presynaptic

Clodronate disodium tetrahydrate (Clastoban) inhibits bone resorption and soft tissue calcification.

Bekanamycin (Kanamycin B) is an aminoglycoside antibiotic extracted from Streptomyces kanamyceticus, which inhibits a range of Gram-positive and Gram-negative bacteria.

6-Chloromelatonin is a potent melatonin receptor agonist, a 5-methoxyindole compound that competes for presynaptic melatonin receptor sites in the rabbit retina, inhibiting the calcium-dependent release of [3H]dopamine with higher metabolic stability than melatonin. Chloromelatonin competitively binds to [3H]melatonin at MT2 receptors (pKi=9.77) and may be used to study insomnia and sleep disorders associated with depression.

Atomoxetine hydrochloride (LY 139603) is the hydrochloride salt of atomoxetine, a phenoxy-3-propylamine derivative and selective non-stimulant, norepinephrine reuptake inhibitor with cognitive-enhancing activity. Although its precise mechanism of action is unknown, atomoxetine appears to selectively inhibit the pre-synaptic norepinephrine transporter, resulting in inhibition of the presynaptic reabsorption of norepinephrine and prolongation of norepinephrine activity in the synaptic cleft. The effect on cognitive brain function may result in improved attention and decreased impulsivity and activity levels.

Doxepin hydrochloride (Aponal) is a dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.

Yohimbine hydrochloride is a plant-derived alkaloid with alpha-2 adrenergic receptor blocking activity. By blocking presynaptic or postsynaptic alpha-2 adrenergic receptors, it promotes the release of norepinephrine and dopamine. It has been used in studies related to mydriasis and erectile dysfunction and is commonly used to induce hypertension models.

Dendrotoxin K, a Kv1.1 channel blocker, modulates glutamate release in CA3 neurons by regulating the presynaptic spike waveform in a time-dependent manner [1].

CGP 25454A is a novel and selective antagonist of the presynaptic dopamine autoreceptor (CGP 25454A).

MSOP is a selective antagonist of group III metabotropic glutamate receptor (KD of 51 μM for the L-AP4-sensitive presynaptic mGluR).

SM 21 is an analgesic with a presynaptic cholinergic mode of action.

Acetylethylcholine mustard hydrochloride is a choline acetyl-transferase inhibitor that decreases muscle contraction frequency by inhibiting the synthesis of acetyl-beta-methylcholine (Ach), with a half-maximal inhibitory concentration (IC50) of 1.22 mM. It serves as an irreversible ligand for the high-affinity choline transport system and functions as a specific presynaptic long-acting cholinergic toxin. Additionally, acetylethylcholine mustard hydrochloride is a precursor to the ethylcholine mustard aziridinium ion.

PD-147693 (compound II) is an active metabolite of the presynaptic dopamine autoreceptor agonist CI-1007, and it exhibits antipsychotic activity similar to CI-1007.

Metaphit methylsulfate is a specific PCP antagonist and an acylating agent for the [3H] phencyclidine binding site in rat brain homogenate. It inhibits PCP-induced motor activity through a presynaptic mechanism.

Atomoxetine (HSDB 7352) is a selective norepinephrine inhibitor that may cause an increase in blood pressure by increasing norepinephrine concentrations in peripheral sympathetic neurons .Atomoxetine is a highly selective antagonist of presynaptic norepinephrine transporters with little or no affinity for other norepinephrine receptors or other neurotransmitter transporters or receptors, but has little or no affinity for 5- hydroxytryptamine transporter. Atomoxetine selectively inhibits reuptake of norepinephrine and can be used to treat adolescents with ADHD and chronic tics.

Lumateperone (ITI 722) is a 5HT2A receptor antagonist and a dopamine receptor phosphoprotein modulator (DPPM).

ML352 is a selective and potent inhibitor of the presynaptic choline transporter (CHT), inhibits non-competitive choline uptake.

Aganodine is a guanidine that activates presynaptic imidazoline receptors. Aganodine inhibits the presynaptic release of norepinephrine through its agonism at imidazoline receptors.

Mezilamine is an antagonist of dopamine. It also blocks presynaptic but stimulating postsynaptic alpha-adrenoceptors.

WAY-100135 dihydrochloride is a potent and selective antagonist of both presynaptic and postsynaptic 5-HT 1A receptors, exhibiting an IC 50 value of 34 nM specifically at the rat hippocampal 5-HT 1A receptor. This compound displays promising antipsychotic effects.

α-Synuclein (61-75) is a peptide fragment derived from the larger protein α-Synuclein, which is predominantly found in presynaptic nerve terminals and considered a biomarker candidate for Parkinson's disease (PD).

Poloxamer 188 is a nonionic triblock copolymer surfactant and bioactive excipient used as a medical excipient to exacerbate cerebral amyloidosis, presynaptic dystrophy, and pathogenic microglial cell activation in 5XFAD mice.

3- Deoxyaconitine is a derivative of Aconitine (A189875), which activates tetrodotoxin-sensitive Na+ channels, inducing presynaptic depolarization, thus blocking the nerve action potential which, in turn, blocks the release of neurotransmitters and decreases the end plate potential at the neuromuscular junction.

Lamotrigine hydrate is an effective oral active anticonvulsant or antiepileptic agent that selectively blocks voltage-gated Na + channels, stabilizes presynaptic neuronal membranes and inhibits glutamate release. Lamotrigine hydrate can be used in epilepsy, focal seizure, et al [1] [2].

The alpha-adrenoceptors blocking effect of (N-piperidinomethyl)-2-chromanne was studied in vivo and in vitro in the rat. In the pithed rat, (N-piperidinomethyl)-2-chromanne (1 mg kg i.v.) antagonized the pressor effects induced by alpha agonists. (N-piperidinomethyl)-2-chromanne competitively antagonized the pressor effects of M7 (alpha 2-agonist) and cirazoline (alpha 1-agonist). (N-piperidinomethyl)-2-chromanne antagonized the inhibitory effects of clonidine on presynaptic alpha 2-receptors in stimulated pithed rats.