|
T0957 |
Isradipine
|
PN 200-110 |
Calcium Channel
,
Autophagy
|
|
Isradipine (PN 200-110) is a dihydropyridine calcium channel blockers with antihypertensive and vasodilator activities. Isradipine blocks the calcium entry through the calcium ion channels of coronary and peripheral vasc... |
|
T3173 |
DAA-1106
|
DAA1106 |
Others
,
GABA Receptor
|
|
DAA-1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), acting as a potent and selective agonist at the peripheral benzodiazepine receptor. |
|
T21447 |
Tolazoline
|
Priscol,Priscoline,Pridazole,Divascol,Vasimid,Benzalolin |
Adrenergic Receptor
|
|
Tolazoline (Benzalolin), a non-selective competitive α-adrenergic receptor antagonist, is used as a vasodilator to treat spasms of peripheral blood vessels. It has also been used successfully as an antidote to reverse th... |
|
T16411 |
Otenzepad
|
AF-DX 116 |
AChR
|
|
Otenzepad (AF-DX 116) is a selective antagonist of M2 mAChR with IC50s of 386 nM and 640 nM for rat heart and rabbit peripheral lung. |
|
T10244 |
ACY-1083
|
|
HDAC
|
|
ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor (IC50: 3 nM) and effectively reverses chemotherapy-induced peripheral neuropathy. |
|
T0806 |
Flunarizine dihydrochloride
|
Flunarizine 2HCl,KW-3149,R14950 |
Calcium Channel
,
Dopamine Receptor
,
Sodium Channel
|
|
Flunarizine dihydrochloride (R14950) is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. Flunarizine dihydrochloride (R14950) is effective in the prophylaxis of mig... |
|
T5385 |
Radiprodil
|
RGH-896 |
NMDAR
,
iGluR
|
|
Radiprodil (RGH-896) (RGH-896) is an orally active and selective NMDA NR2B receptors antagonist. It was a potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPNP). |
|
T2371 |
Emapunil
|
AC-5216,XBD-173 |
Others
|
|
Emapunil (XBD-173) is an anxiolytic drug which acts as a selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO. |
|
T10998 |
Deriglidole
|
SL 86-0715 |
Adrenergic Receptor
|
|
Deriglidole (SL 86-0715) is a peripheral adrenergic receptor antagonist that is a selective inhibitor of alpha2 receptors. Deriglidole inhibits colistin and Idazoxan but does not show activity against prazosin and rat co... |
|
T10073 |
2-Iodomelatonin
|
|
Melatonin Receptor
|
|
2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 over MT2. 2-iodomelatonin can be used to identify, characterize and localize melatonin bind... |
|
TP1918L |
Lys-[Des-Arg9]Bradykinin,TFA
|
Lys-[Des-Arg9]Bradykinin,TFA 71800-36-7(fb-tfa) |
Bradykinin Receptor
|
|
Lys-[Des-Arg9]Bradykinin,TFA is Endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripher... |
|
TP1918L1 |
Lys-[Des-Arg9]Bradykinin acetate
|
Lys-[Des-Arg9]Bradykinin acetate (71800-36-7 free base) |
Bradykinin Receptor
|
|
Lys-[Des-Arg9]Bradykinin acetate is an endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces p... |
|
T13664 |
DSP-4 hydrochloride
|
Neurotoxin DSP 4 (hydrochloride) |
Others
|
|
DSP-4 hydrochloride (Neurotoxin DSP 4 (hydrochloride)) (Neurotoxin DSP 4 hydrochloride) can be used for the temporary selective degradation of the central and peripheral noradrenergic neurons, mainly those from the locus... |
|
T2525 |
Alosetron hydrochloride
|
Lotronex,GR 68755C,GR 68755,GR 68755X |
5-HT Receptor
|
|
Alosetron hydrochloride (GR 68755) is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist. Alosetron blocks the actions of serotonin at 5-HT3 sites in the peripheral nervous system,... |
|
T1050 |
Prazosin hydrochloride
|
Prazosin hydrochloride,Prazosin HCl,cp-12299-1,Peripress,Vasoflex,Minipress |
Potassium Channel
,
MRP
,
Adrenergic Receptor
,
ABC
,
Autophagy
|
|
Prazosin hydrochloride (Vasoflex) reduces peripheral resistance and relaxes vascular smooth muscles as a selective adrenergic alpha-1 antagonist by a mechanism not completely known. Prazosin hydrochloride is a synthetic ... |
|
TP1992L |
M40 acetate(143896-17-7 free base)
|
|
Neuropeptide Y Receptor
|
|
M40 acetate is a potent, non-selective galanin receptor antagonist (Ki values are 1.82 and 5.1 nM at GAL1 and GAL2 respectively) that inhibits galanin (1-29) binding in rat brain in vitro (IC50 = 3 - 15 nM). Attenuates ... |
