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searching for Inverse agonist 56 found (272 total)

alternate case: inverse agonist

Carazolol (71 words) [view diff] exact match in snippet view article find links to article

Carazolol is a high affinity inverse agonist (also referred to as a beta blocker) of the β-adrenergic receptor. Innis RB, Corrēa FM, Synder SH (1979)
Cataplexy (2,364 words) [view diff] exact match in snippet view article find links to article
histaminergic neurons by an inverse agonist of the histamine H3 receptor, which enhances histamine release in hypothalamus. An inverse agonist of the histamine H3
PSB-10 (342 words) [view diff] exact match in snippet view article find links to article
binding assay using hA3-CHO-cells indicated that PSB-10 acts as an inverse agonist (IC50 = 4 nM). It has been shown to produce antiinflammatory effects
RVD-Hpα (629 words) [view diff] exact match in snippet view article find links to article
subunit of hemoglobin which has previously been shown to act as a CB1 inverse agonist. All three polypeptides have been isolated from various mammalian species
GABRA5 (1,057 words) [view diff] exact match in snippet view article find links to article
cognitive deficit in Down syndrome. L-655,708 MRK-016 PWZ-029: moderate inverse agonist Pyridazines Ro4938581 TB-21007 GABAA receptor GRCh38: Ensembl release
Chloropyramine (643 words) [view diff] exact match in snippet view article find links to article
competitive reversible H1 receptor antagonist (also known as an H1 inverse agonist), meaning that it exerts its pharmacological action by competing with
Cholecystokinin antagonist (770 words) [view diff] exact match in snippet view article find links to article
293, YF-476, RP-69758, LY-288,513, PD-145,942 and the CCKB receptor inverse agonist L-740,093 have since been developed, and while all of the drugs developed
Risperidone (4,544 words) [view diff] exact match in snippet view article find links to article
Antagonist 5-HT1D 84.6 Antagonist 5-HT2A 0.17 Inverse agonist 5-HT2B 61.9 Inverse agonist 5-HT2C 12.0 Inverse agonist 5-HT5A 206 Antagonist 5-HT6 2,060 Antagonist
5-HT1B receptor (1,986 words) [view diff] exact match in snippet view article find links to article
Aripiprazole Isamoltane AR-A000002 SB-216,641 SB-224,289 (inverse agonist) SB-236,057 (inverse agonist) Dextromethorphan (Cough Suppressant) In humans the protein
GPR12 (322 words) [view diff] exact match in snippet view article find links to article
Brown KJ, Laun AS, Song ZH (November 2017). "Cannabidiol, a novel inverse agonist for GPR12". Biochemical and Biophysical Research Communications. 493
GPR3 (2,174 words) [view diff] exact match in snippet view article find links to article
it was recently found that cannabidiol is an inverse agonist for GPR3. The affects that the inverse agonist has are still unknown. GRCh38: Ensembl release
Noradrenergic and specific serotonergic antidepressant (494 words) [view diff] exact match in snippet view article find links to article
et al. (March 2012). "S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: I. A mechanistic
MRK-016 (166 words) [view diff] exact match in snippet view article find links to article
2,4]triazine (MRK-016), a GABAA receptor alpha5 subtype-selective inverse agonist". The Journal of Pharmacology and Experimental Therapeutics. 331 (2):
Haloperidol (4,679 words) [view diff] exact match in snippet view article find links to article
Unknown efficiency[citation needed] D2 (inverse agonist) – 0.7 nM D3 (inverse agonist) – 0.2 nM D4 (inverse agonist) – 5–9 nM σ1 (irreversible inactivation
DMCM (367 words) [view diff] exact match in snippet view article find links to article
threshold to clonic convulsions induced by DMCM, a benzodiazepine inverse agonist". Pharmacology Biochemistry and Behavior. 82 (3): 417–26. doi:10.1016/j
Perospirone (1,241 words) [view diff] exact match in snippet view article find links to article
Ki=2.9 nM) 5-HT2A (inverse agonist; Ki=1.3 nM) D2 (Ki = 0.6 nM) And the following receptor with high affinity: H1 (inverse agonist) And the following
CGS-20625 (319 words) [view diff] exact match in snippet view article find links to article
"Pharmacology of the pyrazolo-type compounds: agonist, antagonist and inverse agonist actions". Physiol. Behav. 41 (3): 241–5. doi:10.1016/0031-9384(87)90360-X
O-1238 (179 words) [view diff] exact match in snippet view article find links to article
RG (October 1999). "Structural determinants of the partial agonist-inverse agonist properties of 6'-azidohex-2'-yne-delta8-tetrahydrocannabinol at cannabinoid
Olanzapine (8,393 words) [view diff] exact match in snippet view article find links to article
