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Recent studies have suggested that serotonin reuptake inhibitors (SSRI's), prescribed for the relief of depression, can cause sexual dysfunction in up to fifty percent of those taking them. The SSRI's--including fluoxetine (Prozac), sertraline (Zoloft), and paroxetine (Paxil)--affect mood stabilization by promoting the transmission of the neurotransmitter serotonin, although enhancing serotonergic function can decrease libido or lead to erectile difficulties. As an alternative to lowering antidepressant dosages and risking losing therapeutic gains, administering serotonin-blockers, such as cyproheptadine (Periactin) and yohimbine (Yocon), has been shown to restore sexual function. However, the serotonin antagonist, cyproheptadine, causes sedation and can reverse the antidepressant or anti-obsessive effect of the SSRI. Yohimbine enhances transmission of the neurotransmitter epinephrine, increasing the flow of blood to erectile tissue and stimulating sexual desire by activating the cerebral cortex. Its drawbacks are increased levels of panic attacks and higher required dosages. Other potential biochemical stratagems are: amantadine (Symmetrel), bromcriptine (Parlodel), and buspirone (Buspar), which enhance dopamine and serotonin transmission; and bethanecol (Urechline), which enhances choline transmission. One study indicates improved sexual response when the nonserotonergic, mildly dopamine-enhancing buproprion (Welbutrin) is substituted for fluoxetine.
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We aimed to test the hypothesis that buspirone may exert a beneficial acute effect on esophageal motor dysfunction in symptomatic patients with SSc.
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Differences between the left and right sides of the brain are found throughout the animal kingdom, but the consequences of altered neural asymmetry are not well understood. In the zebrafish epithalamus, the parapineal is located on the left side of the brain where it influences development of the adjacent dorsal habenular (dHb) nucleus, causing the left and right dHb to differ in their organization, gene expression, and connectivity. Left-right (L-R) reversal of parapineal position and dHb asymmetry occurs spontaneously in a small percentage of the population, whereas the dHb develop symmetrically following experimental ablation of the parapineal. The habenular region was previously implicated in modulating fear in both mice and zebrafish, but the relevance of its L-R asymmetry is unclear. We now demonstrate that disrupting directionality of the zebrafish epithalamus causes reduced exploratory behavior and increased cortisol levels, indicative of enhanced anxiety. Accordingly, exposure to buspirone, an anxiolytic agent, significantly suppresses atypical behavior. Axonal projections from the parapineal to the dHb are more variable when it is located on the right side of the brain, revealing that L-R reversals do not necessarily represent a neuroanatomical mirror image. The results highlight the importance of directional asymmetry of the epithalamus in the regulation of stress responses in zebrafish.
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This case illustrates that compliance with the basic principles of geriatric pharmacology (start low, go slow, and avoid polypharmacy) might have prevented a clinical syndrome that could have caused serious complications. Fortunately, serotonin syndrome was recognized early, the offending agents were discontinued, and supportive treatment was provided. The patient was ultimately treated with mirtazapine, an antidepressant not associated with serotonergic effects.
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N-(2-(4-(2-Methoxyphenyl)-1-piperazinyl)ethyl)-N-(2- pyridyl)cyclohexanecarboxamide trihydrochloride (WAY-100635) is a new, potent and selective 5-HT1A receptor antagonist. We have evaluated radiolabelled WAY-100635 as a prospective radioligand for positron emission tomography (PET) by studying biodistribution in rat ex vivo. After intravenous injection, [O-methyl-3H]WAY-100635 cleared rapidly from plasma but was retained in brain. Specific binding was quantified from kinetic studies, using a reference-tissue compartment model, fitting for binding potential (k3/k4). The regional variation in binding potential correlated with the known distribution of 5-HT1A receptors. Saturation studies gave Bmax values in vivo that were consistent with those reported in vitro. At 60 min after injection, the ratio of radioactivity in 5-HT1A receptor-rich regions (e.g. septum, entorhinal cortex and hippocampus) to that in cerebellum reached approximately 16. Pre-dosing the rats with WAY-100635 (2 mg/kg) reduced this ratio to one, whereas similar pre-dosing with citalopram (5-HT uptake site inhibitor), prazosin (alpha 1A-adrenoceptor antagonist) or idazoxan (alpha 2-adrenoceptor antagonist) caused little or no reduction. Substantial (77%) blockade of [3H]WAY-100635 binding was achieved with the 5-HT1A receptor agonist, 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), and the partial agonists, ipsapirone and buspirone. Thus, the properties of WAY-100635 are such that, when labelled with carbon-11, it could provide a radioligand suitable for clinical and pharmacological investigations of central 5-HT1A receptors in man using PET.
