ABSTRACT In order to illustrate the usefulness of the dorid nudibranch Doriopsilla albopunctata for electrophysiological studies, maps of the pleural ganglia were made and gross cellular responses of autorhythmic neurons to applied neuroactive peptides and amines were observed. Dopamine, 5-HT and FMRF-amide all induced both depolarizations and hyperpolarizations in different autorhythmic cells of D. albopunctata. Responses ranged from complete inhibition of firing, to increased rate of repetetive firing in a beating cell, and complete transformation of bursting activity into beating activity. In addition, 5-HT induced in a beating cell a depolarization that attenuated with repeated applications. 5-HT applied in combination with FMRF-amide produced varied responses that were not seen with applications of 5-HT and FMRF-amide separately. CPT-CAMP and forskolin, which both serve to enhance CAMP production, were applied to selected cells in order to observe if any of the previous cellular responses were mediated by an increase in cAMP levels. Application of CPT-CAMP, constituting an increase in CAMP levels only, produced no response. Forskolin produced many effects, but they did not resemble any responses induced by the previously applied neuroactive peptides and amines. It seems then, that the applied neuroactive peptides and amines do not mediate their actions through CAMP levels. In addition, although forskolin is a CAMF analog, from the differing responses to CPT-CAMP and forskolin, forskolin seems to be inducing its cellular responses via a mechanism other than a rise in CAMF concentration. INTRODUCTION Little work has been done on the nudibranch Doriopsilla albopunctata although it is an ideal organism for studying electrophysiology. Easy accessibility and preparation, great viability and large easily identified neurons are all good reasons why D. albopunctata should be taken advantage of and studied further. In our study of the pharmacology of various D. albopunctata bursting and beating cells located in the pleural ganglia, we observed both depolarizing and hyperpolarizing responses to the applied neuroactive peptides and amines, with none having a dominant effect on all of the cells observed. We conclude from our studies that the autorhythmic neurons of D. albopunctata have various, differing mechanisms by which they respond to a particular substance, depending on individual cellular properties. These differences may lie at the level of receptors, second messengers, ion channel properties, etc. Comparing our results with known cellular responses to the same neuroactive peptides and amines on similar Aplysia neurons, we then determined if they could also possibly account for our observations. In some D. albopunctata cells, the mechanisms operating in Aplysia could feasibly underly our observed responses. But in other cells, we saw unexpected results, indicating the presence of new, unknown mechanisms. Further studies to elucidate the mechanisms behind these observed unique responses could add tremendously to our existing knowledge concerning these neuroactive peptides and amines. MATERIALS AND METHODS Doriopsilla albopunctata were collected subtidally from Montery Bay, CA., and stored in flowing natural sea water tanks of approximately 13°C. They were not fed. Ganglia were surgically removed and treated with dispase, a neutral protease, for one hour followed by a minimum of a two hour rinse in ASW to facilitate removal of the epineural sheath. Experiments were performed on the pleural ganglia pinned in a Sylgard dish of approximately 5ml bath volume and perfused with ASW of the following composition: 470mM Nacl, 10mM KCI, 10mM Cacl, 50mM MgCl, and 10mM Hepes (pH 7.8). Bath temperature during experiments was approximately 17’0. Individual cells were impaled with two glass microelectrodes (R = 3-10 MÖhms) filled with 3M KCI solution. One microelectrode injected a square current pulse while the other measured the resulting voltage change. Long hyperpolarizing current pulses were administered in order to measure Tau and input resistance. Various neuroactive peptides and amines were applied directly onto the ganglia in dosages that, unless otherwise stated, resulted in a final bath concentration of 2uM. Except where otherwise noted, perfusion was not operating until after observation of the initial gross effects of the applied substances. Perfusion continued at a rate of 1-10cc/min. until the control condition was resumed. Selected cells were then voltage clamped using