Alcoholism|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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Although alcoholism is common and impairing in elders, and is under-recognized and under-treated by the health care system, elderly alcoholics are at least as treatable as (and probably more than) younger alcoholics.30 Essentials of effective treatment include recognition and screening, involving the family, emphasizing that this is an inheritable medical illness, use of existing Alcoholics

Anonymous members, abstinence (controlled drinking is not recommended), group therapy, and “replacing drinking with people.” Many common problems of elders are worsened or often caused by alcoholism, a treatable but often overlooked medical condition.

Cat. No.	Product Name	CAS No.	Information
H9154	Tianeptine sodium salt	30123-17-2	Tianeptine sodium salt is a selective facilitator of 5-HT uptake. Tianeptine sodium salt has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50>10 μM) and has no effect on noradrenalin or dopamine uptake. Tianeptine sodium salt has antidepressant, anxiolytic, analgesic and neuroprotective activities.
H4953	CVT-10216	1005334-57-5	A potent, highly selective, reversible inhibitor of ALDH2 with IC50 of 29 nM, shows no significant inhibition for ALDH1 (IC50=1,300 nM); demonstrates therapeutic potential to reduce excessive drinking and to suppress relapse in abstinent alcoholics; also shows both anxiolytic and antidipsotropic properties in rats; selectively suppresses binge eating of palatable food and attenuates dopamine release in the accumbens of sugar-bingeing rats.
H4445	Org 25935	949588-40-3	A potent, selective glycine transporter 1 (GlyT1) inhibitor with IC50 of 100 nM; shows negligible action on GlyT2; produces a robust and dose-dependent decrease in EtOH consumption in rats, reduces compulsive relapse-like drinking without the development of tolerance.
H4374	Acamprosate calcium	77337-73-6	A GABA receptor agonist and modulator of glutamatergic systems; reduces alcohol consumption in animal models of alcohol addiction.
H3742	W-212393	610323-32-5	W-212393 (MT-7716 free base) is a highly potent, brain penetrant ORL1 receptor (NOP receptor) agonist with Ki of 0.76 and 0.50 nM for rat and human ORL1 receptors, respectively; displays a relative selectivity over μ receptor and serotonin transporter; significantly suppresses the activity of spontaneously firing rat suprachiasmatic nucleus neurons at 100 nM; induces a significant phase advance at circadian time 6 (CT6) and CT9, but not at other CTs, represents an interesting agent for the study of circadian rhythms; MT-7716 dose-dependently decreases GABAergic transmission and effectively blocks the ethanol-induced increase in GABA release at these synapses.
H3714	Naltrexone hydrochloride	16676-29-2	A potent, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively; also inhibits IL-6 and TNFα production in human immune cell subsets following stimulation with ligands for intracellular TLRs; a TLR-4 antognist that inhibits LPS-induced TLR4 downstream NO production in microglia BV-2 cells (IC50=105 uM).
H3713	Naltrexone	16590-41-3	A potent, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively; also inhibits IL-6 and TNFα production in human immune cell subsets following stimulation with ligands for intracellular TLRs; a TLR-4 antognist that inhibits LPS-induced TLR4 downstream NO production in microglia BV-2 cells (IC50=105 uM).
H3710	MT-7716	1215859-93-0	A highly potent, brain-penetrating ORL1 receptor (NOP receptor) agonist with Ki of 0.76 and 0.50 nM for rat and human ORL1 receptors, respectively; displays a relative selectivity over μ receptor and serotonin transporter; significantly suppresses the activity of spontaneously firing rat suprachiasmatic nucleus neurons at 100 nM; induces a significant phase advance at circadian time 6 (CT6) and CT9, but not at other CTs, represents an interesting agent for the study of circadian rhythms; MT-7716 dose-dependently decreases GABAergic transmission and effectively blocks the ethanol-induced increase in GABA release at these synapses.
H3670	Serlopitant	860642-69-9	Serlopitant (VPD-737, MK-0594) is a potent, selective substance P/neurokinin 1 (NK1) receptor for treating chronic pruritus.
H3332	PF-05190457	1334782-79-4	A potent, selective, and orally bioavailable ghrelin receptor (GHSR) inverse agonist with binding pKi of 8.36; displays excellent off-target activity in the CEREP panel at 10 uM with exception of serotonin 5-HT2B (IC50=3.7 uM); demonstrates robust increases in glucose-stimulated insulin secretion in human islets.

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