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Baseline anxiety levels were not related to antidepressant response to treatment with either bupropion SR or sertraline, nor did they differentiate between responders to bupropion SR and responders to sertraline.
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Alprazolam, at doses double those generally recommended for anxiety disorders, appears to be as effective as tricyclic antidepressants (TCAs) in the acute treatment of mild to moderate MDD. Alprazolam was also found to have a more rapid onset of action than to TCAs, particularly for the improvement of anxiety, somatization, and insomnia. Two azapirones (buspirone and gepirone) also have demonstrated a modest acute antidepressant effect in preliminary studies, albeit only in a depressed outpatient sample with considerable anxiety at baseline. Finally, various antidepressant drugs (imipramine, trazodone, paroxetine) were shown to have, at the least, comparable efficacy to benzodiazepines (BZDs) in the acute treatment of GAD.
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We conducted a systematic review and aimed to answer the following clinical question: What are the effects of treatments for GAD? We searched: Medline, Embase, The Cochrane Library and other important databases up to February 2006 (Clinical Evidence reviews are updated periodically, please check our website for the most up-to-date version of this review). We included harms alerts from relevant organisations such as the US Food and Drug Administration (FDA) and the UK Medicines and Healthcare products Regulatory Agency (MHRA).
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Puerarin (8-β-D-glucopyranosyl-7-hydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one) is a major pharmacological component of Puerariae Radix, the root of Pueraria lobata. We investigated the effect of puerarin on hepatic cytochrome P450-mediated drug metabolism in rats and humans. The in vitro cytochrome P450 inhibitory effect of puerarin in human and rat liver microsomes was evaluated using the following model cytochrome P450 substrates: phenacetin for CYP1A, diclofenac for CYP2C, dextromethorphan for CYP2D, and testosterone for CYP3A. The in vivo pharmacokinetics of intravenous and oral buspirone, a probe substrate for CYP3A, was studied with single simultaneous intravenous coadministration of puerarin in rats. In the in vitro cytochrome P450 inhibition study, the rate of disappearance of testosterone was significantly reduced in the presence of 10 µM PU, while that of other cytochrome P450 substrates was not significantly affected in both human and rat liver microsomes, suggesting that puerarin inhibits the in vitro hepatic CYP3A-mediated metabolism in the human and rat systems (IC50 = 15.5 ± 3.9 µM). After intravenous administration of buspirone with single simultaneous coadministration of intravenous puerarin at a dose of 10 mg/kg in rats, the total area under the plasma concentration-time curve from time zero to time infinity was increased while time-averaged total body clearance decreased. When buspirone was orally administered in rats with the 10 mg/kg intravenous puerarin coadministration, both total area under the plasma concentration-time curve from time zero to time infinity and the extent of absolute oral bioavailability were significantly increased. Therefore, results of the in vitro microsomal and in vivo pharmacokinetic studies suggest the possible inhibition of hepatic CYP3A-mediated drug metabolism by puerarin administration, potentially leading to metabolism-mediated herb-drug interactions with clinical significance.
