Piperazines

Eteplirsen (brand name Exondys 51) is a medication to treat, but not cure, some types of Duchenne muscular dystrophy (DMD), caused by a specific mutation. Eteplirsen only targets specific mutations and can be used to treat about 14% of DMD cases. Eteplirsen is a form of antisense therapy.

Piperacetazine (Quide) is an antipsychotic prodrug, most notably used for schizophrenia. It is a phenothiazine derivative. Based on clinical trial data, it appears to have similar efficacy as chlorpromazine. However, very little research has been done since the 1970s, and it is not a commonly used drug today.

Zosuquidar (development code LY-335979) is an experimental antineoplastic drug. Zosquidir inhibits P-glycoproteins. Other drugs with this mechanism include tariquidar and laniquidar. P-glycoproteins are trans-membrane proteins that pump foreign substances out of cells in an ATP dependent fashion. Cancers overexpressing P-glycoproteins are able to pump out therapeutic molecules before they are able to reach their target, effectively making the cancer multi-drug resistant. Zosuquidar inhibits P-glycoproteins, inhibiting the efflux pump and restoring sensitivity to chemotherapeutic agents.

Picloxydine (trade name Vitabact) is a bisbiguanide antiseptic used in eye drops. It is structurally similar to chlorhexidine.

PIPES ('piperazine-N,N-bis(2-ethanesulfonic acid)') is a frequently used buffering agent in biochemistry. It is an ethanesulfonic acid buffer developed by Good et al. in the 1960s.

thumb|261px|right|class=skin-invert-image|Lodenafil carbonate

Mirodenafil is a PDE5 inhibitor used to treat erectile dysfunction. Developed by SK Chemicals Life Science, mirodenafil is marketed in Korea under the brand name Mvix, offered both as tablets (50 mg and 100 mg) and as orally dissolving films (50 mg).

chemical compound

Cinepazide or cinepazide maleate (Kelinao or Anjieli in China) is a vasodilator used in China for the treatment of cardiovascular and cerebrovascular diseases, and peripheral vascular diseases. It appears to work by potentiating A2 adenosine receptors.

Amdiglurax (), also known by its former developmental code names ALTO-100 and NSI-189 (short for "NeuralStem Inc. 189"), is a drug described as a hippocampal neurogenesis stimulant and indirect brain-derived neurotrophic factor (BDNF) modulator which is under development for the treatment of major depressive disorder (MDD), bipolar depression, and post-traumatic stress disorder (PTSD). There has also been interest in amdiglurax for possible treatment of cognitive impairment and neurodegeneration. It is taken by mouth.

Ensaculin (KA-672) is a drug from the coumarin family, which has been researched as a potential treatment for dementia. It acts on a number of receptor systems, being both a weak NMDA antagonist and a 5HT1A agonist. Animal studies have shown promising nootropic effects, although efficacy in humans has yet to be proven. It was well tolerated in human trials, with the main side effect being orthostatic hypotension (low blood pressure upon standing).

Azaprocin is a drug which is an opioid analgesic with approximately ten times the potency of morphine, and a fast onset and short duration of action. It was discovered in 1963, but has never been marketed.

Naftopidil (INN, marketed under the brand name Flivas) is a drug used in benign prostatic hyperplasia which acts as a selective α1-adrenergic receptor antagonist or alpha-1 blocker.

Zicronapine ( , previously known as Lu 31-130) is an atypical antipsychotic medication formerly under development by H. Lundbeck A/S. In phase II studies zicronapine showed statistically significant separation from placebo and convincing efficacy and safety data when compared to olanzapine.

JZL195 is a potent inhibitor of both fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL), the primary enzymes responsible for degrading the endocannabinoids anandamide (AEA) and 2-arachidonoylglycerol (2-AG), respectively.

Eprazinone (trade names Eftapan, Isilung, Mucitux) is a mucolytic and bronchospasm relieving drug. It has been marketed in many European countries, but not in the US or United Kingdom.

Midafotel (CPPene; SDZ EAA 494) is a potent, competitive antagonist at the NMDA receptor. It was originally designed as a potential therapy for excitotoxicity, epilepsy or neuropathic pain. It looked very promising in in vitro trials proving to be a potent competitive antagonist at the NMDA without affecting other receptors. Research continued through to in vivo cat studies where it proved to limit damage after occluding the middle cerebral artery, leading to ischaemia. It also blocked photosensitive epilepsies in baboons.

Casopitant (), former tentative trade names Rezonic (U.S.) and Zunrisa (Europe), is an NK1 receptor antagonist which was undergoing research for the treatment of chemotherapy-induced nausea and vomiting. It was under development by GlaxoSmithKline. In July 2008, the company filed a marketing authorisation application with the European Medicines Agency. The application was withdrawn and development was discontinued in September 2009 because GlaxoSmithKline decided that further safety assessment was necessary. However, a 2022 review listed casopitant as under development as a potential novel ant

(+)-BW373U86 is an opioid analgesic drug used in scientific research.

Avitriptan (; development code BMS-180048) is an antimigraine drug of the triptan family which was never marketed. It acts as a serotonin 5-HT1B and 5-HT1D receptor agonist. The drug reached phase 3 clinical trials prior to the discontinuation of its development.

