*Aripiprazole

Mailman RB, Murthy V (May 2010). "Third generation antipsychotic drugs: partial agonism or receptor functional selectivity?". ... "Abilify (Intramuscular)". Drugs.com. "Abilify". Drugs.com. Roth, BL; Driscol, J. "PDSP Ki Database". Psychoactive Drug ... ISBN 978-0-07-162442-8. Nguyen CT, Rosen JA, Bota RG (2012). "Aripiprazole partial agonism at 5-HT2C: a comparison of weight ... Wood M, Reavill C (2007). "Aripiprazole acts as a selective dopamine D2 receptor partial agonist". Expert Opin Investig Drugs. ...

*Serotonin modulator and stimulator

As such, a drug which combines the actions of, say, an SRI, 5-HT1A partial agonism, and 5-HT7 receptor antagonism, could, in ... A serotonin modulator and stimulator (SMS), sometimes referred to more simply as a serotonin modulator, is a type of drug with ... An alternative term is serotonin partial agonist/reuptake inhibitor (SPARI), which can be applied only to vilazodone. It is ... March 2005). "Neurochemical evaluation of the novel 5-HT1A receptor partial agonist/serotonin reuptake inhibitor, vilazodone". ...

*Naphthylpiperazine

It acts as a non-selective, mixed serotonergic agent, exerting partial agonism at the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5- ... 1-(1-Naphthyl)piperazine (1-NP) is a drug which is a phenylpiperazine derivative. ...

*Penbutolol

... is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors. It was ... two new beta-adrenergic blockers with partial agonism. Journal of Clinical Pharmacology, 30(5):412-21 PMID 2189902 FDA History ... Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors. ... The ability of penbutolol to act as a partial agonist proves useful in the prevention of bradycardia as a result of decreasing ...

*Pozanicline

It binds with high affinity subtype-selective to the α4β2 nicotinic acetylcholine receptors and has partial agonism to the α6β2 ... CNS Drug Reviews. 2004 Summer;10(2):167-82. PMID 15179445 Wilens TE, Decker MW. Neuronal nicotinic receptor agonists for the ... It has particularly low tendency to cause side effects compared to other drugs in the class, making it an exciting candidate ... Pozanicline (INN, codenamed ABT-089) is a drug developed by Abbott, that has nootropic and neuroprotective effects. Animal ...

*Efficacy

CS1 maint: Uses authors parameter (link) Mukhtasimova N, Lee WY, Wang HL, Sine SM (2009). "On the nature of partial agonism in ... a small molecule drug. Intrinsic activity is a relative term that describes a drug's efficacy relative to a drug with the ... It was found that partial agonism results from deficiency in the first step, and that the opening and shutting steps are ... CS1 maint: Uses authors parameter (link) Lape R, Colquhoun D, Sivilotti L (2008). "On the nature of partial agonism in the ...

*Diprenorphine

Moreover, due to partial agonism of the KOR, where it appears to possess significantly greater intrinsic activity relative to ... The drug is not approved for use in humans. Diprenorphine is the strongest opioid antagonist that is commercially available ( ... which has an improved safety-profile due to its partial agonism character), are not used in humans because the dose for a human ... Since diprenorphine also has partial agonistic properties of its own, it should not be used on humans in the event that they ...

*Labetalol

... relaxes vascular smooth muscle by a combination of this partial beta2- agonism and through alpha1- blockade. Overall ... Adrenoceptor Antagonist Drugs IN: Basic & Clinical Pharmacology (12 ed.). San Francisco: McGraw Hill Lange Medical. pp. 151-168 ... I". Drugs. 28 Suppl 2: 16-34. doi:10.2165/00003495-198400282-00003. ISSN 0012-6667. PMID 6151889. Arulkumaran, N; Lightstone, L ... Long term labetalol use also has different effects from other beta-blocking drugs. Other beta-blockers, such as propranolol, ...

*Lumateperone

... a property which is likely due to its partial agonism of presynaptic D2 receptors. In accordance, similarly to aripiprazole, ... Nancy A. Melville (2015). "Novel Drug Promising for Schizophrenia". Medscape Medical News. Li P, Zhang Q, Robichaud AJ, Lee T, ... It acts as a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of ... List of investigational antipsychotics List of investigational antidepressants List of investigational sleep drugs Sylvain ...