two microelectrodes similar to those used in the current clamp. One electrode maintained the cell at a constant holding voltage of -40mV, while the other measured the underlying currents resulting from voltage steps from the holding voltage. RESULTS Identification of Autorhythmic Cells We were able to map the dorsal side of the asymmetrical pleural ganglia using morphologhical and electophysiological means of identification. Our map represents a composite of all the individual ganglion observed (Figure 1). Each side of the ganglia yielded a cell with a characteristic bursting pattern. These cells were consistently large and whitish in appearance. LP1 is one of two large cells in the left ganglia located furthest anteriorly. RP2, meanwhile, proves more difficult to locate as there are many large cells in the right ganglia, with seemingly greater variablity amongst individual D. albopunctata. The most reliable characteristic of RP1 is its whitish glow, clearly visible even through the epineural sheath. The beating cell LP2, is typically the largest and most posterior cell in this view of the left pleural ganglia. RP2 resides in a cluster of three cells located most anteriorly in this ganglia, each of which is about half the diameter of the numerous large cells below. Due to the aforementioned ganglia topographic variablity, RP3 was difficult to map, although it is usually a medium sized cell found in the vicinity of the base of the nerve root. FMRF-amide FMRF-amide (Phe-Met-Arg-Phe-NH2) instantaneously depolarized the LP1 burster, converting all bursting activity into tonic spiking activity. (Figure 2B) An input resistance drop from a control of 6.5 MÖhms to 1.5 Möhms was also observed. In the beating LP2 cell, on the other hand, we observed complete inhibition of firing upon peptide application. (Figure 24) Disruption of beating pattern was observed in the rapidly firing RP3 beater. After FMRF-amide application, the constant control spike interval of 800ms fluctuated from 680ms to 960ms. From the appearance of synaptic input during these intervals, we hypothesize that cells presynaptic to RP3 exhibit responses to FMRF-amide that consequently affect RP3. AII FMRF-amide effects on all cells studied were reversible upon perfusion. FMRF-amide and 5-HT A 1:1 ratio of 5-HT and FMRF-amide applied during a 5-HT induced tonic spiking condition in the LP1 burster resulted in an input resistance drop greater than that of 5-HT alone. While 5-HT lowered input resistance from 15.4 MÖhms to 14.4 MÖhms, the input resistance dropped to 10.2 MÖhms with the combination of 5-HT and FMRF-amide. Tau also decreased from a control of 360.6ms to 354.3ms with 5-HT alone, then to a final value of 285.7ms when combined with FMRF-amide. Of particular interest in studying this cell's pharmacology is the evidence for synaptic input after the application of 5-HT amd FMRF-amide. It manifested itself in the form of instantaneous, excitatory bursts, which increased spike frequency whether the cell was in a bursting or beating state. In addition, interburst hyperpolarizations were not smooth, and spikes rose sharply rather than gradually depolarizing. 5-HT Serotonin produced a depolarization in the LPI burster (Figure 3A,B) and the LP2 beater (Figure 4B), exciting both to a high rate of repetetive firing. Voltage clamping of the LP2 beater revealed an insignificant change in inward rectification, although the spike interval decreased from 2.75-3.0s to 1.36s. Clamping of the burster LP1 when exposed to a 5-HT bath concetration of 10 uM, however, revealed a marked decrease in inward rectification of 1.43 nA at -90mV to 89 nA at -60mV. (Figure 8) In the beating cell RP3, 5-HT application also induced a higher rate of repetetive firing, but the response attenuated with successive applications. Spike interval was measured 60s after administration of 5-HT in three separate dosages, with perfusion between each. Following the first application, spike interval dropped dramatically from a control of 3.5s to 0.5s, and thereafter increased progressively to 2.9s and 3.25s in the second and third applications, respectively. (Figure 5-1,2,3) Input resistance measurements showed a gradual increase from 12 MOhms to 21.3 MOhms and 22.0 MÖhms in applications one, two and three, respectively. 