Keywords: نفوذ CNS; M1; Muscarinic acetylcholine receptor; Positive allosteric modulator (PAM); CNS penetration; Structure–activity relationship (SAR)
مقالات ISI نفوذ CNS (ترجمه نشده)
مقالات زیر هنوز به فارسی ترجمه نشده اند.
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در صورتی که به ترجمه آماده هر یک از مقالات زیر نیاز داشته باشید، می توانید سفارش دهید تا مترجمان با تجربه این مجموعه در اسرع وقت آن را برای شما ترجمه نمایند.
Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors
Keywords: نفوذ CNS; Pyrrolo[2,3-d]pyrimidine; LRRK2; Parkinson's disease; Kinase selectivity; CNS penetration;
Development of novel amide-derivatized 2,4-bispyridyl thiophenes as highly potent and selective Dyrk1A inhibitors. Part II: Identification of the cyclopropylamide moiety as a key modification
Keywords: نفوذ CNS; Dyrk1A; Neurodegenerative diseases; Cyclopropyl amide; SF3b1 phosphorylation; CNS penetration;
Continued optimization of the M5 NAM ML375: Discovery of VU6008667, an M5 NAM with high CNS penetration and a desired short half-life in rat for addiction studies
Keywords: نفوذ CNS; M5; Muscarinic acetylcholine receptor; Pharmacokinetics; CNS penetration; Structure-Activity Relationship (SAR);
Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors
Keywords: نفوذ CNS; Parkinson's disease; LRRK2 inhibitor; Arylbenzamide; CNS penetration; Kinase selectivity;
Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor
Keywords: نفوذ CNS; Positive allosteric modulator; M4; ML293; CNS penetration; Muscarinic receptor 4
Imidazopyridazinones as novel PDE7 inhibitors: SAR and in vivo studies in Parkinson's disease model
Keywords: نفوذ CNS; PDE7; Imidazopyridazinone; CNS penetration; Parkinson's disease; MPTP; Haloperidol;
Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: Identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H1-antihistamines for insomnia
Keywords: نفوذ CNS; Lead optimization; Structure-activity relationship (SAR); Benzimidazole; H1-antihistamines; Insomnia; CNS penetration;
Isothiazole and isoxazole fused pyrimidones as PDE7 inhibitors: SAR and pharmacokinetic evaluation
Keywords: نفوذ CNS; Phosphodiesterase 7 inhibitors; Isothiazolopyrimidone; Isoxazolopyrimidone; Parkinson's disease; CNS penetration;
Optimisation of a novel series of selective CNS penetrant CB2 agonists
Keywords: نفوذ CNS; CB2 agonist; CNS penetration; Benzimidazole; CB1 selective
Strategies to lower the Pgp efflux liability in a series of potent indole azetidine MCHR1 antagonists
Keywords: نفوذ CNS; MCH; Pgp; Indolyl azetidine; Dihydroindolyl azetidine; CNS penetration;
Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists
Keywords: نفوذ CNS; EP1 antagonist; Pain; CNS penetration; Scaffold hopping
Optimisation of pharmacokinetic properties to afford an orally bioavailable and selective V1A receptor antagonist
Keywords: نفوذ CNS; Peptide GPCR; Vasopressin antagonist; CNS penetration; P-glycoprotein
In vitro screening of blood-brain barrier penetration of clinically used acetylcholinesterase reactivators
Keywords: نفوذ CNS; blood-brain barrier; CNS penetration; HI-6; obidoxime; HPLC; oxime;
Passive diffusion of acetylcholinesterase oxime reactivators through the blood–brain barrier: Influence of molecular structure
Keywords: نفوذ CNS; Immobilized artificial membrane; Blood–brain barrier; CNS penetration; Reactivator; Acetylcholinesterase; HPLC
Discovery of GSK345931A: An EP1 receptor antagonist with efficacy in preclinical models of inflammatory pain
Keywords: نفوذ CNS; EP1 antagonist; Pain; Inflammatory pain; CNS penetration; Free concentration
6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective α1A adrenoceptor partial agonists
Keywords: نفوذ CNS; Alpha1a adrenoceptor; Partial agonist; Pyrroloimidazole; CNS penetration; Selectivity
Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template
Keywords: نفوذ CNS; Noradrenaline reuptake inhibitor; NRI; N-[(3S)-Pyrrolidin-3-yl]benzamides; Reduced lipophilicity; CNS penetration;
Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT2C agonists
Keywords: نفوذ CNS; 5-HT2C; Agonist; Pyrimidinone; CNS penetration
Design and synthesis of pyridazinone-based 5-HT2C agonists
Keywords: نفوذ CNS; 5-HT2C; Agonist; Pyridazinone; CNS penetration
Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP1 receptor antagonist for the treatment of inflammatory pain
Keywords: نفوذ CNS; EP1 antagonist; Inflammatory pain; Pain; CNS penetration; Microdose
Novel 2-imidazoles as potent, selective and CNS penetrant α1A adrenoceptor partial agonists
Keywords: نفوذ CNS; α1A adrenoceptor; Partial agonist; 2-Imidazole; CNS penetration; Selectivity
Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity
Keywords: نفوذ CNS; Noradrenaline reuptake inhibitor; NRI; Carbamate; H-bond acceptor capacity; CNS penetration
Discovery of brain penetrant, soluble, pyrazole amide EP1 receptor antagonists
Keywords: نفوذ CNS; Non-acidic EP1 antagonist; Amide EP1 antagonist; Brain penetration; CNS penetration; Solubility; Improved solubility; Oral exposure; Oral absorption
Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy
Keywords: نفوذ CNS; EP1 antagonist; Non-acidic EP1 antagonist; Pain; In vivo analgesic efficacy; CNS penetration
Azetidinones as vasopressin V1a antagonists
Keywords: نفوذ CNS; Vasopressin; Vasopressin V1a antagonists; Azetidinone; Oral bioavailability; CNS penetration
Cyclobutane derivatives as potent NK1 selective antagonists
Keywords: نفوذ CNS; Cyclobutane; NK1 antagonist; Substance P; CNS penetration; Oral in vivo activity