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Receptor agonist

To mimic melatonin action and increase the half-life is the goal of melatonin receptor agonists, which are the more recent addition to the insomnia therapeutic armamentarium. These compounds, in addition to use for insomnia, may have potential application in the synchronization of disturbed circadian rhythms, sleep disturbances in the elderly, seasonal depression and jet lag, to name a few. Furthermore, studies have shown that melatonin receptor agonists do not induce any of the hypothermic, hypotensive or bradycardic effects caused by melatonin in humans [27,28]. [Pg.68]

Melatonin receptor agonists and their relevance for the treatment of sleep disorders and major depression have been previously reviewed in Ann. Rep. Med. Chem., volume 39 [29]. Since then, ramelteon has been approved, representing an important milestone for the proof of concept of this target, and has opened new possibilities for research. [Pg.68]

Takeda s melatonin (MT1/MT2) receptor agonist ramelteon (11) was approved and launched in 2005 in the U.S., indicated for the treatment of primary insomnia characterized by difficulty with sleep onset. It is the first prescription medication for insomnia with a novel mechanism of action to reach the US market in 35 years. It is also the first and only prescription sleep medication that has not exhibited potential for abuse and dependence, and as such is not designated as a scheduled substance by the DEA. Moreover, ramelteon was also filed in late March 2007 in E.U. for primary insomnia. [Pg.68]

In controlled clinical trials in patients with primary insomnia, ramelteon 4-32 mg demonstrated significant reduction in latency to persistent sleep (LPS) compared with placebo. In elderly patients, objective and subjective LPS were also reduced at doses of 4 and 8 mg. Data on total sleep time are more variable, [Pg.68]


Nicotinic Receptor Agonists. There has been significant activity in the development of muscarinic cholinergic receptor agonists for dementia. In addition, agents that interact with nicotinic cholinergic receptors may also have therapeutic value. Nicotinic receptors have been reported to be... [Pg.99]

Phenylephrine (90) is a selective receptor agonist (+)-niguldipine (91) is a selective antagonist for the receptor. Pra2osin (92) and 5-methylurapidil (93) are nonselective a -receptor antagonists. CEC can differentiate receptors from the other receptors. Pra2osin has low and high affinity for and receptors, respectively. [Pg.535]

Table 10. GABA and GABA Receptor Agonists and Antagonists... Table 10. GABA and GABA Receptor Agonists and Antagonists...
DOI (294) and a-methyl-5-HT (295) are selective 5-HT2 receptor agonists. Ketansetin (296) and ritansetin (297) are potent and selective 5-HT2 antagonists. SB 200646 (298) is an antagonist which has greater selectivity toward 5-HT2g and receptors compared to the 5-HT2 subtype. [Pg.570]

Fig. 2. Molecular modeling of dopamine D2 receptor agonists used to define the molecular conformation needed for selective high affinity binding. Fig. 2. Molecular modeling of dopamine D2 receptor agonists used to define the molecular conformation needed for selective high affinity binding.
Phenylpropylamines are another stmctural class of receptor agonist. The two most important members are methadone [76-99-3] C2 H2yNO, (8) (17), discovered in Germany during World War II, and propoxyphene [469-62-5] C22H22NO2, (9). [Pg.383]

DM Mottola, S Laiter, VJ Watts, A Tropsha, SW Wyrick, DE Nichols, P Mailman. Conformational analysis of d dopamine receptor agonists Pharmacophore assessment and receptor mapping. J Med Chem 39 285-296, 1996. [Pg.366]

Glutamate receptor. agonists ( excitotoxins ) glutamate, kainate,... [Pg.286]

Capsaicin receptor" agonists capsaicin, resmiferatoxin II, Via voltage-gated channels maitotoxm ( ) OH ... [Pg.286]

Krogsgaard-Larsen and co-workers have protected the P-keto functionality as a ketal as a modification to the traditional conditions so attack of hydroxylamine is directed towards the ester. They prepared hydroxamic acid 10 from ester 9 then cyclized with sulfuric acid to isoxazole 11, in route to 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol (THIP), a selective GABAa receptor agonist studied clinically for insomnia. [Pg.221]


