pam 1

Pam 1392 is a chemotherapeutic agent.

Pam3CSK4 TFA (Pam3Cys-Ser-(Lys)4 TFA) is a Toll-like receptor 1 2 agonist with EC50 of 0.47 ng mL for human TLR1 2.

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

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.

(Rac)-E1R is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric (Sig1R PAM) modulator of for the treatment of cognition memory disorders.

NS11394 is a effective and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of α(5) > α(3) > α(2) > α(1) at GABA(A) alpha subunit-containing receptors.

TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier. EC50 expression of TC-N 22A in BHK cells expressing human mGlu4 was 9 nM. TC-N 22A showed very low activity against mGlu 1, 2, 3, 5, and 7 receptors in excitation and forward allosteric models (EC50 >10 μM). TC-N 22A can be used in the study of central nervous system diseases.

GAT211 (AZ-4) is a selective and potent cannabinoid 1 receptor (CB1R) orthosteric modulator (PAM) with high affinity for cAMP and β-arrestin2.GAT211 has IOP-lowering and antipsychotic effects and can be used in the study of epilepsy.

LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu 5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC 50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). In vivo EEG studies demonstrated that LSN2463359 has marked wake-promoting properties with minimal rebound hypersomnolence, and it can be used for schizophrenia research [1].

TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator that induces a transient increase in intracellular Ca2+ with an EC50 of 2.37 μM in HEK cells expressing TRPC6 and enhances OAG-induced platelet aggregation.

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

V-0219 hydrochloride, an orally-active positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R), is utilized in obesity-associated diabetes research.

MMG-11 quarterhydrate is a potent and selective antagonist of human TLR2, inhibiting both TLR2 1 and TLR2 6 signaling with low cytotoxicity. The IC50 values for Pam3CSK4-induced hTLR2 1 and Pam2CSK4-induced hTLR2 6 responses are 1.7 μM and 5.7 μM, respectively [1].

(R)-V-0219, an enantiomer of V-0219, is an orally active positive allosteric modulator (PAM) of the GLP-1 Receptor (GLP-1R). It induces calcium fluxes in HEK cells that stably express hGLP-1R [1].

(S)-V-0219, an enantiomer of V-0219, is an orally active positive allosteric modulator (PAM) of the GLP-1 Receptor (GLP-1R). It activates calcium fluxes in HEK cells stably expressing hGLP-1R, demonstrating its oral activity. Additionally, (S)-V-0219 ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice [1].

VU0453379 hydrochloride is a central nervous system (CNS) penetrant and highly selective positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R), demonstrating efficacy with an EC50 of 1.3 μM [1].

UNC4976 TFA, a positive allosteric modulator (PAM) peptidomimetic of the CBX7 chromodomain, promotes binding to nucleic acids. It concurrently inhibits the H3K27me3-specific recruitment of CBX7 to target genes and enhances non-specific interaction with DNA and RNA [1].

(R)-V-0219 hydrochloride, an enantiomer of V-0219, functions as an orally active positive allosteric modulator (PAM) of the GLP-1 Receptor (GLP-1R). It induces calcium fluxes in HEK cells expressing hGLP-1R [1], highlighting its biochemical activity and potential therapeutic applications.

(S)-V-0219 hydrochloride, an enantiomer of V-0219, serves as an orally active positive allosteric modulator (PAM) of the GLP-1 Receptor (GLP-1R), enhancing calcium fluxes in HEK cells that stably express hGLP-1R. Additionally, it effectively reduces high glucose levels and suppresses feeding behavior in fasted mice [1].

A3AR modulator 1 (MRS8054), an orally active positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR) (Adenosine Receptor), significantly enhances the efficacy (E max) of Cl-IB-MECA-stimulated [35 S]GTPγS binding [1].

AMPA Receptor Modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), serves as an orally active positive allosteric modulator of the AMPA receptors (AMPAR PAMs). This compound is capable of crossing the blood-brain barrier and has been found to enhance cognitive performance and working memory in mice [1].

AMPA receptor modulator-6, an AMPA receptor positive allosteric modulator (PAM), is utilized in the research of neurological diseases [1].

Gentisuric acid, an Aspirin metabolite and a substrate of α-amidating monooxygenase (PAM), mitigates DNA damage induced by Mitomycin C. [1] [2]

DA-023 (Compound 4) acts as a selective positive allosteric modulator (PAM) of EAAT2, exhibiting an EC 50 value of 1 nM [1].