sedation

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

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.

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.

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.

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.

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.

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.

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

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.

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

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

Mesuaxanthone A and mesuaxanthone B are two yellow pigments.They produce varying degrees of C.N.S. depression characterised by ptosis, sedation, decreased spontaneous motor activity, loss of muscle tone, potentiation of pentobarbitone sleeping time and et

Romifidine hydrochloride, an α2 adrenergic receptor agonist, induces sedation effects in vivo.

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.

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

Blonanserin-d5 is a deuterated compound of Blonanserin. Blonanserin has a CAS number of 132810-10-7. Blonanserin 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.

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.

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

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

Tiapride is an atypical neuroleptic agent without propensity for causing catalepsy and sedation. Tiapride is a selective antagonist of dopamine D2-receptor with IC 50 values of 1440, 45.8, >100, and 11.7 μM for D1; D2; D3; D4, respectively [1].

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.