5-HT produced a delayed response in cell RP2 (Figure 4A), inhibiting its beating pattern approximately 1.5 min. after application. The original firing pattern did eventually resume. Forskolin and Chlorophenylthio-CAMP (CPT-CAMP) To observe whether any of the applied neuroactive peptides or amines exerted their effects via CAMP, we increased the intracellular levels of CAMP by applying CPT-CAMP, a membrane permeable cyclic AMP analog, and forskolin, a known stimulator of CAMP production. In cell LP1, forskolin inhibited bursting activity and initiated an erratic beating pattern characterized by much synaptic input. (Figure 6) In addition, doublets, triplets and trains of up to five spikes replaced the single spikes in the original bursting condition. The 10 effects of forskolin were long lasting, being visible over an hour after application even though perfusion was at a rate of1Occ/min. Input resistance measurements reflected an increase from 5.25 MÖhms to 7.0 MÖhms upon application of forskolin. Voltage clamp was performed on the burster RP1 in the opposite ganglion. Voltage was stepped from -90mV to -10mV in steps of +10mV, lasting 100ms each. Under these conditions, inward rectification was found to decrease by a maximum of 39.3 at -60mV. CPT-CAMP was then applied to LPI without perfusion. Even after 30 minutes, no effect on bursting activity or input resistance under current clamping conditions was observed. Voltage clamping under conditions identical to that of forskolin, resulted in a negligible change in inward rectification. (Figure 9) CPT-CAMP, then, does not affect LP1, and more importantly does not seem to reproduce the effects of forskolin. Dopamine Dopamine instantaneously inhibited all firing upon application to the beater LP2. (Figure 7B) The beating pattern did eventually recover after perfusion, initially firing at a slower rate and gradually returning to its original condition. The LP1 burster depolarized in reponse to DA, transforming its bursting activity into a fast rate of repetetive firing. (Figure 7A) With perfusion, tonic spiking activity gradually slowed, with an eventual resumption of the bursting pattern. DISCUSSION The responses of the studied autorhythmic cells to each neuroactive peptide and amine were varied, showing no dominant pattern. It seems then, that there are a number of different mechanisms by which individual D. albopunctata cells respond to a substance. This discussion focuses on some of the possible mechanisms by which these cells may operate. Past studies on FMRF-amide have shown that it elucidates a wide spectrum of responses in many different cells. Effects on Aplysia neurons range from a biphasic excitation-inhibition (Ruben, Johnson and Thompson, 1984), to complete inhibition. (Stone and Mayeri, 1981) Furthermore, the giant serotoninergic neuron of the land snail Helix responds to FMRF-amide by first increasing a K+ -current near resting potential, and then reducing a Ca++ and voltage dependent K+-current at more depolarized voltages. (Cottrell, 1982: Cottrell et al., 1984) The LP1 burster and LP2 and RP3 beaters of D. albopunctata that we studied proved to be equally variable in their responses to FMRF-amide. The LP2 beater's hyperpolarizing response can possibly be explained by Ruben, Johnson and Thompson's (1984) reports of an FMRF-amide induced biphasic response in Aplysia burster neurons L4 and L6. In these cells, an inward current increase carried by Na+ ions starts approximately 100-200ms after FMRF-amide application, followed by an outward current increase carried by K+ ions that begins approximately 2-5s after peptide application. Due to the rapid onset of the voltage change induced by the first depolarizing phase of the FMRF-amide response, it could have easily been obscured using our current clamping methodology. But the latter, delayed, hyperpolarizing phase of the peptide response which is easily seen, could feasibly account for the inhibition of firing that was observed in LP2. An increase in outward K+-current could act to keep LP2 in a hyperpolarized, nonfiring state, as well as to counteract any depolarizing stimuli it might have received. Ruben, Johnson and Thompson (1984) also postulate that the presence of two separate ion channels could account for the observed immediate and delayed responses to FMRF-amide. The inward Na--channels that are instantaneously opened possibly involve one set of receptors located at or near the site of peptide application. The outward K+-channels, however, open with a delay time that could be accounted for by the existence of a separate set of receptors located further away from the site of peptide application. The lag time, then, represents the time taken for the FMRF-amide to 15 diffuse from