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Peptide cleaved from PAR₁ upon receptor activation

3553 | Parstatin (human)

Attenuates endothelial cell migration and proliferation (IC₅₀ ~ 3 μM), and induces cell cycle arrest. Promotes activation of caspase-3 and exhibits pro-apoptotic activity in vitro. Inhibits angiogenesis and exhibits cardioprotective activity in vivo.

Valproic acid derivative

2721 | ABS 205

Exhibits teratogenic and neuroprotective activity. Upregulates neural cell adhesion molecule (NCAM) expression, activates PPARδ (IC₅₀ = 0.6 mM) and increases Hoxa1 expression in rat embryos. Antiproliferative; induces G₁ cell cycle arrest in C6 glioma cells (IC₅₀ ~ 2 mM).

Orally active PDE4 inhibitor

3053 | Mesopram

Inhibits Th1 cell proliferation and decreases production of IFN-γ, TNF-α, IL-10 and iNOS in vitro. Triggers ovulation and exhibits efficacy against experimental autoimmune encephalomyelitis and murine colitis in vivo.

Potent CB₁ agonist

3500 | (±)-CP 47497

K_i = 2.2 nM. Display 3-28-fold > potency than Δ⁹-THC. Exhibits analgesic, motor depressant, anticonvulsant and hypothermic effects in vivo.

Potent and selective D₄ antagonist

3529 | PD 168568

K_i values are 8.8 and 1842 nM at D₄ and D₂ receptors respectively. Reverses amphetamine-stimulated locomotion in vivo and is orally active.

Potent N-type Ca²⁺ channel blocker

3552 | PD 173212

IC₅₀ = 36 nM. Displays selectivity over K⁺, Na⁺ and L-type Ca²⁺ channels. Prevents tonic seizures in the audiogenic seizure model in vivo.

Potent and selective GAL₂ agonist

3629 | M 1145

EC₅₀ = 38 nM, K_i values are 6.55, 497 and 587 nM at GAL₂, GAL₃ and GAL₁ respectively. Has an additive effect on the signal transduction of galanin.

NMDA receptor antagonist. Also NF-κB inhibitor

2861 | HU 211

IC₅₀ = 11 μM for inhibition of [³H]MK-801 binding to rat forebrain membranes. Protects against NMDA- and quisqualate-induced neurotoxicity (EC₅₀ = 3.8 μM) and enhances dopamine D₁ receptor activity. Inhibits NF-κB, reducing TNF-α, IL-6 and nitric oxide production, and acts as a free radical scavenger.

Group III mGlu agonist (mGlu₄ > mGlu₈ > mGlu₇)

3249 | Z-Cyclopentyl-AP4

Exhibits higher potency at mGlu₄ than mGlu₈ (EC₅₀ values are 49 and 124 μM respectively) with no activity at mGlu₇. Selectively inhibits synaptic activity in the lateral perforant pathway (IC₅₀ values are 130 and 1859 μM in the lateral and medial perforant pathways respectively).

Orally active atypical Na⁺ blocker; cardioprotective

3251 | KC 12291

Orally active atypical voltage-gated sodium channel blocker. Inhibits sustained sodium currents (I_NaL) and prevents diastolic contracture in isolated atria in vitro (IC₅₀ values are 9.6 and 0.55 - 0.79 μM respectively). Displays anti-ischemic, bradycardic and cardioprotective activity in vivo.

Neuromodulating neuropeptide fragment; inhibits food intake in vivo

3339 | CART (62-76) (rat, human)

Cocaine- and amphetamine-regulated transcript (CART) peptide fragment that inhibits food intake. Attenuates NPY-induced feeding and decreases food intake in food-restricted goldfish, and induces anxiogenic-like effects in elevated plus-maze test in rats.

Highly selective D₃ antagonist

3355 | PNU 177864

Highly selective dopamine D₃ receptor antagonist. Induces phospholipidosis and exhibits antischizophrenic activity in vivo.

Orally active, selective 5-HT₆ antagonist

3368 | SB 271046

pK_i values are 9.02-8.92, 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT₆, 5-HT_1D, 5-HT_1A, D₃, 5-HT_1B, 5-HT_1F, α_1B, 5-HT_2C, 5-HT_2A, D₂, 5-HT_2B, 5-HT₇, 5-HT₄ and 5-HT_1E respectively. Increases extracellular glutamate and aspartate in the frontal cortex, and exhibits anticonvulsant activity (EC₅₀ = 0.16 μM).

Potent, orally active DPP-IV inhibitor

3506 | NVP DPP 728

K_i = 11 nM, IC₅₀ = 14 nM. Displays > 15 000-fold selectivity over DPP-II and a range of proline-cleaving proteases. Exhibits antidiabetic activity in vivo; improves glucose tolerance, increases glucagon-like peptide 1 (GLP-1) and insulin levels, augments insulin secretion and GLUT-2 levels, and reduces (preserves) islet size.

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