Loperamide D6 hydrochloride (R-18553 D6 hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea[1].
BU09059 is a potent, selective, short-acting kappa-opioid receptor antagonist with Ki of 1.72 nM, displays 15- and 616-fold selectivity over μ- and δ-receptors respectively; BU09059 is a potent and selective κ-antagonist with pA2 of 8.62, significantly blocks U50,488-induced antinociception in vivo (3 and 10 mg/kg), demonstrates a shorter duration of κ-antagonist action in vivo.
GS39783 is a positive allosteric modulator (PAM) of GABABR. Positive modulation of the GABABR can be used for the research of Nicotine addiction[1].
OS-3-106 is a potent, BBB-penetrated and selective dopamine D3 receptor (D3R) agonist. OS-3-106 binds with high affinity (Ki = 0.2 nM) at the D3R. OS-3-106 reduces cocaine self-administration and sucrose reinforcement rates. OS-3-106 can be used for psychostimulant addiction research[1].
Simtuzumab (AB 0024; GS 6624) is a monoclonal antibody directed against Lysyl oxidase like-2 (LOXL2). Simtuzumab can be used for the research of primary sclerosing cholangitis (PSC)[1].
Alosetron D3 Hcl is deuterium labeled Alosetron, which is a serotonin 5HT3-receptor antagonist.
Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist.
L-Phenylalanine-d1 ((S)-2-Amino-3-phenylpropionic acid-d1) is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM.IC50 value: 5 nM (reduces Aβ40 production) [1]Target: γ-secretasein vitro: MK-0752 is identified as a moderately potent γ-secretase inhibitor, which reduces Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells [1]. In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation [2]. in vivo: MK-0752 (240 mg/kg) reduces the generation of newly produced Aβ with 90% decrease of AUV in the brain of rhesus monkeys. In addition, MK-0752 treatment increases levels of Aβ 1-14, Aβ 1-15, and Aβ 1-16 , while decreases levels of Aβ 1-17 [1]. In guinea-pigs, oral administration of MK-0752 (10 mg/kg -30 mg/kg) results in the dose-dependent reduction of Aβ40 in plasma, brain and cerebrospinal fluid (CSF) with IC50 of 440 nM in brain [2].
Amitifadine hydrochloride is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with IC50s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.
GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively.
Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo[1].
Alprenolol is a non-selective beta blocker as well as 5-HT1A receptor antagonist.The reference for administration is 10 mg/kg.
Pregabalin arenacarbil is a prodrug of Pregabalin.Pregabalin is an analog of gamma-aminobutyric acid (GABA) for the research of post herpetic neuralgia, peripheral diabetic neuropathy,fibromyalgia and epilepsy[1].
MAO-B-IN-14 (Compound 9) is a potent and selective monoamine oxidase-B (MAO-B) inhibitor with an IC50 of 0.95 μM and a Ki of 0.55 μM against human MAO-B.
Piperidine-MO-1 is a modulator of dopamine receptor extracted from patent WO/2005/121087A1, compound example 2; exhibits an ED50 of 68 μmol/kg on increase of DOPAC in the rat striatum.
Dimethothiazine (Dimetotiazine; Fonazine) is an orally active tricyclic anti-histamine, anti-5-HT agent with a high activity against decerebrate rigidity, a little sedative activity and little soporific action. Dimethothiazine can reduce or abolish the effects of both static and dynamic fusimotor activity on the muscle spindle in decerebrate cat. Dimethothiazine can be used to research hemicrania and spasticity[1][2][3].
Alosetron is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.IC50 Value: Target: 5-HT ReceptorAlosetron has an antagonist action on the 5-HT3 receptors of the enteric nervous system of the gastrointestinal tract. While being a 5-HT3 antagonist like ondansetron, it is not classified or approved as an antiemetic. Since stimulation of 5-HT3 receptors is positively correlated with gastrointestinal motility, alosetron's 5-HT3 antagonism slows the movement of fecal matter through the large intestine, increasing the extent to which water is absorbed, and decreasing the moisture and volume of the remaining waste products. From Wikipedia.
Atropine methyl bromide, a muscarinic receptor (mAChR) antagonist, is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine[1][2].
rac-BHFF is a potent and orally active allosteric enhancer of GABAB receptor[1].
SKF 38393 hydrochloride is a D1 agonist with IC50 of 110 nM.IC50 value: 110 nM [1]Target: D1 agonistin vitroL SKF 38393 hydrochloride is a benzazepine selective agonist of the D1DR (dopamine D1 receptor). Agonism of the D1DR by SKF 38393 is correlated to induced desynchronization of electroencephalographic activity in rats. SKF 38393 is also reported to demonstrate agonism of the serotonin SR-2C (5-HT1C receptor). SKF 38393 HCl is an activator of D5DR. SKF 38393 is a synthetic compound of the benzazepine chemical class which acts as a selective D1/D5 receptor partial agonist. It has stimulant and anorectic effects. SKF-38393 enhances the frequency of mEPSCs in a concentration-dependent manner. SKF-38393 enhances the frequency of mEPSCs in a concentration-dependent manner. [2]
SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment[1][2][3][4][5][6].
BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM[1][2][3].
5-HT3 antagonist 2 is a 5-HT3 receptor antagonist.
FR260010 free base is a selective 5-HT2C receptor antagonist, with a Ki value of 1.1 nM[1].
Ro 04-6790 is a potent, competitive and selective 5-HT6 receptor antagonist with pKi values of 7.26, 7.35 for rat and human 5-HT6 receptors, respectively. Ro 04-6790 has no affinity at other receptors[1].
(Rac)-Lanicemine ((Rac)-AZD6765) is the racemate of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (Ki of 0.56-2.1 μM for NMDA receptor; IC50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects[1].
BChE-IN-12 (compound 12) is a potent butyrylcholinesterase (BChE) non-competitive inhibitor with an IC50 value of 2.3 μM. BChE-IN-12 can be isolated from Bletilla striata. BChE-IN-12 can be used for the research of Alzheimer's disease (AD)[1].
ST-836 Hcl is a dopamine receptor ligand; Antiparkinsonian agent.
3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifoliaWILLD, with anti-stress effect, prolonging the sleeping time in animals[1][2]. 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits[2].