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A8800 Alprazolam Alprazolam binds the GABAA receptor at the benzodiazepine site, which is different than the ligand-binding site at which GABA binds. Alprazolam has been shown to be an anxiolytic (anti-anxiety agent) as well as having anticonvulsant, muscle relaxant and antidepressant activity.
 
A2861 Astemizole ≥98% (HPLC) Astermizole is a potent hERG potassium channel blocker (IC50 of 0.9 nM) and may used as a pharmacological chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels. It has also been studied for treatment of malaria, hERG and hEAG channel function in cancer and as a second generation antihistamine H-1 antagonist.
 
B5016 Bepridil hydrochloride powder Non-selective calcium channel blocker and class IV antiarrhythmic agent; inhibits Na+-Ca2+ exchange; inhibits growth of brain tumor cells in vitro.
 
C0246 Cabergoline ≥98% (HPLC) Cabergoline, a lysergic acid amide derivative, is a potent dopamine D2 receptor agonist. It also acts on dopamine receptors in lactophilic hypothalamus cells to suppress prolactin production in the pituitary gland. It has been used for monotherapy of Parkinson′s disease in the early phase; combination therapy, together with levodopa and a decarboxylase inhibitor such as carbidopa, in progressive-phase Parkinson′s disease and adjunctive therapy of prolactin-producing pituitary gland tumors (microprolactinomas).
 
C3742 Chk2 Inhibitor II hydrate ≥98% (HPLC) Chk2 Inhibitor II is a checkpoint kinase 2 inhibitor, which controls the p53 response to DNA breaks induced by radiation, leading to apoptosis. Protection of T-cells from apoptosis implies use as an adjuvant for radiation therapy in cancer. IC50 = 15 nM; Ki = 37 nM. Chk2 Inhibitor II shows 1000-fold greater selectivity for the Chk2 serine/threonine kinase than for the Cdk1/B and CK1 kinases (for which IC50 = 12 μM and 17 μM, respectively). Chk2 Inhibitor II weakly inhibits a panel of 31 other kinases (<25% inhibition at a concentration of 10 μM and prevents apoptosis of human CD4+ and CD8+ T-cells subjected to ionizing radiation (EC50 = 3 μM and 7.6 μM, respectively).
human ... CHEK2(11200)
C4397 Chlorzoxazone Chlorzoxazone is a skeletal muscle relaxant.
 
C5270 Cinnarizine powder Ca2+ channel blocker; central and peripheral vasodilator.
human ... CACNA1A(773), DRD2(1813), HRH1(3269)
C4740 Cisapride monohydrate ≥98% (HPLC), solid 5-HT4 serotonin receptor agonist.
 
C4542 Cyclobenzaprine hydrochloride Skeletal muscle relaxant; reduces muscle spasm by depression of brainstem neurons; 5-HT2 serotonin receptor antagonist.
human ... HTR2A(3356), HTR2B(3357), HTR2C(3358)
D1446 Dexrazoxane ≥95% (HPLC) Dexrazoxane is a cardioprotective compound against anthracyclines. It functions by inhibiting topoisomerase II without inducing DNA strand breaks. Dexrazoxane is a + enantiomer of razoxane.
 
D3630 Diphenhydramine hydrochloride ≥98% (HPLC) H1 histamine receptor antagonist
human ... HRH1(3269)
D122 Domperidone powder, ≥98% (HPLC) Peripheral dopamine receptor antagonist that does not cross the blood-brain barrier; anti-emetic.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816), KCNH2(3757)
rat ... Drd1a(24316), Drd2(24318), Drd3(29238), Htr3a(79246)
D1414 Droperidol D1, D2 dopamine receptor antagonist; butyrophenone antipsychotic and anti-emetic.
human ... DRD1(1812), DRD2(1813), KCNH1(3756), KCNH2(3757)
E2661 Estropipate ≥98% (HPLC), powder Estropipate is the piperazine salt of the estrogen receptor agonist estrone-3-sulfate and a potent, specific inhibitor of the organic anion transporting polypeptide 1B1 (OATP1B1, IC50 = 60 nM).
 