application site to receptor site. Alternatively, the rapidly acting Na--channels could interact indirectly with FMRF-amide, via an intermediate mechanism requiring only a few FMRF-amide molecule interactions to initiate an amplified effect. Here then, many channels could open in a short period of time. The slowly activating K+-channels, though, would interact directly with the FMRF-amide, thereby explaining the lag time. If each individual K+-channel had to interact directly with an FMRF-amide molecule, it would take a reasonable amount of time before enough K+-channels could be opened to produce an observable response. If the LP1 burster were to have only the receptors responsible for the rapidly acting Na--channels, its sole depolarizing response to FMRF-amide could easily be explained. Tentative support for this mechanism lies in the decrease in input resistance observed, which could correspond to an increase in number of open Na--channels. The absence of either of these two possible FMRF-amide receptors on RP3 could account for a lack of a gross depolarizing or hyperpolarizing responses. However, the presence of the FMRF-amide induced erratic beating pattern and synaptic input could feasibly represent the depolarizing or hyperpolarizing responses 16 of cells to FMRF-amide presynaptic to RP3, depending on which of the two posssible FMRF-amide receptors these cells had. An interesting point to notice is the unique effect that the combination of 5-HT and FMRF-amide had on the burster LP1. Applied by themselves, neither induced any synaptic input onto LP1. But together, synaptic input that had not been seen previously , ocurred. What possible mechanism could account for this? Because FMRF-amide and 5-HT both induce depolarizing responses in LP1, they may possibly be acting via the same mechanism, such as the opening of the same inward cation channels. FMRF-amide and 5-HT may not be able to produce a depolarization by themselves in cells presynaptic to LPI that is sufficient to exceed the threshold of these cells, resulting in no transmitter release and therefore no synaptic input. But both FMRF-amide and 5-HT applied together may have the dual effect of depolarizing the presynaptic cells more than either is capable of doing alone, resultingly exceeding threshold and producing the synaptic input seen. 5-HT, like FMRF-amide, also produced various responses in D. albopunctata. The burster LP1, and the beaters LP2 and RP3 exhibited a depolarizing response that is possibly explained by Levitan and Levitan's (1988) proposed mechanism of 5-HT. Levitan and Levitan (1988) found that in the Aplysia burster R15, a 5-HT concentration of 500uM (Tremblay et al., 1976) could act via an increase in CAMP levels to increase the subthreshold calcium current, causing an enhancement of the depolarized phase of the bursting cycle. Although the 5-HT concentrations applied to the cells in our experiments only had a final bath concentration of 2uM, application method was such that 5-HT concentrations exceeding 500uM could have been possible. To test this CAMP mediated increase in LACPT-CAMP was applied to LP2, with no observable response. Therefore, although the depolarizing effects caused by 5-HT in LP2 may still be mediated by an increase in L,,5-HT is not acting via CAMP to produce this response. However, a CAMP mediated depolarization has not yet been ruled out for LPI and RP3, as CPT-CAMP was not applied to these cells. The beating cell RP3 also exhibited a depolarizing response to 5-HT, but differed from LPI and LP2 in that the excitatory response desensitized. The progressive increase in spike interval from the first to the third 5-HT application exhibits this attenuation well. A possible mechanism can be deduced from the observation of a gradually increasing input resistance with each 5-HT application. This is consistent with a gradual inactivation of channels responsible for causing the initial large, depolarizing response. These inactivated channels remained in this state during the second and third 5-HT applications, and so were not available for opening and resultingly depolarizing the cell. Each successive 5-HT application then, represents a progressively decreasing population of inward cation channels available to depolarize RP3. However, another possible mechanism that could account for the desensitzation to 5-HT could lie in downregulation of 5-HT receptors on RP3. No experiments were performed to test either of these hypotheses, and therefore represent only speculations at best. Further work to elucidate the exact mechanism of the 5-HT desensitization observed in RP3 is needed. 