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Receptor agonist

Metabolomic study and in silico approach of DLBS1442 as progesterone receptor agonist

Metabolomic study and in silico approach of DLBS1442 as progesterone receptor agonist

... Virtual screening protocol validation for a PR agonist bind to asoprisnil crystalline structure was performed retrospectively. DUD/DUD-E is an example of a benchmark designed for validating virtual screening ...

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Dynamic regulation of leukocyte beta adrenergic receptor agonist interactions by physiological changes in circulating catecholamines

Dynamic regulation of leukocyte beta adrenergic receptor agonist interactions by physiological changes in circulating catecholamines

... binding agonist with a high affinity from a mean (+/- SEM) of 42 +/- 5 to 24 +/- 2% (P less than ...binding agonist with a high affinity were seen after infusion of ...

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Disruption of Drug Effects (Dopamine, Nicotine, Pilocarpine, κ Opioid) in Planarians by UV Light

Disruption of Drug Effects (Dopamine, Nicotine, Pilocarpine, κ Opioid) in Planarians by UV Light

... by receptor-binding ...D2 receptor antagonist (–)sulpiride ...acetylcholine receptor agonist nicotine (1, 3, 5 mM) and the selective mus- carinic acetylcholine receptor agonist ...

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Study to Evaluate the Effect of Dexmedetomidine in Attenuating the Hemodynamic and Neuroendocrinal Responses to Skull-Pin Head-Holder Application during Craniotomy

Study to Evaluate the Effect of Dexmedetomidine in Attenuating the Hemodynamic and Neuroendocrinal Responses to Skull-Pin Head-Holder Application during Craniotomy

... It is a pure α 2 agonist receptor agonist α1:α2 ratio – 1:1600 than clonidine which has only less selective agonist activity α1:α2 ratio 1:200 In this study which was carried out in the [r] ...

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Eye and heart morphogenesis are dependent on melatonin signaling in chick embryos

Eye and heart morphogenesis are dependent on melatonin signaling in chick embryos

... melatonin receptor immunofluorescence was distributed in the optic cups and rudimentary ...(melatonin receptor agonist) groups had regular optic cups and an S-shaped heart, while those from the ...

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Ospemifene for the treatment of dyspareunia associated with vulvar and vaginal atrophy: potential benefits in bone and breast

Ospemifene for the treatment of dyspareunia associated with vulvar and vaginal atrophy: potential benefits in bone and breast

... estrogen receptor modulator (SERM), or estrogen receptor agonist/antagonist, that was recently approved by the US Food and Drug Administration for the treatment of dyspareunia associated with vulvar ...

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Laxative effects and mechanism of action of Brazilian green propolis

Laxative effects and mechanism of action of Brazilian green propolis

... opioid receptor agonist) and clonidine (an α -2 adrenergic receptor ...acetylcholine receptor antagonist (atropine), but not by a 5-HT receptor antagonist ...

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Reduced beta adrenergic receptor activation decreases G protein expression and beta adrenergic receptor kinase activity in porcine heart

Reduced beta adrenergic receptor activation decreases G protein expression and beta adrenergic receptor kinase activity in porcine heart

... antagonist treatment (bisoprolol, 0.2 mg/kg per d i.v., 35 d) on components of the myocardial beta-adrenergic receptor-G-protein-adenylyl cyclase pathway in porcine myocardium. Three novel alterations in cardiac ...

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Octopamine partially restores walking in hypokinetic cockroaches stung by
the parasitoid wasp Ampulex compressa

Octopamine partially restores walking in hypokinetic cockroaches stung by the parasitoid wasp Ampulex compressa

... DA receptor agonists had no measurable effects on spontaneous walking of stung ...be receptor specific. SKF 82958, a D1 DA receptor agonist, had no effect on walking, whereas quinpirole, a D2 ...