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Irritability is a common neuropsychiatric feature of Huntington's disease (HD), with prevalences varying from 38% to 73%. Similar prevalences of irritability are reported in other neurodegenerative disorders and traumatic brain injury, especially when the frontal lobe is involved. Before therapeutic interventions are initiated, the clinician should analyze the severity and frequency of the irritable behavior. By examining irritability in a broader spectrum, a tailor-made treatment can be provided.In general, I recommend as a first step a selective serotonin reuptake inhibitor (SSRI), such as sertraline, or the mood stabilizer valproate; they both have a mild side effect profile. Next, if the result is insufficient, I advise a switch between these two medications. As an alternative, I recommend a switch to a low dose of an atypical antipsychotic, preferably twice daily. Buspirone may be another alternative. Both antipsychotics and buspirone are also used as an add-on. Other mood stabilizers and beta-adrenergic receptor antagonists should only be used when earlier treatments are ineffective. The use of acetylcholinesterase inhibitors for the treatment of irritability is discouraged, as results are unclear. Synthetic cannabinoids are an interesting new therapeutic option, though their "illicit" compound and side effect profile make them not a first-line option.It is important to identify possible comorbid psychiatric disorders, because irritability may be secondary to a psychiatric condition, and the choice of medication partly depends on the co-occurrence of a specific psychiatric disorder. For example, antipsychotic medication would be the treatment of choice in delusional HD patients with excessive irritability, instead of an SSRI or valproate.Besides psychiatric comorbidity, the choice of medication also depends on the general medical condition, the side effect profile, and drug-drug interactions with other medications in concomitant use. Patients with advanced disease are particularly likely to be using various other types of medications.In addition to pharmacotherapy, behavioral therapy or other psychotherapeutic interventions may be helpful to reduce levels of stress and should be considered.
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The 5-HT2B receptor agonist, BW 723C86 (10, 30(mg/kg i.p. 30 min pre-test), increased the number of punishments accepted in a rat Vogel drinking conflict paradigm over 3 min, as did the benzodiazepine anxiolytics, chlordiazepoxide (2.5-10 mg/kg p.o. 1 h pre-test) and alprazolam (0.2-5 mg/kg p.o. 1 h pre-test), but not the 5-HT2C/2B receptor agonist, m-chlorophenylpiperazine (mCPP, 0.3-3 mg/kg i.p) or the 5-HT1A receptor agonist, buspirone (5-20 mg/kg p.o. 1 h pre-test). The effect of BW 723C86 was unlikely to be secondary to enhanced thirst, as BW 723C86 did not increase the time that rats with free access to water spent drinking, nor did it reduce sensitivity to shock in the apparatus. The anti-punishment effect of BW 723C86 was opposed by prior treatment with the 5-HT2/2B receptor antagonist, SB-206553 (10 and 20 mg/kg p.o. 1 h pre-test), and the selective 5-HT2B receptor antagonist, SB-215505 (1 and 3 mg/kg p.o. 1 h pre-test), but not by the selective 5-HT2C receptor antagonist, SB-242084 (5 mg/kg p.o.), or the 5-HT1A receptor antagonist, WAY 100635 (0.1 or 0.3 mg/kg s.c. 30 min pre-test). Thus, the anti-punishment action of BW 723C86 is likely to be 5-HT2B receptor mediated. This is consistent with previous reports that BW 723C86 exhibited anxiolytic-like properties in both the social interaction and Geller-Seifter conflict tests.
The effectiveness of a treatment for alcohol dependence can be appropriately determined only after controlling for the usual clinical course of alcoholism, subgroups of alcohol-dependent individuals, and placebo effects. The results of appropriate treatment trials must also be interpreted in light of the side effects and costs, and there must be assurances that the overall improvement in functioning observed with the drug is significant enough to outweigh the liabilities. In addition, medications are almost always used in combination with education, counseling, and behavioral therapies, and the impact of these additional treatments must be considered. Viewed from this perspective, 3 medications are quite promising regarding their potential future impact in the alcohol field, including naltrexone, the medication with the most available data in the United States. There are additional data regarding buspirone and acamprosate. Intriguing results have also been generated regarding medications that affect serotonin and dopamine brain activity and with alcohol-sensitizing drugs such as disulfiram. However, none of these medications has been proven to be clinically effective in the routine treatment of the average alcoholic. It is hoped that future research will help identify subgroups of alcohol-dependent men and women who are most likely to respond to specific pharmacological treatments.
