positive allosteric modulator

V-0219 is a positive allosteric modulator of GLP-1 and can be used in studies about obesity-associated diabetes.

BMT-145027 is a positive allosteric modulator of mGluR5 without inherent agonist activity (EC50 = 47 nM).

CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases.

Tecalcet Hydrochloride (R-568 hydrochloride) is an allosteric and positive modulator of the calcium-sensing receptor(CaSR). Tecalcet Hydrochloride increases the sensitivity to the activation of extracellular Ca2+.

S 18986 is a selective, orally active, brain-penetrant positive allosteric modulator of AMPA-type receptors that enhances cognition in rodents by inducing the release of noradrenaline and acetylcholine in the rat hippocampus, subsequently improving object-recognition memory.

Positive allosteric modulator of GABAA receptors

JNJ-39393406 is an α7 nicotinic acetylcholine receptor positive allosteric modulator for the study of tobacco dependence and Alzheimer's disease.

GNE-8324 is a GluN2A selective positive allosteric modulator that selectively enhances NMDAR-mediated synaptic responses in inhibitory, but not excitatory, neurons.GNE-8324 is used in the study of neurological disorders.

VU0364770 (VU 0364770)(EC50=1.1 μM), a positive allosteric modulator(PAM) of mGlu4, shows insignificant activity at 68 other receptors, including other mGlu subtypes.

6-Methoxyflavanone (6-MeOF) is a positive allosteric modulator of the GABA response in human recombinant GABA A receptors, exhibiting antianxiety and anti-inflammatory properties, and is used to alleviate cisplatin-induced neuropathic pain.

GNE-0723 is a selective positive allosteric modulator of the NMDA receptor, with an EC50 of 21 nM for GluN2A. It can cross the blood-brain barrier (BBB) and improve outcomes in Dravet syndrome (DS) and Alzheimer's disease (AD).

GNE-5729 is a positive allosteric modulator of NMDAR with the advantage of crossing the blood-brain barrier and being orally available, with EC50 values of 37 nM, 4.7 μM and 9.5 μM for GluN2A, GluN2C and GluN2D, respectively, and can be used for the study of neurological and psychiatric disorders.

E1R is a positive sigma-1 receptor (Sig1R PAM) allosteric modulator. It has a cognition-enhancing activity.

(2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator for treating cognition and memory disorders.

(2S,3S)-E1R (Compound 2d) is an enantiomer of (2R,3R)-E1R, a sigma-1 receptor positive allosteric modulator for the treatment of cognition memory disorders.

CDPPB is a modulator of mGluR5 positive allosteric(with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5).

4-CMTB is a selective agonist of FFA2 and GPR43.It also is a positive allosteric modulator (pEC50=6.38).

GT 949 is a selective excitatory positive allosteric modulator of amino acid transporter-2 (EAAT2) with an EC50 of 0.26 nM.

L-838417 D9 (C-21191) is a novel deuterated subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].

TQS (4-Naphthalen-1-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide) is a positive allosteric modulator of α7 nACh receptors.

VPC171 is a novel adenosine A1 receptor positive allosteric modulator (PAM).

JNJ-42153605 is a mGlu2 receptor positive allosteric modulator (EC50: 17 nM).

COR659 is a GABAB positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats[1]. COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABAB receptor and an action at the cannabinoid CB1 receptor[3]. COR659 (0, 2.5, 5 and 10 mg kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats[1].COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats[2]. Animal Model: Male sP and Wistar rats[1]. [1]. Paola Maccioni, et al. Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABA B and cannabinoid CB 1 receptors. Psychopharmacology (Berl). 2017 Sep;234(17):2525-2543. [2]. Francesca Ferlenghi, et al. The GABA B receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. Eur J Pharm Sci. 2020 Dec 1;155:105544. [3]. Paola Maccioni, et al. Anti-addictive properties of COR659 - Additional pharmacological evidence and comparison with a series of novel analogues. Alcohol. 2019 Mar;75:55-66.

Loreclezole is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit-containing receptors.