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Modulatory Effects of Dopamine D2 Receptors on Spreading Depression in Rat Somatosensory Neocortex

Modulatory Effects of Dopamine D2 Receptors on Spreading Depression in Rat Somatosensory Neocortex

... (i) control period, neocortical slices were superfused with ACSF (30 min), tested for spontaneous SD; (ii) KCl injection, induction of SD (SD1); (iii) application of D 2 dopamine receptor agonist ...

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GnRH-agonist implantation of prepubertal male cats affects their reproductive performance and testicular LH receptor and FSH receptor expression

GnRH-agonist implantation of prepubertal male cats affects their reproductive performance and testicular LH receptor and FSH receptor expression

... (2016) 'GnRH-agonist implantation of prepubertal male cats affects their reproductive performance and testicular LH receptor and FSH receptor expression', Theriogenology, 85(5), 841-84[r] ...

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Leukocyte beta receptor alterations in hypertensive subjects

Leukocyte beta receptor alterations in hypertensive subjects

... the agonist isoproterenol was significantly reduced in hypertensives and was associated with a reduction in the proportion of beta-receptors binding agonist with a high affinity from 42 +/- 6% in ...

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Differential regulation of renal phospholipase C isoforms by catecholamines

Differential regulation of renal phospholipase C isoforms by catecholamines

... phospholipase C (PLC) activity, but whereas dopamine produces a natriuresis, NE has an antinatriuretic effect. To determine if catecholamines differentially regulate the expression of PLC isoforms, we infused fenoldopam, ...

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A Novel Gaba Receptor in the Heart of a Primitive Arthropod, Limulus Polyphemus

A Novel Gaba Receptor in the Heart of a Primitive Arthropod, Limulus Polyphemus

... The Limulus heart receptor has an agonist profile Table ID very similar to at least one well-characterized vertebrate GABA A receptor Barker and Mathers, 1981, but it has a different GAB[r] ...

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Different skeletal effects of the peroxisome proliferator activated receptor (PPAR)α agonist fenofibrate and the PPARγ agonist pioglitazone

Different skeletal effects of the peroxisome proliferator activated receptor (PPAR)α agonist fenofibrate and the PPARγ agonist pioglitazone

... Rats treated with pioglitazone exhibited the opposite skel- etal response. They had a significantly lower whole body BMD and BMC, and tended to have a lower femoral BMD. These data were further corroborated by ...

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Effects of Ovariectomy and 17β Estradiol Replacement on Dopamine D2 Receptors in Female Rats: Consequences on Sucrose, Alcohol, Water Intakes and Body Weight

Effects of Ovariectomy and 17β Estradiol Replacement on Dopamine D2 Receptors in Female Rats: Consequences on Sucrose, Alcohol, Water Intakes and Body Weight

... Other mechanisms which influenced food consumption and body weight, re- lated to steroidal hormones, in particular the 17 β -estradiol (estradiol or E2) in females. There was tangible evidence that the 17 β -estradiol ...

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Smoking cessation in Asians: focus on varenicline

Smoking cessation in Asians: focus on varenicline

... partial agonist for the nicotinic acetylcholine receptor α 4 β 2 subtype, which is believed to be responsible for mediating the reinforcing properties of ...an agonist, stim- ulating the release of ...

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Abnormalities in G protein coupled signal transduction pathways in human disease

Abnormalities in G protein coupled signal transduction pathways in human disease

... Loss of function mutations include those that disrupt synthesis or targeting of signal transduction components, as well as those that impair agonist binding to receptor, receptor-G prote[r] ...

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The C F bond as a conformational probe in agonist receptor interactions

The C F bond as a conformational probe in agonist receptor interactions

... Capsaicin 46 is an active pain stimulant that is responsible for the pungency in chili peppers. Capsaicin is currently used as an analgesic and there is a continuous effort to develop analogues as potent painkillers. ...

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The need for new acutely acting antimigraine drugs: moving safely outside acute medication overuse

The need for new acutely acting antimigraine drugs: moving safely outside acute medication overuse

... CGRP receptor blockade, chronic and fre- quent administration of gepants has been attempted in clinical trials investigating prophylactic treatment of mi- graine [19, 84, 96, 97], and chronic blockade of the CGRP ...

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