5-HT induced a unique response in the beater RP2. After a delay time of approximately one and a half minutes, the cell hyperpolarized and all firing activity was inhibited. A possible mechanism for this response lies in Levitan and Levitan's (1988) finding that in Aplysia R15, 5-HT concentrations at or below 1OuM can act via increasing CAMP levels to increase the inwardly rectifying K+-current. With the resulting increase in K+ conductance, the cell resting potential would be driven 19 to hyperpolarizing voltages near the reversal potential for K+ (around -70my), resulting in an inhibition of cellular activity. The lag time observed before the response, however, could indicate another possible mechanism involving either Cl- channels or a different set of K+-channels located far away from the site of 5-HT application, which do not operate via CAMP. These are only suggested mechanisms, as we did not perform any voltage clamp or CAMP analog experiments, and therefore cannot be sure that 5-HT does actually act through CAMP to affect the inwardly rectifying K+-current. The results of the CPT-CAMP and forskolin applications indicated that none of the applied neuroactive peptides or amines operate using cAMP as an intermediate. In addition, it appears that although forskolin is a stimulator of CAMP production, the effects resulting from its application are due to mechanisms other than increased levels of CAMP. In LP1, forskolin caused a number of effects that did not resemble any of the responses of the other applied neuroactive peptides and amines, giving the first indication that these substances did not operate via a CAMP intermediate. Evidence for a possible mechanism underlying the various responses to forskolin lies in the 20 observation of an increase in input resistance following application. This corresponds well with Coombs and Thompson's (1987) finding that forskolin acts on certain D. albopunctata neurons to close transient K+-channels. Closure of K+-channels would depolarize the cell, and could resultingly contribute to the creation of a new resting potential that exceeds the thresholds of the multiple spike initiating zones located at various points along the axon; or possibly the single spike initiating zones on multiple axons extending from the soma. If this depolarization effect were to occur, trains of spikes would result that were in fact observed upon application of forskolin. The decrease in inward rectification seen under voltage clamp could add to the decreased K+ conductance, assuming that this current was carried mostly by K+ ions. This in turn, would act to depolarize LP1 still further, thus providing even more feasibility for the multiple spikes. The decrease in the transient K+- current that Coombs and Thompson (1987) described could also provide a mechanism by which a number of other effects of forskolin acted. Because is active at subthreshold voltages, it exerts its main effects not on changing spike shape, but on slowing the rate of repetetive firing and controlling spike interval. Therefore, it is reasonable to 21 conclude that if 1is blocked, the effects will be manifested in an increase in repetetive firing as well as erratic spike intervals, which are in fact the effects forskolin induced. Finally, forskolin has been found to cause an increase in an inward cation current near resting potential in a number of nudibranchs.(Coombs and Thompson, 19871 Although this response may contribute to the depolarization of the resting potential and the multiple spikes mentioned earlier, it could also be responsible for the great deal of synaptic input that was observed in LP1. This synaptic input might be the effects of forskolin activating the inward cation current in cells presynaptic to LPI. Because forskolin is a known activator of adenylate cyclase, an increase in cAMP levels is one of the most feasible mechanisms by which it could exert its effects on LP1. To test whether CAMP did serve as an intermediate, we applied CPT-CAMP, a membrane permeable analog of cAMP that would produce effects in LP1 that could be the result of a sole increase in cAMF concentration. Under current and voltage clamping conditions, no effects of CPT-CAMP were observed giving strong evidence that forskolin does not act via CAMP levels, but instead via changes in 1, as suggested 22 earlier. Dopamine proved to exhibit responses that were as variable as those that our other