E6530 Etomidate >98% (HPLC), powder Etomidate is a general anesthetic; potentiates GABAA transmission. The possible neuroprotective effect of etomidate against streptozotocin-induced (STZ-induced) hyperglycaemia were investigated in the rat brain and spinal cord. Etomidate treatment demonstrated neuroprotective effect on the neuronal tissue against the diabetic oxidative damage
human ... GABRA1(2554)
F6889 Famotidine H2 histamine receptor antagonist; anti-ulcer agent
human ... HRH2(3274)
F0430 Fenobam ≥98% (HPLC), solid Fenobam is a potent, selective, noncompetitive glutamate mGluR5 receptor antagonist. Fenobam displays inverse agonist properties; blocks mGluR5 constitutive activity in vitro (IC50 = 87 nM, slightly weaker than MPEP). Fenobam acts at an allosteric modulatory site shared with MPEP and binds the mGlu5 receptor with Kd values of 54 and 31 nM for rat and human receptors, respectively. Fenobam belongs to a structurally different class than MPEP; devoid of GABAergic activity and thus typical benzodiazepine-like side effects; displays anxiolytic activity.
 
F8304 Flavoxate hydrochloride ≥98% (HPLC), solid L-type Ca2+ (Cav1.2) channel inhibitor
 
F8257 Flunarizine dihydrochloride ≥98% (TLC) Blocks T-type Ca2+/Na+ channels; inhibits K+-induced catecholamine release from chromaffin cells
 
F100 Fluspirilene Dopamine receptor antagonist; antipsychotic; calcium channel blocker.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
H1512 Haloperidol powder Butyrophenone antipsychotic; D2, D3, and D4 dopamine receptor antagonist.
human ... ABCB1(5243), ADRA1A(148), ADRA2A(150), ADRA2C(152), CHRM1(1128), DRD2(1813), DRD3(1814), DRD4(1815), EBP(10682), HRH1(3269), HTR2A(3356), HTR2C(3358), HTR7(3363), KCNH1(3756), KCNH2(3757), PRNP(5621)
rat ... Adra1a(29412), Adra2a(25083), Chrm1(25229), Chrm2(81645), Drd1a(24316), Drd2(24318), Drd3(29238), Drd4(25432), Hrh1(24448), Htr1a(24473), Htr1b(25075), Htr2a(29595), Htr2c(25187), Oprs1(29336), Slc6a3(24898), Slc6a4(25553)
I1656   Idarubicin hydrochloride solid Topoisomerase II inhibitor
 
J3830 JNJ 10191584 maleate salt ≥98% (HPLC) JNJ 10191584 maleate is a highly selective histamine H4 receptor silent antagonist.
 
J4649 JNJ-10198409 ≥98% (HPLC), solid JNJ-10198409 is a potent ATP-competitive inhibitor of Platelet-Derived Growth Factor receptor tyrosine kinase (PDGF-RTK) with both antiangiogenic and a direct tumor cell antiproliferative activity. It is selective for PDGF-β kinase with IC50 values of 4.2 nM for PDGF-β and 45 nM for PDGF-α kinase.
 
J3205 JNJ-1661010 ≥98% (HPLC) JNJ-1661010 is a potent and selective fatty acid amide hydrolase (FAAH) inhibitor with >100-fold preferentially selective for FAAH-1 over FAAH-2. FAAH in an integral membrane enzyme within the amidase-signature family. It catalyzes the hydrolysis of several endogenous biologically active lipids and involves in a variety of physiological and pathological processes, including synaptic regulation, regulation of sleep and feeding, locomotor activity, pain and inflammation.
 
J3580 JNJ 17203212 ≥98% (HPLC) JNJ 17203212 is a reversible, competitive and potent TRPV1 antagonist that does not inhibit related TRP channels such as TRPV2, TRPV4, or TRPA1. Listed in BJP with IC50= 65 nM. TRPV1 channels are activated by heat, capsaicin and the endocannabinoid anandamide. Interest in TRPV1 antagonists in the transmission and modulation of pain.
 
J3770 JNJ7777120 ≥98% (HPLC) JNJ7777120 is a potent, selective non-imidazole H4 histamine receptor antagonist.
 
UC280 Ketoconazole Antifungal agent
human ... ABCB1(5243), CYP11B1(1584), CYP11B2(1585), CYP17A1(1586), CYP19A1(1588), CYP1A2(1544), CYP24A1(1591), CYP26A1(1592), CYP3A4(1576), CYP51A1(1595), KCNH1(3756)
mouse ... Abcb1a(18671), Abcb1b(18669)
rat ... Alox5(25290), Cyp17a1(25146), Cyp51(25427), Cyp7a1(25428)
L1167 Latanoprost ≥98% (HPLC), oil Latanoprost is a potent, selective prostaglandin FP receptor agonist.
 