Adatanserin (WY-50,324, SEB-324) is a mixed 5-HT1A receptor partial agonist and 5-HT2A and 5-HT2C receptor antagonist. It was under development by Wyeth as an antidepressant but was ultimately not pursued.

LP-211 is a drug which acts as a potent and selective agonist at the 5HT7 serotonin receptor, with better brain penetration than older 5-HT7 agonists in the same series, and similar effects in animals.

Lidoflazine is a piperazine calcium channel blocker. It is a coronary vasodilator with some antiarrhythmic action. Lidoflazine was discovered at Janssen Pharmaceutica in 1964. In 2025 Lidoflazine has also been reported to interact with tubulin and inhibit its polymerization.

Hexocyclium is an antimuscarinic. It is used in the form of its methyl sulfate, called hexocyclium metilsulfate.

GR-89696 is a drug which acts as a highly selective κ-opioid agonist. It has been studied in various animal species, and has been described as selective for the κ2 subtype. Recent studies have suggested that GR-89696 and related κ2-selective agonists may be useful for preventing the itching which is a common side effect of conventional opioid analgesic drugs, without the additional side effects of non-selective kappa agonists. The structure bound to the κ-opioid receptor has been reported.

explosive chemical compound

Pramiconazole is a triazole antifungal which was under development by Barrier Therapeutics for the treatment of acute skin and mucosal fungal infections but was never marketed.

PB-28 is an agonist of the sigma-2 receptor.

MT-45 (IC-6) is an opioid analgesic drug invented in the 1970s by Dainippon Pharmaceutical Co. It is chemically a 1-substituted-4-(1,2-diphenylethyl) piperazine derivative, which is structurally unrelated to most other opioid drugs. Racemic MT-45 has around 80% the potency of morphine, with almost all opioid activity residing in the (S) enantiomer (the opposite stereochemistry from the related drug lefetamine). It has been used as a lead compound from which a large family of potent opioid drugs have been developed, including full agonists, partial agonists, and antagonists at the three main op

Lesopitron (E-4424) is a selective full agonist of the 5-HT1A receptor which is structurally related to the azapirones. In 2001 it was under development by Esteve as an anxiolytic for the treatment of generalized anxiety disorder (GAD). It made it to phase II clinical trials but was apparently discontinued as no new information on lesopitron has surfaced since.

Fenoverine (INN) is an antispasmodic [also known as spasmolytics] drug, which acts by inhibiting calcium channels [much in the same way as traditional calcium channel blockers, which are used as antianginal drugs]. In the case of Fenoverine, the relaxation occurs in abdominal / intestinal smooth muscles, while in case of antianginal drugs, the relaxation occurs in coronary vessels. Notably Fenoverine does not act as an antianginal agent. ==Toxicity== Fenoverine is known to cause rhabdomyolysis. ==References==

Atiprosin (developmental code name AY-28,228) is an antihypertensive agent which acts as a selective α1-adrenergic receptor antagonist. It also possesses some antihistamine activity, though it is some 15-fold weaker in this regard than as an alpha blocker. It was never marketed.

AD-1211 is an opioid analgesic drug invented in the 1970s by Dainippon Pharmaceutical Co. It is chemically a 1-substituted-4-prenyl-piperazine derivative, which is structurally unrelated to most other opioid drugs. The (S)-enantiomers in this series are more active as opioid agonists, but the less active (R)-enantiomer of this compound, AD-1211, is a mixed agonist–antagonist at opioid receptors with a similar pharmacological profile to pentazocine, and has atypical opioid effects with little development of tolerance or dependence seen after extended administration in animal studies.

Fluanisone is a typical antipsychotic and sedative of the butyrophenone chemical class. It is used in the treatment of schizophrenia and mania. It is also a component (along with fentanyl) of the injectable veterinary formulation fentanyl/fluanisone (Hypnorm) where it is used for rodent analgesia during short surgical procedures.

SB-271046 is a drug which is used in scientific research. It was one of the first selective 5-HT6 receptor antagonists to be discovered, and was found through high-throughput screening of the SmithKline Beecham Compound Bank using cloned 5-HT6 receptors as a target, with an initial lead compound being developed into SB-271046 through a structure-activity relationship (SAR) study. SB-271046 was found to be potent and selective in vitro and had good oral bioavailability in vivo, but had poor penetration across the blood–brain barrier, so further SAR work was then conducted, which led to improved

Amperozide is an atypical antipsychotic of the diphenylbutylpiperazine class which acts as an antagonist at the 5-HT2A receptor. It does not block dopamine receptors as with most antipsychotic drugs, but does inhibit dopamine release, and alters the firing pattern of dopaminergic neurons. It was investigated for the treatment of schizophrenia in humans, but never adopted clinically. Its main use is instead in veterinary medicine, primarily in intensively farmed pigs, for decreasing aggression and stress and thereby increasing feeding and productivity. ==See also== FG-5893 == References ==

Suproclone is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs, developed by the French pharmaceutical company Rhône-Poulenc. Other cyclopyrrolone drugs include zopiclone, pagoclone and suriclone.