Compound 7P 10mg – 60 capsules

Compound 7P 10 mg — 60 oral research capsules. Compound 7P (also known by its development code 7P) is a novel positive allosteric modulator (PAM) of the high-affinity choline transporter ChT (SLC5A7) — the rate-limiting molecular machine that loads choline into cholinergic neurons for acetylcholine biosynthesis. As the only well-characterized small molecule that augments choline uptake at its source rather than acting downstream of acetylcholine release, Compound 7P represents an entirely distinct class from the AChE-inhibitor cognitive enhancers that have dominated cholinergic pharmacology for forty years. In rodent models, oral administration produces sustained, dose-dependent enhancement of central cholinergic tone with measurable improvements in attention, working memory and cognitive-flexibility paradigms.

Research Overview

Acetylcholine is the principal neurotransmitter of attention, working memory and the parasympathetic nervous system, and its synthesis in cholinergic neurons is rate-limited not by the enzyme choline acetyltransferase but by the upstream supply of free choline imported through the high-affinity choline transporter CHT1 (SLC5A7) [1]. CHT1 is a sodium-dependent secondary-active transporter expressed almost exclusively in cholinergic neurons, where its activity is dynamically regulated by neuronal activity itself — a feedforward mechanism that couples synaptic demand to substrate availability. Compound 7P is one of the first well-characterized positive allosteric modulators of CHT1: it does not act as a substrate but enhances the Vmax of choline uptake at physiological choline concentrations, producing a graded, activity-dependent increase in cholinergic tone [1,2]. This pharmacology is mechanistically distinct from acetylcholinesterase inhibitors (donepezil, rivastigmine), which act downstream by prolonging synaptic ACh, and from direct M1/α7-receptor agonists. In rodent attention and working-memory tasks, oral 7P produces dose-dependent improvements without the GI and cardiovascular side-effect profile of AChE inhibitors [2]. The compound has emerged as the leading research probe for upstream cholinergic-tone pharmacology.

Primary Research Areas

• CHT1 / SLC5A7 transporter pharmacology — the cleanest available small-molecule positive allosteric modulator of high-affinity choline uptake [1].
• Cognitive enhancement and attention research — produces dose-dependent improvements in 5-CSRTT, working-memory and cognitive-flexibility paradigms in rodent models [2].
• Acetylcholine homeostasis — research tool for studying activity-dependent coupling of cholinergic demand and choline-substrate supply [1,2].
• Translational cholinergic models — of interest in research on age-related cognitive decline, mild cognitive impairment and post-anaesthetic cognitive recovery, where central cholinergic tone is reduced [2].
• Differentiation from AChE inhibitors — useful comparator molecule in studies designed to dissect upstream (substrate supply) vs downstream (synaptic ACh persistence) cholinergic enhancement [1].

References

1. Sarter M, Parikh V. Choline transporters, cholinergic transmission and cognition. Nat Rev Neurosci. 2005;6(1):48–56.
2. Black SAG, Rylett RJ. Choline transporter CHT regulation and function in cholinergic neurons. Cent Nerv Syst Agents Med Chem. 2012;12(2):114–121.
3. Ennis EA, Blakely RD. Choline on the move: perspectives on the molecular physiology and pharmacology of the presynaptic choline transporter. Adv Pharmacol. 2016;76:175–213.