408 ND 5-HT1F 310 ND 5-HT2A 1.32–24.2 Inverse agonist 5-HT2B 11.8–12.0 Inverse agonist 5-HT2C 6.4–29 Inverse agonist 5-HT3 202 Antagonist 5-HT5A 1,212 Full
L-759,633 (173 words) [view diff] exact match in snippet view article find links to article
Templeton F, Makriyannis A, Pertwee RG (February 1999). "Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656
AM-2233 (529 words) [view diff] exact match in snippet view article find links to article
cannabinoid CB1 receptor converts AM2233 from receptor agonist to inverse agonist". European Journal of Pharmacology. 531 (1–3): 41–6. doi:10.1016/j
L-759,656 (187 words) [view diff] exact match in snippet view article find links to article
Templeton F, Makriyannis A, Pertwee RG (February 1999). "Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656
Metabotropic glutamate receptor 7 (1,277 words) [view diff] exact match in snippet view article find links to article
internalization; non-glutamatergic binding component MMPIP: allosteric antagonist/inverse agonist ADX-71743 Metabotropic glutamate receptor 7 has been shown to interact
Otenabant (149 words) [view diff] exact match in snippet view article find links to article
triazolyl analogues of taranabant (MK-0364), a cannabinoid-1 receptor inverse agonist". Tetrahedron. 64 (48): 10802–10809. doi:10.1016/j.tet.2008.09.057
Fenobam (837 words) [view diff] exact match in snippet view article find links to article
potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity". J. Pharmacol. Exp. Ther. 315 (2): 711–21. doi:10.1124/jpet
GABAA receptor (5,192 words) [view diff] exact match in snippet view article find links to article
QH-ii-066 (full agonist highly selective for α5 subtype) α5IA (selective inverse agonist for α5 subtype) SL-651,498 (full agonist at α2 and α3 subtypes, and
GPR55 (1,697 words) [view diff] exact match in snippet view article find links to article
Palmitoylethanolamide ML-184, ML-185 and ML-186 Antagonists CID-16020046 - inverse agonist at GPR55 O-1918 ML-191, ML-192 and ML-193 PSB-SB-487 and PSB-SB-1203
SB-206553 (772 words) [view diff] exact match in snippet view article find links to article
PMID 20165943. Graves SM, Napier TC (June 2012). "SB 206553, a putative 5-HT2C inverse agonist, attenuates methamphetamine-seeking in rats". BMC Neuroscience. 13:
Adenosine receptor (1,930 words) [view diff] exact match in snippet view article find links to article
A1 receptor antagonist, inhibits osteoclast differentiation as an inverse agonist". Br J Pharmacol. 170 (6): 1167–1176. doi:10.1111/bph.12342. PMC 3838692
Acadia Pharmaceuticals (948 words) [view diff] exact match in snippet view article find links to article
Acadia's proprietary molecule, pimavanserin, a selective serotonin inverse agonist preferentially targeting 5-HT2a receptors. Acadia had partnered with
Ibipinabant (556 words) [view diff] exact match in snippet view article find links to article
expedient atom-efficient synthesis of the cannabinoid CB1 receptor inverse agonist ibipinabant". Tetrahedron Letters. 52 (12): 1303–1305. doi:10.1016/j
C. Robin Ganellin (1,340 words) [view diff] exact match in snippet view article find links to article
co-inventor of pitolisant, the first histamine H3-receptor antagonist/inverse agonist Wakix, for treating narcolepsy. Since graduating, Robin Ganellin has
Metabotropic glutamate receptor 1 (2,213 words) [view diff] exact match in snippet view article find links to article
antagonist FTIDC: highly potent and selective allosteric antagonist/inverse agonist A-841,720: potent non-competitive antagonist; minor hmGluR5 binding
Metabotropic glutamate receptor 1 (2,213 words) [view diff] exact match in snippet view article find links to article
antagonist FTIDC: highly potent and selective allosteric antagonist/inverse agonist A-841,720: potent non-competitive antagonist; minor hmGluR5 binding
Histamine H3 receptor (2,392 words) [view diff] exact match in snippet view article find links to article
inhibition and MAPK activity, antagonist on histamine release, and inverse agonist on arachidonic acid release) These include: A-304121 (No tolerance
Anti-inflammatory (3,452 words) [view diff] exact match in snippet view article find links to article
Honokiol from Magnolia inhibits platelet aggregation, and works as an inverse agonist at the CB2 receptor. Black seed (Nigella sativa) has shown anti-inflammatory
Zafirlukast (2,461 words) [view diff] exact match in snippet view article find links to article
some research to suggest that zafirlukast actually acts as a partial inverse agonist at the CysLT1 receptor, though zafirlukast is still classified as an
GABRA3 (2,246 words) [view diff] exact match in snippet view article find links to article
marketed drugs. Adipiplon PWZ-029 (partial agonist at α3, partial inverse agonist at α5) TP003 (Selective full agonist at α3) α3IA The GABRA3 transcript