|
T21392 |
Flunarizine
|
Flunarizinum,Flunarizin,Sibelium,Flunarizina,R-14950 |
|
|
Flunarizine is a non-selective calcium entry blocker and a histamine H1 receptor blocker. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, a... |
|
T14938 |
CGP 36742
|
SGS-742 |
GABA Receptor
|
|
CGP 36742 is a selective antagonist of the GABAB receptor that can penetrate the blood-brain barrier after peripheral administration (IC50: 32 μM). It is useful in the treatment of depression. |
|
T25102 |
Aprikalim
|
RP52891,RP-52891,RP 52891 |
|
|
Aprikalim is a specific and selective ATP-sensitive K+ (KATP) channel opener. Aprikalim affords cardioprotection and at higher doses also cause peripheral or coronary vasodilatation. |
|
T28335 |
PD 140376
|
PD-140376,PD140376 |
|
|
PD 140376 is a highly selective antagonist radioligand for the cholecystokinin(B)-gastrin receptor in guinea pig gastric mucosa & cerebral cortex in the peripheral and central nervous systems. |
|
T11323L |
Frakefamide
|
|
Others
|
|
Frakefamide is a potent analgesic that functions as a peripheral active μ-selective receptor agonist. It cannot penetrate the blood-brain barrier to enter the central nervous system. |
|
T11482 |
GSK2245035
|
|
Others
|
|
GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine p... |
|
T29933 |
AM-1714
|
UNII-E3OY6PCU04,AM1714 |
|
|
AM-1714 is a reasonable selective agonist for the peripheral cannabinoid receptor CB2. In animal studies, it has been shown to have analgesic and anti-abnormal pain effects. |
|
T27324 |
FK614
|
FK 614,ATx-08-001,ATx-08001,FK-614 |
|
|
FK-614 is a selective agonist of peroxisome proliferator-activated receptor gamma. FK-614 improves peripheral glucose utilization while decreases hepatic insulin extraction in alloxan-induced diabetic dogs. |
|
T14570 |
BI 99179
|
BI99179 |
Fatty Acid Synthase
|
|
|
|
T33583 |
Naldemedine
|
S-297995,S297995,Naldemedine,S 297995,S297,995,S 297,995,S297,995;Naldemedine,S-297,995 |
|
|
Naldemedine (S 297995) is a peripheral selective μ-opioid receptor antagonist being developed by Shionogi for the treatment of opioid-induced adverse reactions, including constipation, nausea, and vomiting. They are usua... |
|
TQ0002L |
A-317491 sodium
|
A-317491,A 317491,A317491 |
|
|
A-317491 is an effective selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, which reverses inflammatory mechanical hyperalgesia and relieves chronic inflammation and neuropathic pain in rats by acting on p... |
|
T28850 |
SR57227A
|
SR 57227A,SR-57227A |
|
|
SR 57227A is a highly selective of peripheral and central 5-HT3 receptors and an inhibitor of NMDA receptor-mediated responses in rat cortical pyramidal cells. It exhibits anti-depressant like effects in rats and decreas... |
|
T11323 |
Frakefamide TFA (188196-22-7 free base)
|
Frakefamide TFA |
Others
|
|
Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system. Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. |
|
T79303 |
IACS-52825
|
|
|
|
IACS-52825 is a potent, selective DLK inhibitor, exhibiting a dissociation constant (Kd) of 1.3 nM, and is valuable for researching chemotherapy-induced peripheral neuropathy (CIPN) [1]. |
|
T14374 |
AZD2906
|
|
|
|
AZD2906, a selective glucocorticoid receptor (GR) agonist, demonstrates inhibitory concentrations (IC50s) of 2.2 nM in human GR, 0.3 nM in rat peripheral blood mononuclear cells (PBMC), 41.6 nM in human whole blood, and ... |
|
TP1918 |
Lys-[Des-Arg9]Bradykinin
|
|
|
|
Endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. ... |
|
T73655 |
Frakefamide TFA
|
|
|
|
Frakefamide TFA is a potent analgesic functioning as a μ-selective receptor agonist with peripheral activity. Notably, Frakefamide cannot cross the blood-brain barrier to enter the central nervous system [1] [2]. |
|
T41183 |
Helianorphin-19
|
|
|
|
Helianorphin-19 is a high affinity, potent and selective κ-opioid receptor (KOR) agonist (Ki = 25 nM; EC50= 45 nM). Helianorphin-19 exhibits approximately 200-fold selectivity for KOR over μ and δ-opioid receptors.In viv... |
|
TP1992 |
M40
|
|
|
|