*Receptor antagonist

Partial agonists are defined as drugs that, at a given receptor, might differ in the amplitude of the functional response that ... In addition, it has been suggested that partial agonism prevents the adaptive regulatory mechanisms that frequently develop ... Competitive antagonists are used to prevent the activity of drugs, and to reverse the effects of drugs that have already been ... Rees S, Morrow D, Kenakin T (2002). "GPCR drug discovery through the exploitation of allosteric drug binding sites". Receptors ...

*Memantine

... only exhibiting partial agonism or antagonism. Some of memantine's adverse effects arise through this route. Memantine was ... a comprehensive review of the non-medical use of dissociative drugs". Drug Testing and Analysis. 6 (7-8): 614-32. doi:10.1002/ ... Sales of the drug reached $1.8 billion for 2014. The cost of Namenda was $269 to $489 a month in 2012. In February 2014 as the ... Nat Rev Drug Discov. 2004 Feb;3(2):109-10. PMID 15040575 "Form 10-KSB For the fiscal year ended June 30, 1996". SEC Edgar. ...

*Acetothiolutamide

... including AR partial agonism and antagonism. In accordance with its poor metabolic stability, acetothiolutamide is not orally ... Drug Metabolism and Disposition. 34 (10): 1713-21. doi:10.1124/dmd.106.009985. PMID 16815963. Kim J, Wu D, Hwang DJ, Miller DD ...

*Atypical antipsychotic

To have partial agonism at the 5-HT1A receptor can yield absence of weight gain in an antipsychotic. This is very relevant for ... These drugs have relatively long half-lives. Each drug has a different half-life, but the occupancy of the D2 receptor falls ... It has been suggested that there is no validity to the term "second-generation antipsychotic drugs" and that the drugs that ... Physical dependence with these drugs is very rare. However, if the drug is abruptly discontinued, psychotic symptoms, movement ...

*4-HO-MiPT

... its method of action is believed to result from its partial agonism of 5-HT2A and 5-HT1A serotonin receptors.[citation needed] ... The substance could also be considered illegal in the UK under the Misuse of Drugs Act 1971. 4-HO-MiPT is an unscheduled drug ... MiPT 4-AcO-MiPT 4-MeO-MiPT 5-MeO-MiPT Dimethyltryptamine Psilocybin Metocin TiHKAL Psychedelic drug Psychoactive drug http:// ...

*Dopamine agonist

... the psychoactivity of which is mainly due to Kappa-opioid receptor agonism; partial agonist at the D2 with an Intrinsic ... Some medical drugs act as dopamine agonists and can treat hypodopaminergic (low dopamine) conditions; they are typically used ... partial agonist. Psychoactivity mainly due to NMDA antagonism) Quinpirole (Partial agonist of the D2 and D3 family of receptors ... There are two classes of drugs that act as indirect agonists of dopamine receptors: dopamine reuptake inhibitors and dopamine ...

*Meta-Chlorophenylpiperazine

EMCDDA ANVISA resolution - Portaria SVS/MS 344/98 "关于印发《非药用类麻醉药品和精神药品列管办法》的通知" (in Chinese). China Food and Drug Administration ... 32.1 and 28.8 nM). It acts as a partial agonist of the human 5-HT2C receptor but as an antagonist of the human 5-HT2A and 5- ... In accordance with its lack of agonism towards the human 5-HT2A receptor, there are no reports that mCPP produces ... It was initially developed in the late-1970s and used in scientific research before being sold as a designer drug in

*Nalfurafine

The drug also shows lower evidence of tolerance for effects such as analgesia and sedation in animals relative to other KOR ... Nalfurafine has been found in vitro to bind to the μ-opioid receptor and to possess weak partial agonist activity at this site ... However, in vivo, nalfurafine has shown no indications of MOR agonism or antagonism in animals or humans, including no evidence ... The drug was originally developed as an analgesic in surgery, but while effective in animal models of nociception, it was ...

