining eight rat tissues, the propo...

journal_title：Molecular pharmacology

authors： Minneman KP,Han C,Abel PW

更新日期：1988-05-01 00:00:00

abstract：:Nitric oxide (NO) possesses potent anti-inflammatory properties; however, an over-production of NO will promote inflammation and induce cell and tissue dysfunction. Thus, the ability to precisely regulate NO production could prove beneficial in controlling damage. In this study, advantage was taken of the well charact...

journal_title：Molecular pharmacology

authors： Bian K,Harari Y,Zhong M,Lai M,Castro G,Weisbrodt N,Murad F

更新日期：2001-04-01 00:00:00

abstract：:Celecoxib (CE) is a nonsteroidal anti-inflammatory drug (NSAID) that is a specific inhibitor of cyclooxygenase 2 (COX2). It is indicated for a variety of chronic inflammatory conditions, including rheumatoid arthritis. Over the last few years, adverse cardiovascular effects and increased risk for heart attacks have be...

journal_title：Molecular pharmacology

authors： Alloza I,Baxter A,Chen Q,Matthiesen R,Vandenbroeck K

更新日期：2006-05-01 00:00:00

abstract：:Freshly isolated rat hepatocytes rapidly lose their cytochrome P450 (P450) proteins and mRNAs, with no evidence of subsequent restoration, after placement into traditional systems of primary culture on type I collagen. We examined the patterns of expression of 10 constitutively expressed P450 mRNAs in rat hepatocytes ...

journal_title：Molecular pharmacology

authors： Kocarek TA,Schuetz EG,Guzelian PS

更新日期：1993-03-01 00:00:00

abstract：:Carbachol is 100 times more potent for inhibiting cyclic AMP formation than for stimulating phosphoinositide (PI) hydrolysis in chick heart cells. To determine whether this reflects differences in agonist affinity of the receptor(s) coupled to the two responses, we measured these functional responses following removal...

journal_title：Molecular pharmacology

authors： Brown JH,Goldstein D

更新日期：1986-12-01 00:00:00

abstract：:Phosphorylation of tau protein promotes stability of the axonal cytoskeleton; aberrant tau phosphorylation is implicated in the biogenesis of paired helical filaments (PHF) seen in Alzheimer's disease. Protein kinases and phosphatases that modulate tau phosphorylation have been identified using in vitro techniques; ho...

journal_title：Molecular pharmacology

authors： Garver TD,Kincaid RL,Conn RA,Billingsley ML

更新日期：1999-04-01 00:00:00

abstract：:Intermediate-conductance (KCa3.1) and small-conductance (KCa2) calcium-activated K+ channels are gated by calcium binding to calmodulin (CaM) molecules associated with the calmodulin-binding domain (CaM-BD) of these channels. The existing KCa activators, such as naphtho[1,2-d]thiazol-2-ylamine (SKA-31), 6,7-dichloro-1...

journal_title：Molecular pharmacology

authors： Brown BM,Shim H,Zhang M,Yarov-Yarovoy V,Wulff H

更新日期：2017-10-01 00:00:00

abstract：:Autophagy is a response of cancer cells to various anticancer therapies. It is designated as programmed cell death type II and characterized by the formation of autophagic vacuoles in the cytoplasm. The Akt/mammalian target of rapamycin (mTOR)/p70 ribosomal protein S6 kinase (p70S6K) and the extracellular signal-regul...

journal_title：Molecular pharmacology

authors： Aoki H,Takada Y,Kondo S,Sawaya R,Aggarwal BB,Kondo Y

更新日期：2007-07-01 00:00:00

abstract：:In the search for 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives, we have found 6-benzyl-1-(ethoxymethyl)-5-isopropyl-uracil (MKC-442) to be a highly potent and selective inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). The IC50 value of MKC-442 for HIV-1 RT was 8 nM....

journal_title：Molecular pharmacology

authors： Yuasa S,Sadakata Y,Takashima H,Sekiya K,Inouye N,Ubasawa M,Baba M

更新日期：1993-10-01 00:00:00