amine, 5-HT, had produced. The inhibitory response shown by LP2 can possibly be explained by the finding that DA has been shown to cause a decrease in the subthreshold Ca++ current in Aplysia R15. (Lewis, et al., 1984) A decrease in Ca++ -current could greatly hinder LP2's ability to fire a spike, as in molluscan neurons, the upstroke of the action potential consists of a combination of Ca+ and Na-- currents. If the Ca+--current is eliminated, opening of Na--channels only may not produce sufficient depolarization to produce a spike. Even more significant is that the Ca++- current operates mainly at subthreshold voltages, and consequently has great power in determining if a cell will reach threshold. If the lgis decreased enough, the cell will never depolarize to the point where enough Na--channels are activated to initiate an action potential. As a result all firing activity will be inhibited, which is in fact what the LP2 response was. The LP1 burster responded to DA by shifting from its bursting pattern to a high frequency tonic firing pattern. In Aplysia R15, the same decrease in L just mentioned acts to increase the interburst hyperpolarization, and at 23 times to stop all bursting activity altogether. (Äscher, 1972) As this reported response is directly contrary to the depolarizing response observed, it seems safe to say that DA is not exerting its effects here via 1-Although DA may be acting to increase an inward cation conductance in LP1, it is hard to say anything about the underlying mechanisms, as the change in firing pattern is all the data that could be collected in this experiment. Doriopsilla albopunctata neurons show a wide spectrum of responses to the various neuroactive peptides and amines applied to them. Although we have just barely scratched the surface of the pharmacology of these various cells, we hope that we have sparked an interest in this useful animal for further studies. As some of the observed responses were unexplainable by traditional mechanisms, elucidation of the exact mechanisms by which the cells responded will serve to enhance knowledge of neuropharmacology immensely. FIGURE LEGEND Fig.1. Map of the dorsal pleural ganglia of Doriopsilla albopunctata. Fig.2. A. FMRF-amide causes inhibition of beating activity in LP2. FMRF-amide transforms LPI bursting pattern into a beating pattern. Bursting activity Fig.3. A,B. 5-HT depolarizes LPI. converted into a high rate of repetetive firing. Fig.4. A. 5-HT has a delayed response on RP2, eventually inhibiting its beating pattern. B. 5-HT excites LP2, increasing its rate of firing. Fig.5. 5-HT induces a higher rate of repetetive firing in RP3, The response attenuates with repeated applications. Arrows represent spike interval measurements 60s after 5-HT application in trials 1,2, and 3. 1. spike interval.5s 2. spike interval 2.9s 3. spike interval 3.25s Effects of forskolin on LPl. Note multiple spikes, Fig.6. erratic beating pattern and synaptic input. Fig.7. A. DA transforms LPI bursting activity into a high rate of repetetive firing. B. DA inhibits firing in LP2. Fig.8. 5-HT causes an increase in inward rectification in LPI. Fig.9. CPT-cAMP causes no significant change in inward rectification in LPl. Fig.10. Summary of autorhythmic neuron responses to applied chemical substances. Fig.11. The varied bursting cycles of RPl and LP1. FIGURE 1 JRP2 S2 Doglees,aalata ew ALPORNCTAT 8 o 8 A NA o NA FIGURE 10 VAS FMRE A DA t c07 CAMI SAT — FNRF+ 54T LPI + O + RPI 70 +++ + ++ ++ O ++ LP2 —— —— + RP2 — RP3 + P C REFERENCES Adams, D.J., S.J. Smith, J.H. Thompson, 1980, lonic currents in molluscan soma, Ann. Rev. Neurosci. J. 141-167. Andesirk, G., 1985, Amine-containing neurons in the brain of Lymnaea stagnalis: Distribution and effects of precursors, Comp. Biochem. Physiol., 814(2), 359-365. 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Barondes, 1976, Dopamine, serotonin and related compounds: Presynaptic effects on synaptic depression, frequency facilitation, and post-tetanic potentiation at a synapse in Aplysia californica Brain Res., 109, 61-81. ACKNOVLEDGEMENTS I would like to thank my advisor, Stuart Thompson, as this project vould not have been possible without his support and quidance. In addition, I would like to thank Ion Ctis, Tony Morielli and Brett Premack for their heln and advice, Finally, areat thanks go to my partner, Scott Forrison, for being a great research covorker, d super buddy, and a wonderfully tolerant person who was always willing to put un with my alleded moodiness.