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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
152 Results for "
Peripheral effects
" in MedChemExpress (MCE) Product Catalog:
Products (152)
152 Results for "Peripheral effects" in MCE Product Catalog:
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1 Cited Publications
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α,β-Methylene-ATP trisodium is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP trisodium can trigger a reflex pressor response by activating P2X receptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP trisodium also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP trisodium can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system .
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1 Cited Publications
Cat. No.: HY-17034
CAS No.: 86347-14-0
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Medetomidine is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine has sedative and analgesic effects. Medetomidine can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels .
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Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels .
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1 Cited Publications
Cat. No.: HY-B1337S
CAS No.: 285979-70-6
Choline-d4 chloride is the d4-labeled Choline chloride (HY-B1337). Choline chloride is an orally active methylxanthine derivative. Choline chloride exhibits weak antihistaminic and anticholinergic activities and potentiates the effects of histamine and acetylcholine. Choline chloride relaxes bronchial smooth muscle, dilates coronary and peripheral blood vessels, increases urine output and electrolyte excretion, stimulates locomotor activity in the central nervous system, and induces transient hypotension following a pressor phase. Choline chloride modulates sleep architecture by increasing wakefulness time and reducing slow-wave sleep, without altering the frequency or severity of nocturnal hypoxemia, apnea, or hypopnea events. Choline chloride is used in studies of bronchospasm, nocturnal asthma, and chronic asthma .
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1 Cited Publications
Synonyms: SR57746A; SR57746 hydrochloride
Target:
5-HT Receptor Dopamine Receptor Trk Receptor PKC ERK Akt JNK
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Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
Cat. No.: HY-16723
CAS No.: 1259933-16-8
Synonyms: TV 45070; XEN402
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Funapide (TV 45070; XEN402) is an orally active inhibitor of voltage-gated sodium channels (VGSC) in the peripheral nervous system with IC50 values ??of 84 nM and 54 nM for Nav1.5 and Nav1.7, respectively. Funapide has analgesic effects .
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PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain .
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GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
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Cat. No.: HY-B1032
CAS No.: 17692-31-8
Synonyms: (±)-Dropropizine; UCB-196
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Dropropizine ((±)-Dropropizine; UCB-196) is an orally effective, peripherally selective antitussive that inhibits the activity of peripheral receptors and afferent nerves in the respiratory tract. Dropropizine acts on the cough reflex pathway, does not pass the blood-brain barrier, and has no central nervous system side effects. Dropropizine mainly regulates the level of sensory neuropeptides and inhibits the afferent signal transmission of the cough reflex, thereby alleviating the symptoms of dry cough, and has both mild local anesthetic and antihistamine activity. Dropropizine is mainly used for symptomatic research on dry cough caused by respiratory diseases .
Cat. No.: HY-P3445
CAS No.: 2269511-95-5
Synonyms: HSK21542
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Synonyms: BIA 5-1058
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Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively . Zamicastat reduces high blood pressure .
Cat. No.: HY-108229
CAS No.: 49625-89-0
Synonyms: 6β-Hydroxynaltrexone
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6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit .
Cat. No.: HY-17034BS1
CAS No.: 1216630-06-6
Synonyms: MPV785-13C,d3
Cat. No.: HY-W010448
CAS No.: 22884-10-2
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Cat. No.: HY-108229S
CAS No.: 1435727-11-9
Synonyms: 6β-Hydroxynaltrexone-d3
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LX2931 is an inhibitor of Sphingosine 1-Phosphate Lyase (S1PL). LX2931 works by increasing levels of S1P inside and outside the cell. The decrease in S1PL activity leads to a significant increase in S1P content in tissues, especially in lymphoid tissues which may lead to a restricted exodus of lymphocytes from secondary immune tissues, resulting in lymphocytopenic and immunosuppressive effects in the peripheral circulation. LX2931 can be used in research for the study of autoimmune diseases, especially rheumatoid arthritis .
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TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .
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Xylamidine is a peripheral 5-HT receptor antagonist used to investigate possible peripheral appetite suppressant effects of 5-hydroxytryptophan (5-HTP) and fenfluramine. In a 1-hour food intake test, xylamidine attenuated the decrease in food intake induced by 5-HT and 5-HTP, but had no effect on fenfluramine, suggesting that the appetite suppressant effect of 5-HTP is mediated in part through peripheral 5-HT receptors. Microstructural analysis revealed that 5-HTP and fenfluramine induced a decrease in food intake rate and a reduction in feeding batch size. Xylamidine reversed the effects of 5-HTP on food intake rate and induced a slight increase in feeding batch size itself, thus, the peripheral effect of 5-HTP appears to be to slow food intake rate. No effect of xylamidine on fenfluramine-induced changes in feeding was observed. The results suggest that the appetite suppressant effects of 5-HTP and fenfluramine are differentiated based on the peripheral effects of 5-HTP. The peripheral effects of 5-HTP are distinct from the previously reported 5-HT-induced decreases in feeding batch size and duration. Possible mechanisms underlying the differences in peripheral effects of 5-HT and 5-HTP are discussed.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