Cariprazine (1,589 words) [view diff] exact match in snippet view article find links to article
Partial agonist 5-HT2A 18.8 Antagonist 5-HT2B 0.58 Antagonist 5-HT2C 134 Inverse agonist 5-HT7 111 Antagonist α1A 155 Antagonist D2L 0.49 ~40% Partial agonist
Honokiol (2,872 words) [view diff] exact match in snippet view article find links to article
4-O-methylhonokiol was shown to be a potent and selective cannabinoid CB2 receptor inverse agonist and to possess antiosteoclastic effects. Honokiol inhibits platelet
RAR-related orphan receptor alpha (2,661 words) [view diff] exact match in snippet view article find links to article
ovaries, and prostate. SR3335 has also been discovered as a RORα inverse agonist. CGP 52608 RAR-related orphan receptor REV-ERBα Aromatase deficiency
Agouti-related peptide (2,760 words) [view diff] exact match in snippet view article find links to article
from PVN stimulate AgRP neurons. AGRP has been demonstrated to be an inverse agonist of melanocortin receptors, specifically MC3-R and MC4-R. The melanocortin
25CN-NBOH (1,623 words) [view diff] exact match in snippet view article find links to article
in conditioned fear that was countered by pretreatment with 5-HT2AR inverse agonist MDL100907. An analytical method for the detection of 25CN-NBOH has
ZK-93423 (614 words) [view diff] exact match in snippet view article find links to article
relationship study of some benzodiazepine-receptor ligands having inverse agonist/antagonist and agonist actions". Drug Design and Discovery. 9 (2):
Agouti-signaling protein (3,316 words) [view diff] exact match in snippet view article find links to article
that may (1) affect the quality of hair pigmentation, (2) act as an inverse agonist of alpha-melanocyte-stimulating hormone, (3) play a role in neuroendocrine
Dopamine hypothesis of stuttering (1,048 words) [view diff] exact match in snippet view article find links to article
targets dopamine receptors (through silent antagonist for D1, D5 and inverse agonist for D2, D3, D4) unlike other neuroleptics as well as its effectiveness
Cannabinoid receptor type 2 (3,812 words) [view diff] exact match in snippet view article find links to article
β-Caryophyllene - - <200 nM Full agonist Phytogenic Falcarinol <1 μM Inverse agonist ? ? Phytogenic Rutamarin - - <10 μM ? Phytogenic 3,3'-Diindolylmethane
Spontaneous recovery (6,737 words) [view diff] exact match in snippet view article find links to article
partial inverse agonist, FG 7142, to the GABAA receptor resulted in attenuated recovery in both the ABA and ABB test scenarios. The GABAA receptor inverse agonist
Georges Chapouthier (1,435 words) [view diff] exact match in snippet view article find links to article
mouse lines differing in sensitivity to a benzodiazepine receptor inverse agonist". Brain Research. 787 (1): 85–90. doi:10.1016/S0006-8993(97)01483-2
Short-term effects of alcohol consumption (5,033 words) [view diff] exact match in snippet view article find links to article
PMID 2457076. Becker HC, Anton RF (1989). "The benzodiazepine receptor inverse agonist RO15-4513 exacerbates, but does not precipitate, ethanol withdrawal
Stimulant (9,445 words) [view diff] exact match in snippet view article find links to article
catecholamine transmission in the brain. Pitolisant is an H3-receptor inverse agonist. As H3 receptors mainly act as autoreceptors, pitolisant decreases
Adenosine A2A receptor antagonist (2,063 words) [view diff] exact match in snippet view article find links to article
believed it acts as an adenosine A2A receptor neutral antagonist or as an inverse agonist. Caffeine’s A2A receptor inverse agonism may be the cause of the well-known
Benzodiazepine dependence (8,454 words) [view diff] exact match in snippet view article find links to article
NMDA, and AMPA receptors. The shift of benzodiazepine receptors to an inverse agonist state after chronic treatment leads the brain to be more sensitive
Opioid (18,266 words) [view diff] no match in snippet view article find links to article
opioid receptors because their activation is not reversed by the opioid inverse-agonist naloxone, they do not exhibit high-affinity binding for classical opioids
Idiopathic hypersomnia (5,481 words) [view diff] exact match in snippet view article find links to article
apnea. Pitolisant, a selective histamine 3 (H3) receptor antagonist/inverse agonist, was approved by FDA during August 2019. It works by increasing the
List of drugs by year of discovery (2,413 words) [view diff] exact match in snippet view article find links to article
discovery Name of the drug Active ingredients 10th century Coffee Caffeine (adenosine receptor antagonist) Beta carboline (GABAA receptor inverse agonist)