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Buspirone is an azaspirodecanedione that has anxiolytic actions in man and anticonflict actions in experimental animals. In contrast to many commonly used anxiolytic agents, buspirone does not appear to have significant sedative, muscle relaxant or anticonvulsant actions. Consequently, it has been termed an "anxioselective" agent. The effects of buspirone and related compounds have been examined in a number of neurotransmitter systems that have been linked to the actions of other anxiolytic agents. Buspirone has been shown to affect dopaminergic, serotonergic and noradrenergic pathways, as well as the GABA-benzodiazepine receptor chloride ionophore complex. Nonetheless, the doses (in vivo) and/or concentrations (in vitro) of buspirone (and related compounds) needed to affect these systems are not consistent with a causal relationship between the anxiolytic actions of buspirone and any of these systems. The neurochemical mechanism by which buspirone and related compounds exert both anticonflict and anxiolytic actions remains unknown.
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Buspirone is known to stimulate prolactin release. Clinical studies (e.g. in chronic fatigue syndrome) suggest that the response may be influenced by baseline cortisol levels. We conducted a double-blind placebo-controlled study to examine the relationship between the prolactin response to buspirone challenge and baseline cortisol level. Fifty healthy volunteers took part in the study. Buspirone was found to consistently elevate PRL levels above those seen following placebo administration. The PRL response as measured by area under the curve was highly correlated with the baseline cortisol level.
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Buspirone treatment leads to significant changes in CD8 T-cell count and in CD4/CD8 ratio. Thus, agents affecting the adenosine 3', 5'-cyclic monophosphate/protein kinase A type 1 (cAMP/PKA-1) pathway may be candidates for positive immune modulation in patients with HIV-1 infection.
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Testicular pain is rarely caused by medications. Product labeling for statins does not list urinary adverse events as common. However, labeling for atorvastatin and pravastatin lists rare urologic adverse effects. A literature search did not reveal any previously reported cases of testicular adverse effects from statins. However, statins have been shown to inhibit cholesterol synthesis in the testis. Some data indicate that statins reduce serum testosterone concentrations, but other data indicate that statins have no effect on sex hormones or spermatogenesis. Data are also available indicating that aspirin might affect testosterone concentrations and testicular function. It is difficult to know whether either of the above hormonal mechanisms was associated with our patient's testicular discomfort, but the time course and challenge/rechallenge aspects of the case suggest that the statins were the cause.
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Tandospirone is an azapirone drug that has high affinity for serotonin-1A (5-HT-1A) receptors and preclinical effects predictive of antidepressant and/or anxiolytic efficacy. 5-HT-1A receptor agonists, such as 8-hydroxy-2-(di-n-propyl-amino)tetralin, increase the plasma prolactin concentration in rats, probably by an action in the brain that leads to an increase in prolactin release from the pituitary gland. The purpose of this study was to examine the effect of tandospirone on plasma prolactin concentration in awake, freely moving male rats. We found that i.v. administration of tandospirone results in a rapid and dose-related increase in the plasma prolactin concentration. The plasma prolactin level peaks about 10 min after injection and returns to base-line values within 30 min after injection. The ED50 of tandospirone to increase plasma prolactin levels is approximately 0.3 mg/kg. This effect of tandospirone is blocked by pretreatment with the 5-HT antagonists metergoline and NAN-190 and shows cross-desensitization with the 5-HT-1A agonist 8-hydroxy-2-(di-n-propyl-amino)tetralin. Thus the effect of tandospirone on plasma prolactin concentration appears to be mediated by 5-HT-1A receptors. In contrast to this effect of tandospirone, 1-(2-pyrimidyl)-piperazine (1-PP), the common metabolite of tandospirone and other azapirone drugs, has no effect on plasma prolactin levels. The effect of chronic administration of tandospirone was examined by measuring the prolactin response to an acute i.v. injection of tandospirone 24 hr after the last of chronic injections of tandospirone (10 mg/kg, s.c., twice a day for 2 weeks).(ABSTRACT TRUNCATED AT 250 WORDS)
