the opposite effect and pure antagonists reverse the effectcausethe opposite effect and pure antagonists reverse the effect

constitutively active targets to become inactivecauseconstitutively active targets to become inactive

a negative response (= reduce baselinetriggera negative response (= reduce baseline

receptor up - regulation ... the effect of chronic exposure to anticholinergics on the expression levels of hM3-R was also testedto causereceptor up - regulation ... the effect of chronic exposure to anticholinergics on the expression levels of hM3-R was also tested

the receptor to stop signalling altogether , or at least - less than its normal baseline activitycausesthe receptor to stop signalling altogether , or at least - less than its normal baseline activity

an opposite action to that of agonistscausean opposite action to that of agonists

receptors to respond in ways opposite their response to agonists such as THC and anandamideto causereceptors to respond in ways opposite their response to agonists such as THC and anandamide

a specific response from a receptortriggera specific response from a receptor

to the opposite response to a full agonistleadingto the opposite response to a full agonist

reduced epinasty due to GABA ( Braestrup & Nielson , 1981 , Nature , 294 , 472 - 474discoverreduced epinasty due to GABA ( Braestrup & Nielson , 1981 , Nature , 294 , 472 - 474

only the first part of this activation processmay triggeronly the first part of this activation process

active receptor conformations(passive) are prevented byactive receptor conformations

changes in fluorescence that are opposite to agonist - induced alterationscausedchanges in fluorescence that are opposite to agonist - induced alterations

from three structurally diverse chemotypes ( Table EV1originatingfrom three structurally diverse chemotypes ( Table EV1

the spontaneous receptor activation by inserting relatively deep across the main ligand - binding pocket and sterically blocking the movement of TM - VI and -VII into their inward - bend , active conformationpreventthe spontaneous receptor activation by inserting relatively deep across the main ligand - binding pocket and sterically blocking the movement of TM - VI and -VII into their inward - bend , active conformation

the spontaneous receptor activation by inserting relatively deeply across the main ligand - binding pocket and sterically blocking the movement of TM - VI and TM - VII into their inward - bend , active conformationpreventthe spontaneous receptor activation by inserting relatively deeply across the main ligand - binding pocket and sterically blocking the movement of TM - VI and TM - VII into their inward - bend , active conformation

the spontaneous receptor activation by inserting relatively deep across the main ligand - binding pocket and sterically blocking the movement of TM - VI and ... into their inward - bend , active conformationpreventthe spontaneous receptor activation by inserting relatively deep across the main ligand - binding pocket and sterically blocking the movement of TM - VI and ... into their inward - bend , active conformation

literallycould ... preventliterally

conformational change that closes the ion channel bottom rightcauseconformational change that closes the ion channel bottom right

the normal baseline activity of the g - protein Adversariespreventthe normal baseline activity of the g - protein Adversaries

to treat organ specific fibrotic liver diseases , such as nonalcoholic steatohepatitis , or NASHdesignedto treat organ specific fibrotic liver diseases , such as nonalcoholic steatohepatitis , or NASH

to the identification of an INV-17 clinical compound candidate demonstrating potent in vitro pharmacological effects against TH17 cells and cytokines coupled with optimal druggable propertiesledto the identification of an INV-17 clinical compound candidate demonstrating potent in vitro pharmacological effects against TH17 cells and cytokines coupled with optimal druggable properties

to the recruitment of different corepressor complexes resulting in more pronounced repression of transcriptionleadto the recruitment of different corepressor complexes resulting in more pronounced repression of transcription

contraction of the binding pocket and the rotamer conformational change of Ser215 ( 5.46preventcontraction of the binding pocket and the rotamer conformational change of Ser215 ( 5.46

histamine from bonding with a receptor ... but they also suppress the active functional level of the receptor to below it 's normal statedo ... preventhistamine from bonding with a receptor ... but they also suppress the active functional level of the receptor to below it 's normal state

both of these occurrencesmay preventboth of these occurrences

gaggingcausegagging

this inactive state(passive) caused bythis inactive state

a decrease in GTP binding compared to baseline ... and antagonists will have little to no effect when added in isolation on baseline GTP bindingwill causea decrease in GTP binding compared to baseline ... and antagonists will have little to no effect when added in isolation on baseline GTP binding

to significant suppression of IL-17 under the same assay conditionsledto significant suppression of IL-17 under the same assay conditions

to their anxiogenic and convulsant effects.[1likely contributingto their anxiogenic and convulsant effects.[1

to the development of several orally available inverse RORhas ledto the development of several orally available inverse ROR

tolerance to antagonism through increases in receptor levelswould causetolerance to antagonism through increases in receptor levels

recruitment and up - regulation of G - protein - coupled receptors ( GPCRs ) to the cell surface ( Daeffler and Landry , 2000causerecruitment and up - regulation of G - protein - coupled receptors ( GPCRs ) to the cell surface ( Daeffler and Landry , 2000

in positive outcomes in asthmaticsmay resultin positive outcomes in asthmatics

age - related rise in plasma insulin concentration in male Zucker ratspreventage - related rise in plasma insulin concentration in male Zucker rats

to the pharmacological characterization of orphan GPCRsmay also contributeto the pharmacological characterization of orphan GPCRs

to strengthening of PPARg and corepressor NCOR2 interactionwill leadto strengthening of PPARg and corepressor NCOR2 interaction

in an increase in adenylyl cyclase activity and an increase in CRE - mediated gene transcription ( Figure 4 ; Baker and Hill , 2007however ... resultin an increase in adenylyl cyclase activity and an increase in CRE - mediated gene transcription ( Figure 4 ; Baker and Hill , 2007

to strengthening of RetCOR and NR2E3 interaction , thereby increasing the interaction of the fluorescent tags , leading to increased well FRETwill leadto strengthening of RetCOR and NR2E3 interaction , thereby increasing the interaction of the fluorescent tags , leading to increased well FRET