sedation

Guanfacine hydrochloride (Intuniv) is a centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS.

Dexmedetomidine is a Central alpha-2 Adrenergic Agonist. The mechanism of action of dexmedetomidine is as an Adrenergic alpha2-Agonist. The physiologic effect of dexmedetomidine is by means of General Anesthesia.

Dexmedetomidine hydrochloride (Precedex) is a potent, selective, orally active α2-adrenoceptor agonist with a Ki value of 1.08 nM. It shows 1620-fold selectivity over α1-adrenoceptors. Dexmedetomidine hydrochloride (Precedex) can protect against sepsis-induced acute lung injury through anti-inflammatory, anti-oxidative, and anti-apoptotic effects.

Medetomidine hydrochloride (MPV785) is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.

Blonanserin (AD-5423) is an atypical antipsychotic approved in Japan in January, 2008. Relative to many other antipsychotics, blonanserin has an improved tolerability profile, lacking side effects such as extrapyramidal symptoms, excessive sedation, or hypotension.

Flumazenil (Ro 15-1788) antagonizes the benzodiazepine binding site of the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex in the central nervous system (CNS), thereby preventing the chloride channel opening events and inhibiting neuronal hyperpolarization. As a result, flumazenil reverses benzodiazepine-induced effects including sedation, psychomotor deficits, amnesia, and hypoventilation in a dose-dependent manner. Flumazenil is an imidazobenzodiazepine derivative, effective in reversing benzodiazepine-induced activities.

Fexofenadine (Carboxyterfenadine), an antihistamine pharmaceutical drug, is used to treat allergy symptoms, such as nasal congestion, hay fever, and urticaria. Compared to first-generation antihistamines, Fexofenadine is less able to pass the blood-brain barrier and cause sedation.

Ebastine (Kestine) (trade names Evastin, Kestine, Ebastel, Aleva) is a non-sedating H1 antihistamine. It does not penetrate the blood-brain barrier and thus allows an effective block of the H1 receptor in peripheral tissue without a central side effect, i. e not causing sedation or drowsiness.

L-Theanine is a relaxing and nondietary amino acid found pretty much exclusively in teas from Camellia sinensis and is known to promote relaxation without sedation.

Org GC 94 is a psychoactive small-molecule compound belonging to the tetracyclic antidepressant (TeCA) therapeutic family, extensively characterized as a noradrenergic and specific serotonergic antidepressant (NaSSA) with clinically documented antidepressant, anxiolytic, hypnotic, antiemetic, orexigenic, and antihistamine pharmacological effects. Org GC 94 mechanistically acting as an antagonist or inverse agonist at H1, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT6, 5-HT7, α1-adrenergic, and α2-adrenergic receptors, inhibiting norepinephrine reuptake, exhibiting high-affinity H1 inverse agonism associated with sedation and weight gain, showing negligible affinity for muscarinic acetylcholine receptors and thus lacking anticholinergic effects.

Triflupromazine is a dopamine receptor D1/D2 antagonist and LHDA inhibitor that suppresses dopamine activity in the central nervous system (CNS) and promotes LDHA-mediated AMBRA1 ubiquitination, used for treating mental disorders, sedation, and antiemesis.

Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the GABAA receptor. Imidazoleacetic acid is generated through histamine oxidation in the mouse brain and exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces centrally mediated responses including analgesia, sedation, hypnosis, and reductions in blood pressure, body temperature, isolation-induced aggression, and motor activity. Imidazoleacetic acid is valuable for neuropharmacology and neurotransmitter signaling investigations involving histaminergic and GABAergic pathways.

MK-0343, also known as MRK-409, is a GABAA receptor subtype-selective partial agonist that exhibits non-sedating anxiolytic activity in preclinical species but induces sedation in humans, binding with high affinity to α1-, α2-, α3-, and α5-containing human recombinant GABA(A) receptors while demonstrating greater agonist efficacy at α3 relative to α1 subtypes, thereby providing mechanistic insight into subtype-specific modulation of inhibitory neurotransmission.

Tilozepine is a derivative of thienobenzodiazepine, exhibiting pharmacological activities including hypnosis, sedation, antipsychotic effects, and muscle relaxation.

Primaperone is a substituted aminoketone compound used for blood pressure reduction and sedation.

DBPR116 is a prodrug of BPRMU191 that can penetrate the blood-brain barrier. It significantly enhances the delivery efficiency of drugs targeting the central nervous system. When combined with the antagonist Naltrexone, DBPR116 demonstrates superior safety and analgesic effects compared to morphine in various in vivo pharmacological studies, including thermal pain models, cancer pain models, constipation, sedation, psychological dependence, heart rate, and respiratory frequency. As a strategy for peripheral administration, DBPR116 effectively alleviates pain while reducing adverse effects, showing promise as a safer opioid analgesic.

Nitrazolam is a benzodiazepine compound that may exhibit central nervous system depressant properties similar to traditional benzodiazepine drugs by acting on the GABA receptors (GABA receptor). These effects include sedation, hypnosis, anxiolytic, and anticonvulsant activities.

RP-60503 is an orally active anxiolytic cyclopyrrolone derivative with a low potential for sedation. It binds to the γ-aminobutyric acid A (GABA)/benzodiazepine receptor, exhibiting a Ki value of 1.16 nM. RP-60503 is applicable in research related to neurological disorders.

Propiomazine maleate is an orally active antihistamine. It acts as a potent stimulant for prolactin (PRL) release through antagonism of the dopaminergic system and inhibits luteinizing hormone (LH) secretion. Propiomazine maleate is primarily utilized as an adjunct in anesthesia, in the management of psychiatric disorders and anxiety sedation, and is also used in research related to insomnia.

PF 0713, a GABAA receptor agonist, is used as an intravenous sedative-hypnotic for general anaesthesia, ICU sedation, procedural sedation, chemotherapy.

Triclofos Sodium is used to treat insomnia and used for sedation.

ZK-91296 is a GABA receptor agonist. ZK 91296 can reduce anxiety in animals at doses well below those causing sedation. ZK 91296 may possess pharmacological selectivity for a particular type of BZ receptor interaction, perhaps including topographic as wel

Helianorphin-19 is a high affinity, potent and selective κ-opioid receptor (KOR) agonist (Ki = 25 nM; EC50= 45 nM). Helianorphin-19 exhibits approximately 200-fold selectivity for KOR over μ and δ-opioid receptors.In vivoHelianorphin-19 shows potent peripheral analgesic efficacy in a mouse model of visceral pain without affecting motor coordination/sedation.

Triclofos is a potent, orally active sedative that is rapidly hydrolyzed in vivo into trichloroethanol (TCEOH) and monosodium phosphate, facilitating its sedative effects [1].