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Remission, i.e. the complete absence of symptoms, is the major goal in the treatment of major depressive disorders because residual symptoms cause less functioning and a worse outcome. Despite several treatment steps, numerous patients do not reach complete remission of symptoms. In these patients, it is necessary to rule out several possible causes, including inadequate pharmacotherapy, to confirm the diagnosis of treatment-resistant depression (TRD). In the treatment of TRD, pharmacotherapy plays a central role. Nonpharmacological treatment strategies such as psychotherapy, electroconvulsive therapy, and other brain stimulation methods are also used for TRD treatment and are discussed elsewhere in this issue. Regarding complex pharmacotherapy of TRD, only a limited number of randomized-controlled trials have been done. In consequence, treatment decisions are often based on clinical experience, case series, and uncontrolled studies. Nevertheless, there are some interesting new developments, which are summarized and assessed on the basis of existing evidence in this article. Afore, we present an overview of the most important definitions, epidemiologic data, diagnostic needs and methods for treatment optimization. We end with a critical view on the present and future development of antidepressant drugs.
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The available literatures show that 5-HT(1A) receptors are widely distributed throughout the basal ganglia, and their activation facilitate dopamine release. Neuroleptic drugs such as haloperidol induce Parkinson-like syndrome through blocking brain D(2) receptors. This study aimed to investigate effect of buspirone, a partial agonist of 5HT(1A) receptor, on motor dysfunctions induced by haloperidol and involvement of 5HT(1A) receptors in this regard.
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Thirteen [(aryl/heteroaryl-piperazinyl)alkyl]benzotriazoles were prepared as potential trazodone- and buspirone-like drugs. The synthesized compounds displayed from moderate to good affinity to the serotonin 5-HT1A receptor and only modest or poor affinity to the dopamine D2 receptor, similar to buspirone. The introduction of substituents on the benzotriazole ring did not improve the affinity to the 5-HT1A receptor, compared to the previously described unsubstituted derivatives. In a general pharmacological screening, which concerned only three of these compounds so far (5, 7 and 13), several in vitro and in vivo activities were observed. The guinea pig ileum contractions, induced either electrically or by several agonists, were strongly inhibited; at higher concentrations also the spontaneous tone of the guinea pig trachea was reduced. Compound 13 exhibited good analgesic activity in mice in the formalin-induced algesia and in the writhing test. The same at 30 mg kg(-1) p.o. also displayed antihypertensive activity probably related to calcium channel blockade and adrenergic alpha1 antagonism. In binding assays, 13 showed a IC50 = 580 nM for displacing [3H]prazosin from alpha1 receptor. Finally, compound 5 (and, to a minor extent, compound 13) protected mice against potassium cyanide induced hypoxia.
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Buspirone has previously been demonstrated to be efficacious in the treatment of anxiety. This four-week double-blind parallel study compared buspirone to diazepam and placebo in the treatment of 119 outpatients diagnosed as having generalized anxiety disorder. After a seven-day placebo washout period, eligible patients were randomized to one of three treatment groups. Buspirone (5 mg) and diazepam (5 mg) were administered BID and individually titrated to an optimal therapeutic dose by the end of week two. Buspirone and diazepam were equally effective in reducing Hamilton Anxiety (HAM-A) total and psychic factor scores from baseline values. Buspirone alone was significantly better than placebo in reducing the HAM-A somatic factor score. Sixty-seven percent of both active treatment groups who were classified as "ill" on the baseline global psychopathology rating scale achieved a "not ill" status by study end. There were no significant differences between treatment groups at endpoint on the 56-item Symptom Checklist self-rating scale. Buspirone was demonstrated to be as effective as diazepam in relieving anxiety in this outpatient sample.