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5-HT1A receptor agonists

5-HT1A receptor partial agonist

5-HT1D receptor agonists

5-HT3 receptor agonists and

5-HT4 receptor partial agonist

5-Hydroxytryptamine receptors agonists

5-Receptor agonists pharmacological activity

8 - selective receptor agonist

A,-Adrenergic receptor agonists

A2-Adrenergic receptor agonists

A7 nicotinic receptor agonist

AMPA receptors agonists

Acetylcholine receptors agonists

Adenosine receptor agonists

Adenosine receptor agonists and antagonists

Adenosine receptor agonists antagonists

Adenosine receptor agonists effects

Adenosine receptor agonists tachycardia

Adenosine receptor agonists, and

Adenosine receptors selective agonists

Adrenergic beta-receptor agonists

Adrenergic receptor agonist antagonists

Adrenergic receptor agonist applications

Adrenergic receptor agonists and antagonists

Agonist receptor activation

Agonist receptor activity

Agonist receptor proportion with

Agonist-bound steroid hormone receptor

Agonist-directed trafficking, of receptor

Agonist-directed trafficking, of receptor stimulus

Agonist-directed trafficking, receptor

Agonist-directed trafficking, receptor evidence

Agonist-directed trafficking, receptor signaling overview

Agonist-directed trafficking, receptor stimulus

Agonist-receptor complex

Agonist-receptor interactions

Agonists GABA receptors

Agonists adrenergic receptors

Agonists at the cholinergic receptor

Agonists benzodiazepine receptor interactions with

Agonists glutamate receptors

Agonists receptor down-regulation

Agonists sigma receptors

Alpha-2 receptor agonist

Alpha-adrenergic-receptor agonists/antagonists

Alpha2-adrenergic receptor agonists

Aryl hydrocarbon receptor agonists

As vanilloid receptor agonist

Benzodiazepine receptor agonists

Benzodiazepine receptor agonists adverse effects

Benzodiazepines receptor, partial agonists

Beta-adrenergic-receptor agonists/antagonists

CCK-A receptor agonists

CCKa receptor agonists

Cannabinoid receptor agonists

Cannabinoid receptor agonists 760 Subject

Cannabinoid-1 receptor inverse agonist

Centrally acting dopamine D2 receptor agonists

Choline nicotinic receptor agonist

Cholinergic receptor agonists

Cholinomimetic) Receptor Agonists

Constitutively Active Receptors and Inverse Agonists

D-2 receptor agonists

Delta-selective opioid receptor agonists

Denufosol Tetrasodium), a Nucleotide P2Y2 Receptor Agonist

Dopamine D, receptor agonists

Dopamine D2 receptor agonists

Dopamine D3-receptor agonist

Dopamine receptor agonist

Dopamine receptor agonists antiparkinsonian

Dopamine receptor agonists nervous system

Dopamine receptor agonists sleep disorders

Dopamine-receptor agonist interactions

Epibatidine nicotinic receptor agonist

Erythropoietin receptor agonists

Estrogen receptor (3 selective agonist

Estrogen receptor agonists

Exocrine glands muscarinic receptor agonists

Gamma-aminobutyric acid receptor agonist

Glaucoma Serotonergic 5-HT2 Receptor Agonists

Glucagon-like peptide receptor agonists

Glutamate receptor agonists/antagonists

Glutamate receptors ionotropic, agonists

High-affinity agonist-receptor

Histamine receptors agonists and antagonists

Hormone Receptor Agonists

How agonists and antagonists act on receptors

Hypnotics benzodiazepine-receptor agonists

Hypotensive drug 2 receptor agonist

Insomnia benzodiazepine receptor agonists

K-Receptor agonists

K-Receptor agonists pharmacological activity

Kappa opioid receptor agonist

Kappa receptor agonists

Kappa receptors agonist-antagonists/partial agonists

Kappa-selective opioid receptor agonists

Lactate receptor , agonists