L1292 Latanoprost acid ≥98% (HPLC) Potent, selective FP prostanoid receptor agonist, F-series prostaglandin analog. 200 times as potent as isopropyl ester form.
mouse ... Ptgfr(19220)
L3042 Levocabastine hydrochloride ≥99% (HPLC), solid Non-peptide histamine H1 receptor antagonist; neurotensin NTS2 receptor ligand.
 
L4762 Loperamide hydrochloride Loperamide hydrochloride (HCl) is a non-selective Ca2+ channel blocker. At nanomolar concentrations, it binds to μ-opioid receptors. Loperamide HCl does not cross the blood-brain barrier.
human ... OPRM1(4988)
SML0064   MBX-102 ≥98% (HPLC) MBX-102 has a potent transrepression effect on PPARγ. It is an oral glucose-reducing agent and also has insulin-sensitizing properties. It is useful as treatment for type 2 diabetes. MBX-102 also lowers triglycerides in a PPARα-independent manner.
MBX-102 is a selective PPAR modulator (SPPARM) and has been shown to inhibit phosphorylation of PPARγ. MBX-102 is converted to the active form, MBX-102 acid, in vivo.
 
M5824 MBX-102 acid ≥98% (HPLC), powder MBX-102 is a selective PPAR modulator (SPPARM) and has been shown to inhibit phosphorylation of PPARγ.
 
M2892 Methylphenidate hydrochloride CNS stimulant; releases catecholamines; potent inhibitor of dopamine reuptake
 
M4145 Minoxidil ≥99% (TLC) Activates ATP-activated K+ channels; vasodilator; slow or stop hair loss and promote hair regrowth.
human ... KCNJ1(3758)
M7920 Minoxidil sulfate salt    
O9387   Oxatomide ≥99% Oxatomide is an anti-allergy compound, H1 receptor antagonist. Oxatomide suppresses PAF-induced bronchoconstriction; inhibits leukotriene production.
human ... DRD3(1814)
O2881 Oxybutynin chloride ≥98% (TLC), powder Muscarinic acetylcholine receptor antagonist; inhibits proliferation of bladder smooth muscle cells, perhaps by downregulation of growth promoting genes.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
P0099 Paliperidone ≥98% (HPLC) Paliperidone is an atypical antipsychotic; active metabolite of risperidone.
 
P3371 Penfluridol ≥97% (HPLC), powder T-type Ca2+ channel blocker; antipsychotic
 
P6126 (R)-(−)-Phenylephrine hydrochloride powder α1-adrenoceptor agonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
P3246 Pipamperone dihydrochloride ~99% (HPLC), powder D2 dopamine receptor antagonist; 5-HT2 serotonin receptor antagonist; antipsychotic.
 
P6004 Prednisolone ≥99% Prednisolone is a glucocorticoid with anti-inflammatory and immunosuppressive activity.
human ... AR(367), ESR1(2099), NR3C1(2908), NR3C2(4306), PGR(5241), SERPINA6(866)
mouse ... Nr3c1(14815)
rat ... Ar(24208)
R3530   Rifabutin >98% (HPLC), powder Rifabutin is an antibiotic; antitumor. Rifabutin interferes with HSP-90 molecular chaperone, enhances ubiquitination and protein degradation, and inactivates bacterial RNA polymerase.
 
R3030 Risperidone ≥98% (HPLC), powder Risperidone is an antipsychotic; serotonin-dopamine antagonist.
 
T0575 Topiramate ≥98% (HPLC), solid Kainate GluR5 receptor antagonist; anticonvulsant.
Topiramate is a derivative of suphamate fructopyranose that inhibits the release of mesocorticolimbic dopamine. It facilitates GABA activity and inhibits glutamate function to alleviate the rewarding effects of alcohol. It modulates the trigeminovascular signaling that is effective in migraine prevention. Topiramate is structurally similar to fructose- 1,6-diphosphate and has the ability to inhibit the enzyme fructose 1,6-bisphosphatase, thereby preventing gluconeogenesis. It is found to inhibit the AMPA/kainate receptor-mediated signaling pathway in cultured neurons.
human ... CA1(759), CA2(760), CA4(762), CA5A(763), CA5B(11238), CA9(768)
mouse ... Car5a(12352)
rat ... Car2(54231), Car4(29242)
T9772 Triazolam Anxiolytic; ligand for the GABAA receptor benzodiazepine modulatory site.
human ... GABRA1(2554)