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Disease-free women who had successfully completed treatment for early-stage breast cancer were assessed. On the basis of the diagnostic interview for CRFS and a structured psychiatric interview, women were classified as either "cases" of CRFS or "controls." Women with comorbid psychiatric diagnoses were excluded. Volunteers underwent a challenge test using buspirone (a serotonin-selective agonist) using a double-blind, randomized, placebo-controlled protocol. Cortisol and prolactin responses were assessed at hourly intervals for the four hours after administration of buspirone.
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The authors review recent progress in the pharmacological treatment of anxiety disorders. Most research within the last five years has focused on panic disorder; the findings include support for the usefulness of imipramine and clomipramine and probably other agents; evidence that the benzodiazepines alprazolam, diazepam, lorazepam, and clonazepam are approximately equally effective as antipanic agents; and high variability in relapse rates after discontinuation of drug treatment. Further work is required to determine whether buspirone and other forthcoming serotonin agonist drugs have a role in treating panic disorder and other anxiety disorders. For generalized anxiety disorder, scientific studies do not support the effectiveness of beta blocker; tricyclics may be potentially useful. Psychopharmacological treatments for social phobia, obsessive-compulsive disorder, and posttraumatic stress disorder are also reviewed.
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PPI and SH were evaluated in four strains of mice: BALB/cByJ, MORO, 129/SvEv and C57BL/6J. The effects of antipsychotic [haloperidol (1, 3 and 6 mg/kg), clozapine (0.3, 1, 3 and 30 mg/kg) and risperidone (0.1, 0.3 and 1 mg/kg)] and non-antipsychotic [diazepam (3, 10 and 30 mg/kg), buspirone (1, 3 and 10 mg/kg), desipramine (3, 10 and 30 mg/kg), morphine (3, 10 and 30 mg/kg) and scopolamine (0.3, 1 and 3 mg/kg)] drug treatments were studied on PPI.
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Almorexant reduced FPS, but did not affect EPM behavior. Almorexant's overall pattern of effects on FPS was comparable to but less pronounced than that of the anxiolytic benzodiazepine diazepam. The endogenous orexin system actively contributes to fear-conditioned startle reactions in the rat.
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Buspirone may have similar efficacy as fluoxetine in reducing bulimic and depressive symptoms in patients with bulimia, however may not cause significant changes of serotonin level in serum.
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IMR-32 and SK-N-MC cells were found to contain [3H]quinuclidinyl benzilate specific binding sites inhibited by pirenzepine in a manner suggesting the presence of both M1-type and M2-type muscarinic receptor recognition sites. Neither cell had detectable [3H]8-OH-DPAT binding sites. Carbachol stimulated the rate of inositol phospholipid breakdown in IMR-32 and SK-N-MC human neuroblastoma cells with an EC50 value of about 50 microM in both cases. Pirenzepine inhibited the carbachol (100 microM)-stimulated inositol phospholipid breakdown in both cells with Hill slopes of unity and IC50 values of 15 nM (IMR-32) and 12 nM (SK-N-MC). The 5-HT1A receptor agonist 8-OH-DPAT competitively inhibited carbachol-stimulated inositol phospholipid breakdown with pA2 values of 5.78 (IMR-32) and 5.61 (SK-N-MC). These values are consistent with the inhibitory potency of 8-OH-DPAT towards [3H]quinuclidinyl benzilate binding in these cells. The 5-HT agonists 5-MeODMT and buspirone at micromolar concentrations inhibited carbachol-stimulated breakdown in IMR-32 cells. The inhibition by 8-OH-DPAT and 5-MeODMT was not affected by preincubation with (-)alprenolol. 5-HT (10-100 microM) was without effect on either basal or carbachol-stimulated breakdown. It is concluded that IMR-32 and SK-N-MC neuroblastoma cells express muscarinic M1-type but not serotoninergic receptors coupled to phosphoinositide-specific phospholipase C. 8-OH-DPAT acts as a weak antagonist at these muscarinic receptors.