*Cannabidiol

In 2016, the Drug Enforcement Administration added "marihuana extracts" to the list of Schedule I drugs, which it defined as " ... It has also been shown to act as a 5-HT1A receptor partial agonist, and this action may be involved in the antidepressant, ... Cannabidiol's pharmacological effects have additionally been attributed to PPARγ agonism and intracellular calcium release. ... Cannabidiol is currently a class B1 controlled drug in New Zealand under the Misuse of Drugs Act. It is also a prescription ...

*Sarizotan

"Putative antipsychotics with pronounced agonism at serotonin 5-HT1A and partial agonist activity at dopamine D2 receptors ... "Merck KGaA discontinues development of Parkinson drug Sarizotan UPDATE". Forbes. 23 June 2006. ...

*Capeserod

Hille C, Bate S, Davis J, Gonzalez MI (December 2008). "5-HT4 receptor agonism in the five-choice serial reaction time task". ... Capeserod (INN, previously known as SL65.0155) is a selective 5-HT4 receptor partial agonist with Ki = 0.6 nM and IA = 40-50% ( ... RS-67,333 "WHO Drug Information. Vol. 20, No. 3, 2006. International Nonproprietary Names for Pharmaceutical Substances (INN). ... Micale V, Leggio GM, Mazzola C, Drago F (November 2006). "Cognitive effects of SL65.0155, a serotonin 5-HT4 receptor partial ...

*Agonist

However, a drug can act as a full agonist in some tissues and as a partial agonist in other tissues, depending upon the ... Kenakin T (March 2001). "Inverse, protean, and ligand-selective agonism: matters of receptor conformation". FASEB J. 15 (3): ... When a drug is used therapeutically, it is important to understand the margin of safety that exists between the dose needed for ... It might be argued that the endogenous agonist is simply a partial agonist in that tissue. An irreversible agonist is a type of ...

*Beta blocker

"First-line drugs inhibiting the renin angiotensin system versus other first-line antihypertensive drug classes for hypertension ... See partial agonist for a more general description. Some beta blockers (e.g. oxprenolol, pindolol, penbutolol, labetalol and ... this term is used particularly with beta blockers that can show both agonism and antagonism at a given beta receptor, depending ... Adverse drug reactions associated with the use of beta blockers include: nausea, diarrhea, bronchospasm, dyspnea, cold ...

*Opioid antagonist

... and is in fact a partial inverse agonist at μ-opioid receptors, and so is the preferred antidote drug for treating opioid ... by virtue of the fact that both MOR and KOR agonism independently confer pain relief). However, these opioid analgesics have ... These drugs are used mainly as antidotes to reverse opioid overdose and in the treatment of alcohol dependence and opioid ... A variety of partial agonists or mixed agonists-antagonists of the MOR and KOR are also marketed, and include butorphanol, ...

*Buspirone

The drug has also been found to be effective in the treatment of depression as a standalone drug. There is evidence that ... The metabolite is a high-affinity partial agonist of the 5-HT1A receptor (Ki = 25 nM) similarly to buspirone, and has ... Some of its effects may be mediated via oxytocin release secondary to 5-HT1A receptor agonism.[non-primary source needed] ... Jajoo, HK; Mayol, RF; LaBudde, JA; Blair, IA (1989). "Metabolism of the antianxiety drug buspirone in human subjects". Drug ...

*Lisuride

... of cardiac valvulopathy adverse drug reaction reports supports the concept of a crucial role for 5-HT2B receptor agonism in ... Lisuride is a dopamine and a partial agonist for several serotonin receptors. It is an antagonist at the serotonin 5-HT2B ... Lisuride is not currently available in the US, as the drug was not a commercial success in comparison with other dopamine ... Newer findings suggest the lack of psychedelic action arises from the phenomenon of biased agonism. Stimulation of the 5-HT2A ...

*Butorphanol

... exhibits partial agonist and antagonist activity at the μ-opioid receptor, as well as partial agonist activity at ... Butorphanol can cross the placenta, and it will be present in the milk of lactating mares who are given the drug. The drug is ... Additionally, κ-agonism can cause dysphoria at therapeutic or supertherapeutic doses; this gives butorphanol a lower potential ... Butorphanol is listed under the Single Convention on Narcotic Drugs 1961 and in the United States is a Schedule IV Narcotic ...