selective peripheral

Isradipine (PN 200-110) is a dihydropyridine calcium channel blocker with antihypertensive and vasodilator activities. Isradipine blocks calcium entry through calcium ion channels in coronary and peripheral vascular smooth muscle, dilating coronary arteries and peripheral arterioles. This action increases oxygen delivery by enhancing blood flow and decreases oxygen requirements by reducing total peripheral resistance.

ZT 52656A hydrochloride belongs to synthetic small molecule compounds and is a highly selective kappa opioid receptor (KOR) agonist with good receptor selectivity and potential peripheral action characteristics. This compound effectively prevents or significantly alleviates ocular pain through KOR activation, and can be used in pain-related mechanism research.

Suzetrigine (VX-548) is a small molecule inhibitor and a highly selective inhibitor of the NaV1.8 target, with oral activity and good peripheral nerve selectivity. Suzetrigine is used for the treatment of moderate to severe acute pain following abdominoplasty or bunionectomy.

2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, exhibiting over 5-fold selectivity for MT1 compared to MT2. It can be used to identify, characterize, and localize melatonin binding sites in the brain and peripheral tissues.

ACY-1083 is a small molecule inhibitor, a highly selective HDAC6 inhibitor (IC50=3 nM), with 260-fold higher selectivity over other classes of HDAC isoforms. It is brain-penetrant and used for research on chemotherapy-induced peripheral neuropathy.

Deriglidole (SL 86-0715) is a peripheral adrenergic receptor antagonist that is a selective inhibitor of alpha2 receptors. Deriglidole inhibits colistin and Idazoxan but does not show activity against prazosin and rat cortical and human platelet α2-adrenergic receptors.

ZD-0892 is a selective and potent inhibitor of neutrophil elastase, targeting human neutrophil elastase and porcine pancreatic elastase with Kis of 6.7 nM and 200 nM, respectively.

Flunarizine dihydrochloride (R14950) is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. Flunarizine dihydrochloride (R14950) is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.

Prazosin hydrochloride (Vasoflex) reduces peripheral resistance and relaxes vascular smooth muscles as a selective adrenergic alpha-1 antagonist by a mechanism not completely known. Prazosin hydrochloride is a synthetic piperazine derivative with hypotensive antiadrenergic properties, It is used in the treatment of heart failure, hypertension, pheochromocytoma, Raynaud's syndrome, prostatic hypertrophy, and urinary retention.

Tolazoline (Benzalolin), a non-selective competitive α-adrenergic receptor antagonist, is used as a vasodilator to treat spasms of peripheral blood vessels. It has also been used successfully as an antidote to reverse the severe peripheral vasoconstriction as a result of overdose with certain 5-HT2A agonist drugs.

(±)-C3001a is the racemic mixture of C3001a (CAS: 2415154-29-7). C3001a is a selective activator of the TREK channel within the two-pore-domain potassium channel (K2P) family. C3001a specifically binds to a cryptic site formed by P1 and TM4 in TREK-1, thereby promoting the selective regulation of TREK-1 activity. C3001a targets TREK channels in the peripheral nervous system, reducing the excitability of pain-sensing neurons.

AM-1714 is a reasonable selective agonist for the peripheral cannabinoid receptor CB2. In animal studies, it has been shown to have analgesic and anti-abnormal pain effects.

M40 acetate is a potent, non-selective galanin receptor antagonist (Ki values are 1.82 and 5.1 nM at GAL1 and GAL2 respectively) that inhibits galanin (1-29) binding in rat brain in vitro (IC50 = 3 - 15 nM). Attenuates the antidepressant effects of fluoxetine and blocks galanin-induced food intake in vivo. Also exhibits weak partial agonist activity at peripheral GAL2 receptors at doses > 100 nM.

Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system. Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist.

Frakefamide, a potent analgesic, functions as a peripheral active μ-selective receptor agonist and cannot penetrate the blood-brain barrier to enter the central nervous system.

GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood

DSP-4 hydrochloride (Neurotoxin DSP 4 (hydrochloride)) (Neurotoxin DSP 4 hydrochloride) can be used for the temporary selective degradation of the central and peripheral noradrenergic neurons, mainly those from the locus coeruleus (LC). is a highly selective neurotoxin and readily passes the blood-brain barrier with neurotoxic effects on noradrenergic neurons of adult and developing rats,

AZD2906, a selective glucocorticoid receptor (GR) agonist, demonstrates inhibitory concentrations (IC50s) of 2.2 nM in human GR, 0.3 nM in rat peripheral blood mononuclear cells (PBMC), 41.6 nM in human whole blood, and 7.5 nM in rat whole blood, respectively[1]. Additionally, it induces an increase in micronucleated immature erythrocytes within rat bone marrow.

Biperiden Hydrochloride (KL 373 Hydrochloride) is an anticholinergic antiparkinsonian agent that selectively blocks central M1 cholinoreceptors while exerting atropine-like effects on peripheral parasympathetic structures. Biperiden Hydrochloride is approved for the adjunctive treatment of postencephalitic, idiopathic, and arteriosclerotic Parkinson’s disease, demonstrates minimal impairment of novelty preference compared with other anticholinergics in comparative cognitive studies, and is associated with known adverse effects including drowsiness, vertigo, headache, and dizziness.

CGP 36742 is a selective antagonist of the GABAB receptor that can penetrate the blood-brain barrier after peripheral administration (IC50: 32 μM). It is useful in the treatment of depression.

Otenzepad (AF-DX 116) is a selective M2 mAChR antagonist with IC50 values of 386 nM in rat heart and 640 nM in rabbit peripheral lung.

Tedalinab is an effective and selective cannabinoid receptor 2 agonist. Tedalinab demonstrates >4700-fold functional selectivity for CB2 over CB1 and is utilized in neuroimmune research focused on cannabinoid receptor signaling specificity, peripheral immune modulation pathways, and CB2-associated sensory neuron regulation in pain-related biological models.

Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine that functions as a selective, orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride effectively stimulating exocrine secretion from salivary glands and thereby serving as a clinically relevant sialogogue for the treatment of xerostomia, while its demonstrated ability to cross the blood–brain barrier supports its utility in central and peripheral cholinergic signaling studies and translational neuropharmacological investigations.

6β-Naltrexol is a selective peripheral opioid receptor antagonist that inhibits the morphine-induced slowing of gastrointestinal transit.