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They may also be considered ligands which display both agonistic and antagonistic effects—when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist, [citation needed] competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation ...
buspirone is a selective agonist for serotonin 5-HT1A. Partial agonists (such as buspirone, aripiprazole, buprenorphine, or norclozapine) also bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist, even at maximal
3356 15558 Ensembl ENSG00000102468 ENSMUSG00000034997 UniProt P28223 P35363 RefSeq (mRNA) NM_001165947 NM_000621 NM_001378924 NM_172812 RefSeq (protein) NP_000612 NP_001159419 NP_001365853 NP_766400 Location (UCSC) Chr 13: 46.83 – 46.9 Mb n/a PubMed search Wikidata View/Edit Human View/Edit Mouse The 5-HT 2A receptor is a subtype of the 5-HT 2 receptor that belongs to the serotonin receptor ...
Lorcaserin is a full agonist for 5-HT 2C and 5-HT 2B receptors and partial agonist for 5-HT 2A receptors (75% of the maximal response elicited by serotonin). [7] Lorcaserin is a potent and selective 5-HT 2C agonist with rapid oral absorption that shows dose-dependent decrease in food intake and body weight.
Partial agonists are any chemical that can bind to a receptor without eliciting the maximum downstream response as compared to the response from a full agonist. A given partial agonist's affinity for a given receptor is also irrelevant to the consequent effect.
RO5263397 is a trace amine-associated receptor 1 (TAAR1) partial agonist to full agonist. [9] [4] Its EC 50 Tooltip half-maximal effective concentration values are 0.12 to 7.5 nM for the mouse TAAR1 (mTAAR1), 35 to 47 nM for the rat TAAR1 (rTAAR1), 251 nM at the cynomolgus monkey TAAR1, and 17 to 85 nM for the human TAAR1 (hTAAR1).
4-PhPr-2,5-DMA, also known as 4-(3-phenylpropyl)-2,5-dimethoxyamphetamine (DOPP or DOPhPr), is a serotonin receptor modulator of the phenethylamine, amphetamine, and DOx families.
Modulators that increase only the affinity of partial and full agonists allow their efficacy maximum to be reached sooner at lower agonist concentrations – i.e. the slope and plateau of a dose-response curve shift to lower concentrations. [4] Efficacy increasing modulators increase maximum efficacy of partial agonists.