Potent, non-selective galanin receptor antagonist (Ki values are 1.82 and 5.1 nM at GAL1 and GAL2 respectively) that inhibits galanin (1-29) binding in rat brain in vitro (IC50 = 3 - 15 nM). Attenuates the antidepressant... |
|
T36109 |
L Moses dihydrochloride
|
|
|
|
High affinity and selective cell-permeable p300/CBP-associated factor (PCAF) inhibitor (Ki = 47 nM). Exhibits no significant activity against a panel of 48 other bromodomains except GCN5 (Kd = 600 nM). Exhibits >4500-fo... |
|
T21411 |
Isoproterenol
|
Norisodrine,Isoprenaline,Novodrin,Isuprel,Medihaler-Iso |
Endogenous Metabolite
,
Adrenergic Receptor
|
|
Isoproterenol (Norisodrine) is a non-selective and orally active β-adrenoceptor agonist.Isoproterenol is a potent peripheral vasodilator and bronchodilator.Isoproterenol can be used in the study of bradycardia and bronch... |
|
T61850 |
Adenosine receptor inhibitor 1
|
|
|
|
Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR). It exhibits exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >100... |
|
T73522 |
CR 665
|
FE 200665,JNJ 38488502 ; FE 200665,JNJ 38488502 |
|
|
CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist, capable of activating the kappa opioid receptor with an EC50 value of 10.9 nM. It is utilized in the research of peripheral pain. |
|
T79195 |
Cav 3.2 inhibitor 4
|
|
Calcium Channel
|
|
Cav 3.2 Inhibitor 4 (Compound 21) is a selective and potent inhibitor of the T-type calcium channel (Ca v 3.2), demonstrating peripheral restriction with an IC50 value of 0.6 μM. It is utilized in atrial fibrillation res... |
|
T82515 |
E104
|
|
|
|
E104 (compound 1), a selective TLR7 agonist, exhibits potent anticancer activity when delivered via antibody-drug conjugate (ADC) technology. It effectively activates mouse macrophages and human peripheral blood mononucl... |
|
T62541 |
AChE-IN-22
|
|
|
|
AChE-IN-22 (compound 10q) is a selective inhibitor of acetylcholinesterase (AChE) that acts on both AChE (IC50: 0.88 μM) and BuChE (IC50: 10 μM). AChE-IN-22 binds to both the CAS (catalytic active site) and PAS (peripher... |
|
T62732 |
S1P1 agonist 5
|
|
|
|
S1P1 agonist 5 is a selective, orally active S1P1 agonist. S1P1 agonist 5 inhibits the drainage of lymphocytes from lymphoid tissue into peripheral blood. S1P1 agonist 5 has potential for studies in multiple sclerosis (M... |
|
T63173 |
BTK-IN-8
|
|
|
|
BTK-IN-8 is a potent, selective, peripheral covalent BTK inhibitor with an IC50 value of 0.22 nM and a Kd value of 0.91 nM. BTK-IN-8 exhibits good potency in whole blood CD69 cells with an IC50 value of 0.029 μM. |
|
T40572 |
Lesogaberan napadisylate
|
AZD-3355 napadisylate |
|
|
Lesogaberan (AZD-3355) napadisylate is a potent and selective agonist of GABA B receptors, with an EC 50 of 8.6 nM for human recombinant GABA B receptors. It demonstrates an affinity (Ki) of 5.1 nM for rat GABA B recepto... |
|
T63287 |
HPK1-IN-3
|
|
|
|
HPK1-IN-3 is a selective, potent, ATP-competitive inhibitor of hematopoietic progenitor cell kinase 1 (HPK1; MAP4K1) (IC50: 0.25 nM). HPK1-IN-3 has IL-2 cellular potency and is able to act on human peripheral blood monon... |
|
T71955 |
C3001a
|
|
|
|
C3001a is a selective activator for TREK, against other two-pore domain K+(K2P) channels. C3001a binds to the cryptic binding site formed by P1 and TM4 in TREK-1. C3001a targets TREK channels in the peripheral nervous sy... |
|
T37523 |
Tenofovir diphosphate (sodium salt)
|
|
|
|
Tenofovir diphosphate is an inhibitor of HIV reverse transcriptase (Kis = 0.022 and 1.55 μM for RNA and DNA, respectively) and hepatitis B virus (HBV) polymerase (Ki = 0.18 μM). It is selective for these enzymes over DNA... |
|
T69081 |
KRH-1636
|
|
|
|
KRH-1636 is an orally active, selective and extremely potent CXC chemokine receptor 4 antagonist. KRH-1636 exhibits a potent and selective anti-HIV-1 activity. KRH-1636 efficiently blocked replication of various T cell ... |
|
T37273 |
BLX3887
|
|
|
|
BLX3887 is an inhibitor of 15-lipoxygenase type 1 (15-LO-1; IC50 = 32 nM in a cell-free enzyme assay).1 It is selective for 15-LO-1 over 15-LO-2, which it does not inhibit, 5-LO (IC50 = 472 nM), and 12-LO (IC50 = 3,310 n... |
