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searching for Inverse agonist 69 found (297 total)

Carazolol (72 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)

GPR6 (471 words) [view diff] no match in snippet view article find links to article

G protein-coupled receptor 6, also known as GPR6, is a protein which in humans is encoded by the GPR6 gene. GPR6 is a member of the G protein-coupled receptor

Cataplexy (2,504 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

Alpha-1B adrenergic receptor (1,333 words) [view diff] exact match in snippet view article find links to article

the α1B-adrenergic receptor has been determined in complex with the inverse agonist (+)-cyclazosin. There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A

PSB-10 (349 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

Alpha-1 adrenergic receptor (1,528 words) [view diff] exact match in snippet view article find links to article

α1B-adrenergic receptor subtype has been determined in complex with the inverse agonist (+)-cyclazosin. The α1-adrenergic receptor has several general functions

GABRA5 (1,061 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 (734 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 (788 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

Α3IA (194 words) [view diff] exact match in snippet view article find links to article

α3IA, also known as GTPL4094, is an inverse agonist of the GABAA receptor. It is more selective for the α3 subunit, hence its name. Agonism of the α3

Risperidone (5,138 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 (1,984 words) [view diff] exact match in snippet view article find links to article

Isamoltane AR-A000002 GR-55562 SB-216,641 SB-224,289 (inverse agonist) SB-236,057 (inverse agonist) Dextromethorphan (Cough Suppressant) In humans the protein

GPR3 (1,905 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. Source: GPR6 GPR12 S1PR5

List of investigational autism and pervasive developmental disorder drugs (1,971 words) [view diff] exact match in snippet view article find links to article

receptor agonist Pitolisant (Wakix; tiprolisant) – histamine H3 receptor inverse agonist Racemetirosine (DL-α-methyltyrosine; L1-79) – tyrosine hydroxylase

GPR12 (346 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

Noradrenergic and specific serotonergic antidepressant (500 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):

Mitochondrial biogenesis (2,583 words) [view diff] exact match in snippet view article find links to article

Compounds that target the pathway between PGC1α and ERRα, such as the ERRα inverse agonist, XCT-790, have been found to significantly decrease mitochondrial biogenesis

Perospirone (1,253 words) [view diff] exact match in snippet view article find links to article

= 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

Jane Mellanby (1,418 words) [view diff] exact match in snippet view article find links to article

toxin act?" (1981, with Jane Green) "The effect of Ro 15-4513, an inverse agonist at the benzodiazepine receptor, on the exploratory response to novelty

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 (180 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 (9,053 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

Herbert Y. Meltzer (354 words) [view diff] exact match in snippet view article find links to article

Bahr, D; Friedman, J (2010). "Pimavanserin, a serotonin(2A) receptor inverse agonist, for the treatment of parkinson's disease psychosis". Neuropsychopharmacology

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

L-759,656 (190 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

Fenobam (839 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

AM-2233 (544 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): 41–46. doi:10.1016/j

Metabotropic glutamate receptor 7 (1,359 words) [view diff] exact match in snippet view article find links to article

LSP2-9166: mixed agonist at mGluR4 and mGluR7 MMPIP: allosteric antagonist/inverse agonist XAP044 ADX71743 Metabotropic glutamate receptor 7 has been shown to

TAS2R16 (1,677 words) [view diff] exact match in snippet view article find links to article

oxygen atom to a phenyl group. Arbutin was the first known natural inverse agonist for TAS2Rs. Many plants, including cruciferous vegetables such as broccoli

Metamizole (4,674 words) [view diff] exact match in snippet view article find links to article

and its active arachidonic acid metabolite AM404. The CB1 receptor inverse agonist AM-251 was able to reduce the cataleptic response and thermal analgesia

H4-CBD (303 words) [view diff] exact match in snippet view article find links to article

In contrast, CBD has been found to bind to the CB1 receptor as an inverse agonist/antagonist with a Ki ranging from 3.3 to 4.8 mM. In 2023 H4CBD epimers

SB-206553 (786 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:

MDA-19 (1,053 words) [view diff] exact match in snippet view article find links to article

and CB2 receptors as well as rat CB1 receptors but functions as an inverse agonist in rat CB2 receptors. MDA-19 along with its shortened Pentyl tailchain

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

GPR55 (1,704 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

Histamine H3 receptor (2,345 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

Ibipinabant (547 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

Acadia Pharmaceuticals (1,013 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

GABAA receptor (5,956 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

Metabotropic glutamate receptor 1 (2,342 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

Adenosine receptor (2,072 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

Alpha-2 adrenergic receptor (2,231 words) [view diff] exact match in snippet view article find links to article

Xylometazoline Partial agonists Oxymetazoline (also α1 agonist) TDIQ Inverse agonist Caffeine ( and methylxanthines) Antagonists 1-PP (active metabolite

Iloperidone (1,004 words) [view diff] exact match in snippet view article find links to article

affinity to serotonin 5HT2A (Ki value of 5.6 nM) where it acts as a inverse agonist. Antagonism occurs at all other receptors following Dopamine D2 (6

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):

Zafirlukast (2,484 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 (2,247 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

List of investigational antidepressants (11,184 words) [view diff] exact match in snippet view article find links to article

(ACP-103; BVF-048; Nuplazid) – serotonin 5-HT2A receptor antagonist or inverse agonist Psilocybin (COMP-360) – non-selective serotonin receptor agonist and

Cannabinol (2,084 words) [view diff] exact match in snippet view article find links to article

GPR55, GPR18, 5-HT3A, with highest potency as antagonist at TRPM8 Inverse agonist at GPR3, GPR6, and GPR12 Anti-inflammatory Anti-convulsant Potential

Dopamine hypothesis of stuttering (1,058 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

Georges Chapouthier (1,452 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

Cariprazine (2,619 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 ~30% Partial agonist

Agouti-signaling protein (3,257 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

25CN-NBOH (1,822 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. A bioanalytical method for the detection of 25CN-NBOH has

CYP2D6 (3,776 words) [view diff] exact match in snippet view article find links to article

dextromethamphetamine Lisdexamfetamine NRI atomoxetine H3 receptor antagonist/inverse agonist pitolisant chlorphenamine (antihistamine) dexfenfluramine (serotoninergic

Cannabinoid receptor 2 (3,887 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

Paliperidone (2,054 words) [view diff] exact match in snippet view article find links to article

antagonism except Paliperidone like its parent compound functions as an inverse agonist at 5-HT2A 15. Paliperidone is also active by acting as an antagonist

Short-term effects of alcohol consumption (5,429 words) [view diff] exact match in snippet view article find links to article

Becker HC, Anton RF (January 1989). "The benzodiazepine receptor inverse agonist RO15-4513 exacerbates, but does not precipitate, ethanol withdrawal

Adenosine A2A receptor antagonist (2,065 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

Methylphenidate (13,780 words) [view diff] exact match in snippet view article find links to article

have prompted the hypothesis that methylphenidate may act as a "DAT inverse agonist" or "negative allosteric modifier of the DAT" by reversing the direction

Benzodiazepine dependence (8,523 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

Radioligand (4,347 words) [view diff] exact match in snippet view article find links to article

agonists, including endogenous agonists, super agonist, full agonist, inverse agonist, and irreversible agonist. Radioligands are made up of the radioisotope

Cocaine (19,615 words) [view diff] exact match in snippet view article find links to article

evoked a hypothesis that cocaine may also function as a so-called "DAT inverse agonist" or "negative allosteric modifier of DAT" resulting in dopamine transporter

Idiopathic hypersomnia (5,193 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 (2,391 words) [view diff] exact match in snippet view article find links to article

ingredients 10th century Coffee Caffeine (adenosine receptor antagonist)[citation needed] Beta carboline (GABAA receptor inverse agonist)[citation needed]

Opioid (19,664 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

Clozapine (14,536 words) [view diff] exact match in snippet view article find links to article

receptors. It acts as an antagonist at both receptors. Clozapine is an inverse agonist at the 5-HT2A subtype of the serotonin receptor, putatively improving

Depressant (13,432 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. The nociception opioid peptide receptor (NOP) (ORL1) is an