Ligand affinity agonist-receptor binding, dissociation

Liver x-receptor agonists

Loperamide, opioid receptor agonist

Melanocortin receptor agonists

Melatonin receptor agonist

Metabotropic receptors agonist structures

Motilin receptor agonist

Mu opioid receptor agonists

Muscarinic acetylcholine receptor agonists

Muscarinic cholinergic receptors selective agonists

Muscarinic receptor agonists

Muscarinic receptor agonists gastrointestinal effects

Muscarinic receptor agonists respiratory effects

Muscarinic receptor agonists specific agents

NMDA Receptor Glycine-site Agonists

NMDA receptors, agonists

Narcotic agonists opioid receptor affinities

Nicotinic Acetylcholine Receptor Agonists, Target and Selectivity Aspects

Nicotinic acetylcholine receptor agonists

Nicotinic acetylcholine receptors, neuronal agonists

Nicotinic receptor agonists antagonists

Nicotinic receptor partial agonist

Nicotinic-receptor agonists

Nonsteroidal androgen receptor agonists

ORL1 receptor agonists

Opioid receptor agonist

Opioid receptors agonist binding

Opioid receptors agonist-antagonists/partial agonists

Opioid receptors chronic agonist treatment

Opioids receptor agonists

Opioids, receptor agonists and antagonists

Other Estrogen Receptor Agonists Complexes

P-Receptor agonists

P-Receptor agonists pharmacological activity

P-adrenergic receptor agonists

P-opioid receptor agonists

P2-Adrenergic receptor agonists

P3-Adrenergic receptor agonist

Partial agonists benzodiazepine receptor interactions with

Partial opioid receptor agonists

Peripheral cannabinoid receptor agonists

Peroxisome Proliferator-Activated Receptor y-Agonists and Stroke

Peroxisome proliferator activated receptor -a agonists

Peroxisome proliferator-activated receptor 7 agonists

Peroxisome proliferator-activated receptor PPAR agonists)

Peroxisome proliferator-activated receptor PPARy) agonists

Peroxisome proliferator-activated receptor agonists thiazolidinediones

Peroxisome proliferator-activated receptor-y agonists

Peroxisome proliferator-activated receptors dual agonists

Peroxisome proliferators activator receptor PPAR) agonists

Pro-drugs of dopamine receptor agonists

Prostacyclin receptors agonists

Ragweed toll-like receptor 9 agonist vaccine

Receptor Agonist/antagonist bound

Receptor agonist binding

Receptor agonists action

Receptor agonists examples

Receptor agonists/activators

Receptor agonists/antagonists

Receptor inverse agonist

Receptor signaling agonist

Receptors agonists and antagonists

Receptors and Their Endogenous Agonist, Anandamide

Receptors hormone receptor agonists

Selective serotonin receptor agonists

Serotonin receptor agonists

Somatostatin Receptor Agonists Treatment of Excess Gastrointestinal Secretion

Somatostatin receptor agonist

Somatostatin receptor agonists found

Structure-activity relationships of dopamine receptor agonists

Test Systems Addressing 5-HT4 Receptor Agonist Activity

The Distinction between Agonist Binding and Receptor Activation

The del Castillo-Katz Mechanism 1. Relationship between Agonist Concentration and Fraction of Receptors in an Active Form

Thrombin receptor agonist peptid

Thrombin receptor agonist peptide

Thrombopoietin-receptor agonists

Thromboxane A2 Receptor Agonists

Thromboxane receptor agonists

Toll-like receptor agonists

Treatment of Circadian Rhythm Disorders using 5HT7 Receptor Agonists

Vanilloid receptor agonist

Vanilloid receptor agonist capsaicin

Vanilloid receptor agonist olvanil

Vanilloid receptor agonist structure

Vasopressin receptor agonists

Y receptor agonist

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